Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

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 Smiles

 DOI
187 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
8593 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 255 39 None -1 8 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
2551 794 23 None -27 13 Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 794 23 None -27 13 Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 794 23 None -27 13 Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 794 23 None -27 13 Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 794 23 None -27 13 Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
334 236 27 None -24 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
9928284 236 27 None -24 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
CHEMBL2022960 236 27 None -24 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
25199525 16081 0 None -39 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223807 16081 0 None -39 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25207745 16126 0 None -100 5 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 16126 0 None -100 5 Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
17516658 53622 5 None - 1 Human 5.0 pEC50 = 5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1 10.1021/jm500995y
CHEMBL1602658 53622 5 None - 1 Human 5.0 pEC50 = 5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1 10.1021/jm500995y
3257 4028 61 None -1047 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2009.11.089
42633508 4028 61 None -1047 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2009.11.089
CHEMBL466253 4028 61 None -1047 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2009.11.089
71737628 114206 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329738 114206 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737628 114206 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329738 114206 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
3257 4028 61 None -1047 2 Human 5.9 pEC50 = 5.9 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm900286j
42633508 4028 61 None -1047 2 Human 5.9 pEC50 = 5.9 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm900286j
CHEMBL466253 4028 61 None -1047 2 Human 5.9 pEC50 = 5.9 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm900286j
24967746 16055 0 None -31 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 16055 0 None -31 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
118712536 114226 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329764 114226 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
118712537 114227 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1 10.1021/jm500995y
CHEMBL3329765 114227 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1 10.1021/jm500995y
118712537 114227 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1 10.1021/jm500995y
CHEMBL3329765 114227 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1 10.1021/jm500995y
44208359 16705 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
CHEMBL1242979 16705 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
306 3456 21 None -3 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3536 3456 21 None -3 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
53930639 3456 21 None -3 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
9577995 3456 21 None -3 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
CHEMBL134641 3456 21 None -3 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
118712536 114226 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329764 114226 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
42599068 16079 0 None -39 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 16079 0 None -39 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598359 16106 0 None -100 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 16106 0 None -100 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16123945 80459 12 None -251 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
CHEMBL2146599 80459 12 None -251 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
71771056 114224 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329762 114224 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
3652 4097 79 None -263 15 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4097 79 None -263 15 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4097 79 None -263 15 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4097 79 None -263 15 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4097 79 None -263 15 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
118712538 114228 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1 10.1021/jm500995y
CHEMBL3329766 114228 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1 10.1021/jm500995y
118712538 114228 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1 10.1021/jm500995y
CHEMBL3329766 114228 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1 10.1021/jm500995y
139414008 164361 0 None -10 3 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of M5 receptor (unknown origin)Positive allosteric modulation of M5 receptor (unknown origin)
ChEMBL 346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4212760 164361 0 None -10 3 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of M5 receptor (unknown origin)Positive allosteric modulation of M5 receptor (unknown origin)
ChEMBL 346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
71771056 114224 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329762 114224 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
3652 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
3652 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
57 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
60809 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
CHEMBL21536 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
DB15357 4097 79 None -263 15 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
118712535 114225 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329763 114225 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
46945663 17542 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 432 5 0 5 4.6 O=C1C(=O)N(Cc2ccc(Oc3cccc(F)n3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257975 17542 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 432 5 0 5 4.6 O=C1C(=O)N(Cc2ccc(Oc3cccc(F)n3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737627 114210 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329743 114210 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
118712535 114225 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329763 114225 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
71737627 114210 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329743 114210 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71771058 114221 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329756 114221 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
