Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
187 253 34 None -1 6 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
294 253 34 None -1 6 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
65 253 34 None -1 6 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 253 34 None -1 6 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 253 34 None -1 6 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 253 34 None -1 6 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
187 253 34 None -1 6 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
294 253 34 None -1 6 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
65 253 34 None -1 6 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 253 34 None -1 6 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 253 34 None -1 6 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 253 34 None -1 6 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 780 23 None -27 12 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
298 780 23 None -27 12 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
488 780 23 None -27 12 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 780 23 None -27 12 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 780 23 None -27 12 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
334 234 21 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 234 21 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 234 21 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 15890 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 15890 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 15935 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 15935 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 53325 6 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 53325 6 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 3953 57 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 3953 57 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 3953 57 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 113694 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 113694 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 113694 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 113694 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 3953 57 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 3953 57 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 3953 57 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 15864 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 15864 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 113714 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 113714 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 113715 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 113715 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 113715 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 113715 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 16511 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 16511 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 3387 18 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 3387 18 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 3387 18 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 3387 18 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 3387 18 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 113714 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 113714 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 15888 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 15888 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 15915 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 15915 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 80034 8 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 80034 8 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 113712 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 113712 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 113716 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 113716 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 113716 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 113716 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 163798 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 163798 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 113712 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 113712 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 4022 72 None -263 9 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 113713 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 113713 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 17345 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 17345 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 113698 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 113698 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 113713 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 113713 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 113698 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 113698 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 113709 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 113709 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 113688 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 113688 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 15912 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 15912 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 15913 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 15913 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 15934 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 15934 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 63471 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 63471 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 113709 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 113709 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 17161 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 17161 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 198039 44 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 198039 44 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 113688 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 113688 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 113700 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 113700 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 113700 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 113700 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 113689 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 113689 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 1996 63 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 1996 63 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 1996 63 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 178223 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 178223 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 113689 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 113689 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 113710 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 113710 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 113711 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 113711 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 113710 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 113710 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 113711 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 113711 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 171532 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 171532 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 186901 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 186901 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
187 253 34 None -1 6 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
294 253 34 None -1 6 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
65 253 34 None -1 6 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 253 34 None -1 6 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 253 34 None -1 6 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 253 34 None -1 6 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 15886 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 15886 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 15887 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 15887 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 2529 14 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 2529 14 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 2529 14 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 199673 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 199673 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 178196 2 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 178196 2 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 2529 14 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 2529 14 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 2529 14 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 188075 40 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 188075 40 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 17201 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 17201 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 113699 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 113699 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 188075 40 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 188075 40 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 113699 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 113699 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 17378 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 17378 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 113687 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 113687 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 17202 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 17202 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 113687 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 113687 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 55649 1 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 55649 1 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 55649 1 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 113701 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 113701 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 113701 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 113701 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 198039 44 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 198039 44 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 198359 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 198359 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 199489 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 199489 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 102777 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 102777 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 17162 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 17162 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 17379 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 17379 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 113690 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 113690 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 113690 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 113690 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 113686 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 113686 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 17242 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 17242 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 113686 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 113686 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 15933 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 15933 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 188577 2 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 188577 2 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 17096 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 17096 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 17344 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 17344 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 178117 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 178117 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 188211 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 188211 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 198476 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 198476 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 113685 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 113685 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 113685 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 113685 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 184696 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 184696 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 