71737578 114200 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329730 114200 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
42598828 16103 0 None -125 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 16103 0 None -125 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598360 16104 0 None -63 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 16104 0 None -63 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 16125 0 None -63 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 16125 0 None -63 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44204999 63817 6 None -31 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1 10.1021/ml100105x
CHEMBL1802360 63817 6 None -31 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1 10.1021/ml100105x
71771058 114221 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329756 114221 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
52947398 17358 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3cccnc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257388 17358 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3cccnc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
45281794 199731 49 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL593506 199731 49 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737578 114200 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329730 114200 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
71737646 114212 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329745 114212 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737646 114212 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329745 114212 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737611 114201 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329731 114201 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
135409468 2035 69 None -3 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2035 69 None -3 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2035 69 None -3 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
44158075 178811 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1cccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1 10.1021/jm900286j
CHEMBL469144 178811 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1cccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1 10.1021/jm900286j
71737611 114201 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329731 114201 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71771053 114222 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329757 114222 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
118712534 114223 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1 10.1021/jm500995y
CHEMBL3329760 114223 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1 10.1021/jm500995y
71771053 114222 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329757 114222 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
118712534 114223 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1 10.1021/jm500995y
CHEMBL3329760 114223 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1 10.1021/jm500995y
44158221 172108 0 None 3 2 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 389 3 0 3 4.3 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
CHEMBL447265 172108 0 None 3 2 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 389 3 0 3 4.3 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
44157243 187494 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 405 4 0 4 4.2 O=C1C(=O)N(Cc2ccc(OC(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
CHEMBL494190 187494 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 405 4 0 4 4.2 O=C1C(=O)N(Cc2ccc(OC(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
187 255 39 None -1 8 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
294 255 39 None -1 8 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
65 255 39 None -1 8 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
8593 255 39 None -1 8 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL667 255 39 None -1 8 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
DB03128 255 39 None -1 8 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
42598591 16077 0 None -39 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223803 16077 0 None -39 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599070 16078 0 None -50 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 16078 0 None -50 5 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
71737672 2576 19 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2576 19 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2576 19 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
44602489 201368 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL604482 201368 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
44157160 178783 3 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 333 2 0 2 3.3 O=C1C(=O)N(Cc2ccc(Br)cc2)c2c(F)cccc21 10.1021/jm900286j
CHEMBL468925 178783 3 None 2 2 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 333 2 0 2 3.3 O=C1C(=O)N(Cc2ccc(Br)cc2)c2c(F)cccc21 10.1021/jm900286j
71737672 2576 19 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2576 19 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2576 19 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
44158142 188670 43 None 1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
CHEMBL503735 188670 43 None 1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
52947457 17398 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cncnc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257498 17398 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cncnc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737647 114211 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329744 114211 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
44158142 188670 43 None 1 4 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL503735 188670 43 None 1 4 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
71737647 114211 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329744 114211 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
46945864 17575 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 444 6 0 6 4.5 COc1cccc(Oc2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)n1 10.1016/j.bmcl.2010.08.042
CHEMBL1258090 17575 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 444 6 0 6 4.5 COc1cccc(Oc2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)n1 10.1016/j.bmcl.2010.08.042
71737606 114199 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1 10.1021/jm500995y
CHEMBL3329729 114199 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1 10.1021/jm500995y
52950176 17399 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 356 3 0 4 3.4 O=C1C(=O)N(Cc2ccc(Cl)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257499 17399 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 356 3 0 4 3.4 O=C1C(=O)N(Cc2ccc(Cl)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737606 114199 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1 10.1021/jm500995y
CHEMBL3329729 114199 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1 10.1021/jm500995y
25010776 55955 2 None -11 5 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
CHEMBL1559151 55955 2 None -11 5 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
CHEMBL1624037 55955 2 None -11 5 Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
71737645 114213 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329746 114213 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737645 114213 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329746 114213 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
45281794 199731 49 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL593506 199731 49 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
45281808 200052 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2009.11.089
CHEMBL595628 200052 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2009.11.089
45281797 201184 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 403 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccsc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL603445 201184 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 403 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccsc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
76313419 103265 0 None -69 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1 10.1016/j.bmcl.2012.03.088
CHEMBL3084447 103265 0 None -69 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1 10.1016/j.bmcl.2012.03.088
52949833 17359 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccncc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257389 17359 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccncc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
46945865 17576 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 420 5 0 6 4.6 O=C1C(=O)N(Cc2ccc(Oc3nccs3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1258091 17576 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 420 5 0 6 4.6 O=C1C(=O)N(Cc2ccc(Oc3nccs3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71771054 114202 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1 10.1021/jm500995y
CHEMBL3329732 114202 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1 10.1021/jm500995y
71771054 114202 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1 10.1021/jm500995y
CHEMBL3329732 114202 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1 10.1021/jm500995y
71737574 114198 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1 10.1021/jm500995y
CHEMBL3329717 114198 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1 10.1021/jm500995y
52941424 17439 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cn2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257619 17439 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cn2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737574 114198 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1 10.1021/jm500995y
CHEMBL3329717 114198 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1 10.1021/jm500995y
42599071 16124 0 None -125 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 16124 0 None -125 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
10946670 189176 3 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 305 2 0 2 3.4 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccccc21 10.1021/jm900286j
CHEMBL511206 189176 3 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 305 2 0 2 3.4 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccccc21 10.1021/jm900286j
52943684 17293 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 365 3 0 5 3.0 O=C1C(=O)N(Cc2ccc3c(c2)OCO3)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257151 17293 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 365 3 0 5 3.0 O=C1C(=O)N(Cc2ccc3c(c2)OCO3)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
46945664 17541 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 414 5 0 5 4.5 O=C1C(=O)N(Cc2ccc(Oc3ccccn3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257974 17541 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 414 5 0 5 4.5 O=C1C(=O)N(Cc2ccc(Oc3ccccn3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
44158139 178704 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(F)cccc21 10.1021/jm900286j
CHEMBL468290 178704 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(F)cccc21 10.1021/jm900286j
44158003 188808 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 335 3 0 3 3.6 Cc1ccccc1CN1C(=O)C(=O)c2cc(OC(F)(F)F)ccc21 10.1021/jm900286j
CHEMBL506043 188808 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 335 3 0 3 3.6 Cc1ccccc1CN1C(=O)C(=O)c2cc(OC(F)(F)F)ccc21 10.1021/jm900286j
45281803 200170 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 401 4 0 5 3.7 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)cn1 10.1016/j.bmcl.2009.11.089
CHEMBL596510 200170 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 401 4 0 5 3.7 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)cn1 10.1016/j.bmcl.2009.11.089
26415265 114197 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1 10.1021/jm500995y
CHEMBL3329716 114197 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1 10.1021/jm500995y
26415265 114197 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1 10.1021/jm500995y
CHEMBL3329716 114197 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1 10.1021/jm500995y
44589681 185288 0 None -3 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485913 185288 0 None -3 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
22745278 187063 1 None -16 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491209 187063 1 None -16 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
71737709 114220 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329754 114220 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
71737709 114220 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329754 114220 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
45281801 200169 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 416 4 0 4 4.5 O=C1C(=O)N(Cc2ccc(-c3ccc(F)nc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL596509 200169 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 416 4 0 4 4.5 O=C1C(=O)N(Cc2ccc(-c3ccc(F)nc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
53385782 74313 0 None -117 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024331 74313 0 None -117 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
46945662 17477 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257741 17477 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
45281796 200013 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 427 5 0 4 5.0 COc1ccccc1-c1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2009.11.089
CHEMBL595403 200013 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 427 5 0 4 5.0 COc1ccccc1-c1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2009.11.089