186470 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 186470 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 113708 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 113708 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 113708 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 113708 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 198475 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 198475 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 73949 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 73949 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 17280 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 17280 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 198320 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 198320 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 188588 2 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 188588 2 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 15889 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 15889 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 15914 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 15914 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 17315 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 17315 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 188822 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 188822 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 3948 48 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 3948 48 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 3948 48 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 178012 0 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 178012 0 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 3948 48 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 3948 48 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 3948 48 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 102779 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 102779 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 77983 32 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 77983 32 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 17316 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 17316 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 3948 48 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 3948 48 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 3948 48 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 187027 4 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 187027 4 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 40156 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 40156 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 113706 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 113706 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 113706 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 113706 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 198444 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 198444 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 15911 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 15911 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 15932 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 15932 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 113707 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 113707 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 113707 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 113707 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 198321 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 198321 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 16945 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 16945 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 2529 14 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 2529 14 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 2529 14 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 113684 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 113684 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 113684 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 113684 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
187 253 34 None -1 6 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
294 253 34 None -1 6 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
65 253 34 None -1 6 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 253 34 None -1 6 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 253 34 None -1 6 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 253 34 None -1 6 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 81733 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 81733 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 113705 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 113705 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 113705 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 113705 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 54114 10 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 54114 10 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 54114 10 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 188789 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 188789 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 188825 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 188825 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 113695 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 113695 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 113695 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 113695 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 113697 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 113697 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 113691 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 113691 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 113697 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 113697 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 113691 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 113691 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 113704 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 113704 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 113696 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 113696 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 113704 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 113704 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 113696 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 113696 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 15863 15 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 15863 15 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 15863 15 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 15863 15 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 113702 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 113702 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 113703 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 113703 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 113702 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 113702 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 113703 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 113703 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 27097 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 27097 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 780 23 None -27 12 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
298 780 23 None -27 12 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
488 780 23 None -27 12 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 780 23 None -27 12 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 780 23 None -27 12 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 113693 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 113693 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 113693 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 113693 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 113692 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 113692 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 113692 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 113692 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 780 23 None -27 12 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
298 780 23 None -27 12 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
488 780 23 None -27 12 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 780 23 None -27 12 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 780 23 None -27 12 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 203923 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 203923 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 96028 4 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 96028 4 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 192058 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 192058 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 104188 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 104188 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 115034 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 115034 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 156323 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 156323 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 2528 13 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 2528 13 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 2528 13 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 104183 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 104183 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 192062 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 192062 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 104183 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 104183 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 192053 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 192053 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 191741 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 191741 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 191741 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 191741 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 94661 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 94661 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 115042 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 115042 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 104189 0 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 104189 0 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 192098 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 192098 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 2528 13 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 2528 13 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 2528 13 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 158458 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 158458 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 189614 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 189614 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 189614 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 189614 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 155493 12 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 155493 12 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 189500 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 189500 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 189500 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 189500 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 155493 12 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 155493 12 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 155493 12 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 155493 12 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 115028 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 115028 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 190186 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 190186 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 190186 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 190186 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 191566 4 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 191566 4 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 158812 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 158812 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 104190 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 104190 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 192047 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 192047 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 8165 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 8165 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 104190 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 104190 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 115025 