44157241 189187 3 None 1 2 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 301 3 0 3 3.1 COc1ccc(CN2C(=O)C(=O)c3cccc(Cl)c32)cc1 10.1021/jm900286j
CHEMBL511254 189187 3 None 1 2 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 301 3 0 3 3.1 COc1ccc(CN2C(=O)C(=O)c3cccc(Cl)c32)cc1 10.1021/jm900286j
42598829 16080 0 None -50 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223806 16080 0 None -50 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598357 16105 0 None -125 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223863 16105 0 None -125 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
52949292 17512 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cccnc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257862 17512 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cccnc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
44157714 189421 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 355 3 0 3 4.0 O=C1C(=O)N(Cc2ccccc2Cl)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
CHEMBL513299 189421 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 355 3 0 3 4.0 O=C1C(=O)N(Cc2ccccc2Cl)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
3008304 4023 52 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
7632 4023 52 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
CHEMBL523685 4023 52 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
44158077 178597 1 None 1 2 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccccc2C(F)(F)F)c2ccc(F)cc21 10.1021/jm900286j
CHEMBL467281 178597 1 None 1 2 Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccccc2C(F)(F)F)c2ccc(F)cc21 10.1021/jm900286j
3008304 4023 52 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
7632 4023 52 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
CHEMBL523685 4023 52 None 1 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
76324306 103267 0 None -61 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 379 6 2 4 2.5 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2012.03.088
CHEMBL3084449 103267 0 None -61 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 379 6 2 4 2.5 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2012.03.088
71792 78406 38 None 1 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
CHEMBL2111051 78406 38 None 1 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
52941977 17513 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3ccncc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257863 17513 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3ccncc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
3008304 4023 52 None 1 4 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
7632 4023 52 None 1 4 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
CHEMBL523685 4023 52 None 1 4 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
13248082 187620 5 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 367 2 0 2 4.0 O=C1C(=O)N(Cc2ccc(Br)cc2F)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL494846 187620 5 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 367 2 0 2 4.0 O=C1C(=O)N(Cc2ccc(Br)cc2F)c2c(Cl)cccc21 10.1021/jm900286j
644390 40412 6 None -1 4 Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
CHEMBL1482157 40412 6 None -1 4 Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
71737648 114218 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329751 114218 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737648 114218 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329751 114218 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
45281798 200138 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 432 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccc(Cl)nc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL596289 200138 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 432 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccc(Cl)nc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
42598358 16102 0 None -50 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 16102 0 None -50 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598586 16123 0 None -25 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 16123 0 None -25 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
71737683 114219 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329752 114219 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737683 114219 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329752 114219 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
45281807 200014 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(CN2C(=O)C(=O)c3ccc(OC(F)(F)F)cc32)cc1 10.1016/j.bmcl.2009.11.089
CHEMBL595404 200014 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(CN2C(=O)C(=O)c3ccc(OC(F)(F)F)cc32)cc1 10.1016/j.bmcl.2009.11.089
52940924 17141 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 415 4 0 3 5.1 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2F)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1255607 17141 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 415 4 0 3 5.1 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2F)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737672 2576 19 None 1 6 Rat 6.2 pEC50 = 6.2 Functional
Activity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2576 19 None 1 6 Rat 6.2 pEC50 = 6.2 Functional
Activity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2576 19 None 1 6 Rat 6.2 pEC50 = 6.2 Functional
Activity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
26415263 114196 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1021/jm500995y
CHEMBL3329715 114196 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1021/jm500995y
26415263 114196 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1021/jm500995y
CHEMBL3329715 114196 3 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1021/jm500995y
187 255 39 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
294 255 39 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
65 255 39 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
8593 255 39 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL667 255 39 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB03128 255 39 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
44418764 82159 0 None -2 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 82159 0 None -2 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
71737675 114217 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329750 114217 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737675 114217 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329750 114217 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
650899 54414 11 None -23 5 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 54414 11 None -23 5 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 54414 11 None -23 5 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
11056389 189388 0 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(F)cc21 10.1021/jm900286j
CHEMBL512977 189388 0 None 1 2 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(F)cc21 10.1021/jm900286j
44158005 189425 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 335 3 0 3 3.7 COc1cccc(CN2C(=O)C(=O)c3c(Cl)ccc(Cl)c32)c1 10.1021/jm900286j
CHEMBL513311 189425 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 335 3 0 3 3.7 COc1cccc(CN2C(=O)C(=O)c3c(Cl)ccc(Cl)c32)c1 10.1021/jm900286j
71737624 114207 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329739 114207 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737624 114207 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329739 114207 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737617 114209 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329741 114209 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737760 114203 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1 10.1021/jm500995y
CHEMBL3329734 114203 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1 10.1021/jm500995y
71737617 114209 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329741 114209 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737760 114203 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1 10.1021/jm500995y
CHEMBL3329734 114203 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1 10.1021/jm500995y
71737763 114216 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329749 114216 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737618 114208 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329740 114208 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737763 114216 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329749 114216 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737618 114208 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329740 114208 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
16071018 16054 20 None -125 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223753 16054 20 None -125 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
16071018 16054 20 None -125 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL1223753 16054 20 None -125 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
71737681 114214 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329747 114214 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737677 114215 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329748 114215 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737681 114214 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329747 114214 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737677 114215 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329748 114215 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
647412 27319 9 None -6 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
CHEMBL1367424 27319 9 None -6 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
2551 794 23 None -27 13 Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
298 794 23 None -27 13 Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
488 794 23 None -27 13 Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL965 794 23 None -27 13 Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB00411 794 23 None -27 13 Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
71737619 114205 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329737 114205 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737619 114205 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329737 114205 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737602 114204 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329736 114204 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737602 114204 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329736 114204 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
2551 794 23 None -27 13 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 794 23 None -27 13 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 794 23 None -27 13 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 794 23 None -27 13 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 794 23 None -27 13 Human 5.9 pED50 = 5.9 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
5487543 205646 4 None -64 6 Human 5.2 pED50 = 5.2 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
CHEMBL81878 205646 4 None -64 6 Human 5.2 pED50 = 5.2 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
9795428 96488 5 None -20 5 Human 6.1 pED50 = 6.1 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
CHEMBL262455 96488 5 None -20 5 Human 6.1 pED50 = 6.1 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M5 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
168299773 192669 0 None 10 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 457 4 1 7 2.7 Cn1ncc(S(=O)(=O)N2CC[C@H](C(=O)Nc3ccc4scnc4c3)[C@@H](F)C2)c1Cl 10.1016/j.bmcl.2022.128988
CHEMBL5218711 192669 0 None 10 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 457 4 1 7 2.7 Cn1ncc(S(=O)(=O)N2CC[C@H](C(=O)Nc3ccc4scnc4c3)[C@@H](F)C2)c1Cl 10.1016/j.bmcl.2022.128988
71607130 104680 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 424 2 0 2 4.4 O=C(c1cc(F)cc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
CHEMBL3105212 104680 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 424 2 0 2 4.4 O=C(c1cc(F)cc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
118719486 115546 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 452 2 0 4 3.6 O=C(c1cc(F)c(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2 10.1016/j.bmcl.2014.11.082
CHEMBL3353274 115546 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 452 2 0 4 3.6 O=C(c1cc(F)c(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2 10.1016/j.bmcl.2014.11.082
137638270 156877 0 None -8 5 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M5 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M5 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4071900 156877 0 None -8 5 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M5 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M5 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
71598521 2575 16 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
7631 2575 16 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
CHEMBL3105228 2575 16 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
71607097 104675 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105208 104675 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
162523027 192673 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 416 4 1 6 3.0 Cc1ccc(S(=O)(=O)N2CCC(C(=O)Nc3ccc4scnc4c3)CC2)cn1 10.1016/j.bmcl.2022.128988
CHEMBL5218928 192673 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 416 4 1 6 3.0 Cc1ccc(S(=O)(=O)N2CCC(C(=O)Nc3ccc4scnc4c3)CC2)cn1 10.1016/j.bmcl.2022.128988
71607097 104675 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105208 104675 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
162523004 192664 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 457 4 1 6 3.8 CC1COc2ccc(S(=O)(=O)N3CCC(C(=O)Nc4ccc5scnc5c4)CC3)cc21 10.1016/j.bmcl.2022.128988