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 115025 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 115032 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 115032 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 115045 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 115045 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 115046 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 115046 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 115969 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 115969 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 97303 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 97303 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 115969 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 115969 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 158812 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 158812 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 192063 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 192063 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 192137 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 192137 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 104178 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 104178 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 189498 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 189498 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 104178 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 104178 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 189498 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 189498 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 115035 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 115035 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 192057 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 192057 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 155738 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 155738 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 157555 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 157555 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 155738 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 155738 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 191900 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 191900 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 191900 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 191900 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 192078 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 192078 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 115038 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 115038 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 115968 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 115968 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 155493 12 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 155493 12 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 115968 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 115968 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 155493 12 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 155493 12 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 192093 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 192093 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 156257 10 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 156257 10 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 156257 10 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 156257 10 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 115962 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 115962 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 192075 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 192075 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 158103 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 158103 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 115962 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 115962 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 158103 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 158103 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 115041 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 115041 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 104179 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 104179 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 104179 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 104179 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 103897 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 103897 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 115031 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 115031 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 103897 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 103897 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 104191 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 104191 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 104191 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 104191 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 115970 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 115970 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 104183 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 104183 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 190760 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 190760 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 115970 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 115970 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
168270600 189435 0 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 378 5 0 5 3.1 O=S(=O)(c1ccc2c(c1)CCO2)N1CCC(CCc2nccs2)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5171868 189435 0 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 378 5 0 5 3.1 O=S(=O)(c1ccc2c(c1)CCO2)N1CCC(CCc2nccs2)CC1 10.1021/acs.jmedchem.2c00192
168270600 189435 0 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 378 5 0 5 3.1 O=S(=O)(c1ccc2c(c1)CCO2)N1CCC(CCc2nccs2)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5171868 189435 0 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 378 5 0 5 3.1 O=S(=O)(c1ccc2c(c1)CCO2)N1CCC(CCc2nccs2)CC1 10.1021/acs.jmedchem.2c00192
118719501 115048 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 456 5 0 4 4.6 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)ccc1C 10.1016/j.bmcl.2014.11.082
CHEMBL3353289 115048 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 456 5 0 4 4.6 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)ccc1C 10.1016/j.bmcl.2014.11.082
168271588 189601 0 None - 1 Human 6.6 pIC50 = 6.6 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 371 2 0 5 1.8 Cn1ccnc1C#CC1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5174465 189601 0 None - 1 Human 6.6 pIC50 = 6.6 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 371 2 0 5 1.8 Cn1ccnc1C#CC1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
168285490 191050 0 None 9 2 Human 6.6 pIC50 = 6.6 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 Cc1cn(C)c(SCC2CCN(S(=O)(=O)c3ccc4c(c3)CCO4)CC2)n1 10.1021/acs.jmedchem.2c00192
CHEMBL5196183 191050 0 None 9 2 Human 6.6 pIC50 = 6.6 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 Cc1cn(C)c(SCC2CCN(S(=O)(=O)c3ccc4c(c3)CCO4)CC2)n1 10.1021/acs.jmedchem.2c00192
168285490 191050 0 None 9 2 Human 6.6 pIC50 = 6.6 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 Cc1cn(C)c(SCC2CCN(S(=O)(=O)c3ccc4c(c3)CCO4)CC2)n1 10.1021/acs.jmedchem.2c00192
CHEMBL5196183 191050 0 None 9 2 Human 6.6 pIC50 = 6.6 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 Cc1cn(C)c(SCC2CCN(S(=O)(=O)c3ccc4c(c3)CCO4)CC2)n1 10.1021/acs.jmedchem.2c00192
168271551 189571 0 None - 1 Human 5.6 pIC50 = 5.6 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 392 5 0 6 3.5 Cn1ccnc1SCC1CCC(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5174003 189571 0 None - 1 Human 5.6 pIC50 = 5.6 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 392 5 0 6 3.5 Cn1ccnc1SCC1CCC(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
168271551 189571 0 None - 1 Human 5.6 pIC50 = 5.6 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 392 5 0 6 3.5 Cn1ccnc1SCC1CCC(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
CHEMBL5174003 189571 0 None - 1 Human 5.6 pIC50 = 5.6 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 392 5 0 6 3.5 Cn1ccnc1SCC1CCC(S(=O)(=O)c2ccc3c(c2)CCO3)CC1 10.1021/acs.jmedchem.2c00192
1090202 8391 11 None -2 3 Human 5.6 pIC50 = 5.6 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 377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1094003 8391 11 None -2 3 Human 5.6 pIC50 = 5.6 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 377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
59025695 104184 0 None - 1 Human 5.6 pIC50 = 5.6 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 472 3 0 3 5.1 O=C(c1ccc(OC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
CHEMBL3105209 104184 0 None - 1 Human 5.6 pIC50 = 5.6 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 472 3 0 3 5.1 O=C(c1ccc(OC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
71607084 104194 0 None - 1 Human 5.6 pIC50 = 5.6 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 404 2 0 2 4.1 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)cc(F)c2)cc1 10.1021/jm4013246
CHEMBL3105226 104194 0 None - 1 Human 5.6 pIC50 = 5.6 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 404 2 0 2 4.1 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)cc(F)c2)cc1 10.1021/jm4013246
59025695 104184 0 None - 1 Human 5.6 pIC50 = 5.6 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 472 3 0 3 5.1 O=C(c1ccc(OC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
CHEMBL3105209 104184 0 None - 1 Human 5.6 pIC50 = 5.6 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 472 3 0 3 5.1 O=C(c1ccc(OC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
71607084 104194 0 None - 1 Human 5.6 pIC50 = 5.6 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 404 2 0 2 4.1 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)cc(F)c2)cc1 10.1021/jm4013246
CHEMBL3105226 104194 0 None - 1 Human 5.6 pIC50 = 5.6 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 404 2 0 2 4.1 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)cc(F)c2)cc1 10.1021/jm4013246
168294490 191605 0 None - 1 Human 6.6 pIC50 = 6.6 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 443 5 0 7 1.2 Cn1ccnc1S(=O)(=O)C[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
CHEMBL5204724 191605 0 None - 1 Human 6.6 pIC50 = 6.6 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 443 5 0 7 1.2 Cn1ccnc1S(=O)(=O)C[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
168294490 191605 0 None - 1 Human 6.6 pIC50 = 6.6 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 443 5 0 7 1.2 Cn1ccnc1S(=O)(=O)C[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
CHEMBL5204724 191605 0 None - 1 Human 6.6 pIC50 = 6.6 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 443 5 0 7 1.2 Cn1ccnc1S(=O)(=O)C[C@H]1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)C[C@@H]1F 10.1021/acs.jmedchem.2c00192
118719485 115033 0 None - 1 Human 5.6 pIC50 = 5.6 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 466 4 0 3 4.7 CC(C)Oc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.bmcl.2014.11.082
CHEMBL3353273 115033 0 None - 1 Human 5.6 pIC50 = 5.6 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 466 4 0 3 4.7 CC(C)Oc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1 10.1016/j.bmcl.2014.11.082
118724904 115971 0 None - 1 Human 5.6 pIC50 = 5.6 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 382 2 0 2 3.9 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCC1 10.1016/j.bmcl.2014.11.082
CHEMBL3361331 115971 0 None - 1 Human 5.6 pIC50 = 5.6 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 382 2 0 2 3.9 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCC1 10.1016/j.bmcl.2014.11.082
118724904 115971 0 None - 1 Human 5.6 pIC50 = 5.6 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 382 2 0 2 3.9 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCC1 10.1016/j.bmcl.2014.11.082
CHEMBL3361331 115971 0 None - 1 Human 5.6 pIC50 = 5.6 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 382 2 0 2 3.9 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCC1 10.1016/j.bmcl.2014.11.082
118719502 115049 0 None 2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium responseAntagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
ChEMBL 452 3 0 3 4.2 COc1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C 10.1016/j.bmcl.2016.07.071
CHEMBL3353290 115049 0 None 2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium responseAntagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
ChEMBL 452 3 0 3 4.2 COc1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C 10.1016/j.bmcl.2016.07.071
162523114 192098 0 None -2 3 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat muscarinic M5 receptorAntagonist activity at rat muscarinic M5 receptor
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 192098