CHEMBL5218597 192664 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 457 4 1 6 3.8 CC1COc2ccc(S(=O)(=O)N3CCC(C(=O)Nc4ccc5scnc5c4)CC3)cc21 10.1016/j.bmcl.2022.128988
168295434 192349 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 409 5 0 7 2.4 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5207053 192349 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 409 5 0 7 2.4 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1 10.1021/acs.jmedchem.2c00192
168295434 192349 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 409 5 0 7 2.4 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5207053 192349 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 409 5 0 7 2.4 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1 10.1021/acs.jmedchem.2c00192
24882532 95117 0 None -2 4 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255523 95117 0 None -2 4 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
118719495 115554 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 456 4 0 5 4.0 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2014.11.082
CHEMBL3353283 115554 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 456 4 0 5 4.0 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2014.11.082
71598549 104681 1 None -2 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
CHEMBL3105213 104681 1 None -2 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
162523114 192710 0 None 2 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 443 4 1 6 3.3 O=C(Nc1ccc2scnc2c1)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2022.128988
CHEMBL5219691 192710 0 None 2 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 443 4 1 6 3.3 O=C(Nc1ccc2scnc2c1)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2022.128988
71598521 2575 16 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
7631 2575 16 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
CHEMBL3105228 2575 16 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
137654353 159016 0 None -3 6 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human M5 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M5 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 159016 0 None -3 6 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human M5 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M5 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
168275716 190218 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 5 0 6 2.9 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)CCCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5174730 190218 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 5 0 6 2.9 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)CCCO3)CC1 10.1021/acs.jmedchem.2c00192
168275716 190218 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 5 0 6 2.9 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)CCCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5174730 190218 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 5 0 6 2.9 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)CCCO3)CC1 10.1021/acs.jmedchem.2c00192
134824563 156046 14 None 1 2 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
CHEMBL4062497 156046 14 None 1 2 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
168273459 190103 0 None 23 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 6 0 6 3.0 CCn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5172903 190103 0 None 23 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 6 0 6 3.0 CCn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
168273459 190103 0 None 23 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 6 0 6 3.0 CCn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5172903 190103 0 None 23 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 6 0 6 3.0 CCn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
134824563 156046 14 None 1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1021/acs.jmedchem.2c00192
CHEMBL4062497 156046 14 None 1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1021/acs.jmedchem.2c00192
134824563 156046 14 None 1 2 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
CHEMBL4062497 156046 14 None 1 2 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
118719480 115540 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 3 0 3 4.1 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1C 10.1016/j.bmcl.2014.11.082
CHEMBL3353268 115540 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 3 0 3 4.1 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1C 10.1016/j.bmcl.2014.11.082
168283348 190790 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 427 5 0 6 1.5 Cn1ccnc1[S+]([O-])C[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
CHEMBL5183573 190790 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 427 5 0 6 1.5 Cn1ccnc1[S+]([O-])C[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
168283348 190790 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 427 5 0 6 1.5 Cn1ccnc1[S+]([O-])C[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
CHEMBL5183573 190790 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 427 5 0 6 1.5 Cn1ccnc1[S+]([O-])C[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
164673826 192174 7 None -57 4 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat muscarinic M5 receptorAntagonist activity at rat muscarinic M5 receptor
ChEMBL 411 5 0 6 2.5 Cn1ccnc1SC[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
CHEMBL5204021 192174 7 None -57 4 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat muscarinic M5 receptorAntagonist activity at rat muscarinic M5 receptor
ChEMBL 411 5 0 6 2.5 Cn1ccnc1SC[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
137658629 159371 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 473 4 0 3 4.8 CN(c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1)C1CCC1 10.1016/j.bmcl.2017.02.020
CHEMBL4100518 159371 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 473 4 0 3 4.8 CN(c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1)C1CCC1 10.1016/j.bmcl.2017.02.020
71607117 104682 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
CHEMBL3105215 104682 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
168298068 192658 0 None 23 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 440 4 1 7 3.0 Cc1ncc(S(=O)(=O)N2CC[C@H](C(=O)Nc3ccc4scnc4c3)[C@@H](F)C2)s1 10.1016/j.bmcl.2022.128988
CHEMBL5218449 192658 0 None 23 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 440 4 1 7 3.0 Cc1ncc(S(=O)(=O)N2CC[C@H](C(=O)Nc3ccc4scnc4c3)[C@@H](F)C2)s1 10.1016/j.bmcl.2022.128988
3156646 8264 9 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M5 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1092460 8264 9 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M5 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
71607117 104682 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
CHEMBL3105215 104682 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
118719477 115537 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 2 0 4 3.5 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2 10.1016/j.bmcl.2014.11.082
CHEMBL3353265 115537 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 2 0 4 3.5 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2 10.1016/j.bmcl.2014.11.082
118719483 115544 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 3 0 3 4.1 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1C 10.1016/j.bmcl.2014.11.082
CHEMBL3353271 115544 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 3 0 3 4.1 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1C 10.1016/j.bmcl.2014.11.082
118719498 115557 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 456 5 0 4 4.6 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)cc1C 10.1016/j.bmcl.2014.11.082
CHEMBL3353286 115557 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 456 5 0 4 4.6 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)cc1C 10.1016/j.bmcl.2014.11.082
118719499 115558 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 460 5 0 4 4.4 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)ccc1F 10.1016/j.bmcl.2014.11.082
CHEMBL3353287 115558 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 460 5 0 4 4.4 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)ccc1F 10.1016/j.bmcl.2014.11.082
71737771 116482 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 420 3 0 3 3.8 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2014.11.082
CHEMBL3361328 116482 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 420 3 0 3 3.8 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2014.11.082
44455159 97765 0 None -11 5 Rat 4.9 pIC50 = 4.9 Functional
Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL271704 97765 0 None -11 5 Rat 4.9 pIC50 = 4.9 Functional
Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
71737771 116482 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 420 3 0 3 3.8 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2014.11.082
CHEMBL3361328 116482 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 420 3 0 3 3.8 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2014.11.082
137658629 159371 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 473 4 0 3 4.8 CN(c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1)C1CCC1 10.1016/j.bmcl.2017.02.020
CHEMBL4100518 159371 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 473 4 0 3 4.8 CN(c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1)C1CCC1 10.1016/j.bmcl.2017.02.020
162523094 192674 0 None -4 2 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat muscarinic M5 receptorAntagonist activity at rat muscarinic M5 receptor
ChEMBL 419 4 1 7 2.4 Cc1nn(C)cc1S(=O)(=O)N1CCC(C(=O)Nc2ccc3scnc3c2)CC1 10.1016/j.bmcl.2022.128988
CHEMBL5218950 192674 0 None -4 2 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat muscarinic M5 receptorAntagonist activity at rat muscarinic M5 receptor
ChEMBL 419 4 1 7 2.4 Cc1nn(C)cc1S(=O)(=O)N1CCC(C(=O)Nc2ccc3scnc3c2)CC1 10.1016/j.bmcl.2022.128988
168298989 192749 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 457 4 1 6 3.7 C[C@@H]1C[C@H](C(=O)Nc2ccc3scnc3c2)CCN1S(=O)(=O)c1ccc2c(c1)CCO2 10.1016/j.bmcl.2022.128988
CHEMBL5220906 192749 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 457 4 1 6 3.7 C[C@@H]1C[C@H](C(=O)Nc2ccc3scnc3c2)CCN1S(=O)(=O)c1ccc2c(c1)CCO2 10.1016/j.bmcl.2022.128988
71607066 104670 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 454 3 0 3 5.1 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105203 104670 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 454 3 0 3 5.1 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
168272920 190101 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 402 5 0 6 3.2 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3ncccc3c2)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5172889 190101 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 402 5 0 6 3.2 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3ncccc3c2)CC1 10.1021/acs.jmedchem.2c00192
71607066 104670 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 454 3 0 3 5.1 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105203 104670 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 454 3 0 3 5.1 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
168272920 190101 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 402 5 0 6 3.2 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3ncccc3c2)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5172889 190101 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 402 5 0 6 3.2 Cn1ccnc1SCC1CCN(S(=O)(=O)c2ccc3ncccc3c2)CC1 10.1021/acs.jmedchem.2c00192
118719488 115547 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 472 3 0 3 4.6 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1Cl 10.1016/j.bmcl.2014.11.082
CHEMBL3353276 115547 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 472 3 0 3 4.6 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1Cl 10.1016/j.bmcl.2014.11.082
162523010 192668 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 444 4 1 7 2.7 O=C(Nc1ccc2snnc2c1)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2022.128988
CHEMBL5218709 192668 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 444 4 1 7 2.7 O=C(Nc1ccc2snnc2c1)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2022.128988
137631491 156291 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCC(F)(F)C2)cc1 10.1016/j.bmcl.2017.02.020
CHEMBL4065335 156291 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCC(F)(F)C2)cc1 10.1016/j.bmcl.2017.02.020
137641540 158112 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 541 3 0 3 5.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCCC2C(F)(F)F)cc1 10.1016/j.bmcl.2017.02.020
CHEMBL4086766 158112 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 541 3 0 3 5.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCCC2C(F)(F)F)cc1 10.1016/j.bmcl.2017.02.020
137631491 156291 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCC(F)(F)C2)cc1 10.1016/j.bmcl.2017.02.020
CHEMBL4065335 156291 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCC(F)(F)C2)cc1 10.1016/j.bmcl.2017.02.020
168297098 192508 0 None 9 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 5 0 6 2.9 CC(Sc1nccn1C)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5209198 192508 0 None 9 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 5 0 6 2.9 CC(Sc1nccn1C)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
168297098 192508 0 None 9 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 5 0 6 2.9 CC(Sc1nccn1C)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5209198 192508 0 None 9 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 407 5 0 6 2.9 CC(Sc1nccn1C)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
168298923 192689 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 457 4 1 6 3.5 C[C@H]1CN(S(=O)(=O)c2ccc3c(c2)CCO3)CC[C@@H]1C(=O)Nc1ccc2scnc2c1 10.1016/j.bmcl.2022.128988
CHEMBL5219222 192689 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 457 4 1 6 3.5 C[C@H]1CN(S(=O)(=O)c2ccc3c(c2)CCO3)CC[C@@H]1C(=O)Nc1ccc2scnc2c1 10.1016/j.bmcl.2022.128988
118719491 115550 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 472 3 0 3 4.6 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2014.11.082
CHEMBL3353279 115550 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 472 3 0 3 4.6 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2014.11.082
118724901 116481 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 420 3 0 3 3.8 COc1cccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)c1 10.1016/j.bmcl.2014.11.082
CHEMBL3361327 116481 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 420 3 0 3 3.8 COc1cccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)c1 10.1016/j.bmcl.2014.11.082
134824563 156046 14 None -1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of rat M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
CHEMBL4062497 156046 14 None -1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of rat M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
118724901 116481 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 420 3 0 3 3.8 COc1cccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)c1 10.1016/j.bmcl.2014.11.082
CHEMBL3361327 116481 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 420 3 0 3 3.8 COc1cccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)c1 10.1016/j.bmcl.2014.11.082
134824563 156046 14 None -1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of rat M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
CHEMBL4062497 156046 14 None -1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of rat M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
162523110 192704 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 436 4 1 6 3.4 O=C(Nc1ccc2scnc2c1)C1CCN(S(=O)(=O)c2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2022.128988
CHEMBL5219539 192704 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 436 4 1 6 3.4 O=C(Nc1ccc2scnc2c1)C1CCN(S(=O)(=O)c2ccc(Cl)nc2)CC1 10.1016/j.bmcl.2022.128988
137640100 156810 14 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
CHEMBL4071136 156810 14 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
137640100 156810 14 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
CHEMBL4071136 156810 14 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
59025917 116475 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 418 3 0 3 4.2 COc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2014.11.082
CHEMBL3361317 116475 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 418 3 0 3 4.2 COc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2014.11.082
162523037 192686 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 437 4 1 5 3.2 O=C(Nc1ccc2cccnc2c1)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2022.128988
CHEMBL5219142 192686 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells in the presence of acetylcholine by calcium mobilisation assay
ChEMBL 437 4 1 5 3.2 O=C(Nc1ccc2cccnc2c1)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2022.128988
137653721 158661 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(F)(F)CC2)cc1 10.1016/j.bmcl.2017.02.020
CHEMBL4092786 158661 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(F)(F)CC2)cc1 10.1016/j.bmcl.2017.02.020
59025917 116475 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 418 3 0 3 4.2 COc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2014.11.082
CHEMBL3361317 116475 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 418 3 0 3 4.2 COc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2014.11.082
137653721 158661 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(F)(F)CC2)cc1 10.1016/j.bmcl.2017.02.020
CHEMBL4092786 158661 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(F)(F)CC2)cc1 10.1016/j.bmcl.2017.02.020
118719494 115553 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 470 6 0 4 5.1 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(OC(C)C)cc2)cc1 10.1016/j.bmcl.2014.11.082
CHEMBL3353282 115553 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 470 6 0 4 5.1 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(OC(C)C)cc2)cc1 10.1016/j.bmcl.2014.11.082
71607129 104671 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 422 2 0 2 4.5 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105204 104671 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 422 2 0 2 4.5 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
71607129 104671 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 422 2 0 2 4.5 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105204 104671 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 422 2 0 2 4.5 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
59025979 104389 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 456 2 0 2 5.2 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
CHEMBL3102882 104389 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 456 2 0 2 5.2 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
118719482 115543 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 454 3 0 3 4.4 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2014.11.082
CHEMBL3353270 115543 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 454 3 0 3 4.4 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2014.11.082
59025979 104389 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 456 2 0 2 5.2 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
CHEMBL3102882 104389 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 456 2 0 2 5.2 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
71607067 104683 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 440 2 0 2 4.7 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
CHEMBL3105217 104683 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 440 2 0 2 4.7 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
71607067 104683 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 440 2 0 2 4.7 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
CHEMBL3105217 104683 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 440 2 0 2 4.7 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
118724903 116483 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 396 2 0 2 4.3 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCCC1 10.1016/j.bmcl.2014.11.082
CHEMBL3361330 116483 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 396 2 0 2 4.3 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCCC1 10.1016/j.bmcl.2014.11.082
71607097 104675 0 None -1 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105208 104675 0 None -1 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
71800817 191364 10 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 426 5 0 7 3.4 Cc1csc(SCC2CCN(S(=O)(=O)c3ccc4c(c3)OCCO4)CC2)n1 10.1021/acs.jmedchem.2c00192
CHEMBL5192133 191364 10 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assayAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay
ChEMBL 426 5 0 7 3.4 Cc1csc(SCC2CCN(S(=O)(=O)c3ccc4c(c3)OCCO4)CC2)n1 10.1021/acs.jmedchem.2c00192
118724903 116483 0 None - 1 Human 5.7 pIC50