ChEMBL ligand: CHEMBL3833319 (GSK1160724, GSK-1160724, Revefenacin, TD-4208, Yupelri)
M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] There should be some charts here, you may need to enable JavaScript!
M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] There should be some charts here, you may need to enable JavaScript!
M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229] There should be some charts here, you may need to enable JavaScript!
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173] There should be some charts here, you may need to enable JavaScript!
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL	Antagonist activity at human recombinant M2 receptor expressed in CHO cell membranes assessed as inhibition of oxotremorine-stimulated [35S]GTPgammaS binding incubated for 60 mins by topcount liquid scintillation counting	F	8.3	pKi	<5	nM	Ki	US-20050203133-A1. Biphenyl compounds useful as muscarinic receptor antagonists (2005)
ChEMBL	Antagonist activity at human recombinant M2 receptor expressed in CHO cells assessed as blocking of muscarinic receptor agonist oxotremorine-induced inhibition of forskolin-mediated cAMP accumulation incubated for 10 mins by topcount liquid scintillation counting	F	8.3	pKi	<5	nM	Ki	US-20050203133-A1. Biphenyl compounds useful as muscarinic receptor antagonists (2005)
GtoPdb	Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM2 receptor, and displacement of [3H]NMS tracer.	-	9.52	pKi	0.3	nM	Ki	Pharmacol Res Perspect (2018) 6: e00400 [PMID:29736245]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL	Antagonist activity at human recombinant M3 receptor expressed in CHO cells assessed as inhibition of oxotremorine-stimulated intracellular calcium release preincubated for 20 mins followed by oxotremorine addition measured every 0.5 to 1 secs for 15 mins by fluo-4AM dye based FLIPR assay	F	8.3	pKi	<5	nM	Ki	US-20050203133-A1. Biphenyl compounds useful as muscarinic receptor antagonists (2005)
ChEMBL	Displacement of [3H]-NMS from human recombinant M3 receptor expressed in CHO cell membranes measured after 60 mins by topcount liquid scintillation counting	B	8.3	pKi	<5	nM	Ki	US-20050203133-A1. Biphenyl compounds useful as muscarinic receptor antagonists (2005)
GtoPdb	Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM3 receptor, and displacement of [3H]NMS tracer.	-	9.75	pKi	0.18	nM	Ki	Pharmacol Res Perspect (2018) 6: e00400 [PMID:29736245]
M1 receptor in Human [GtoPdb: 13] [UniProtKB: P11229]
GtoPdb	Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM1 receptor, and displacement of [3H]NMS tracer.	-	9.38	pKi	0.42	nM	Ki	Pharmacol Res Perspect (2018) 6: e00400 [PMID:29736245]
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb	Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM4 receptor, and displacement of [3H]NMS tracer.	-	9.26	pKi	0.55	nM	Ki	Pharmacol Res Perspect (2018) 6: e00400 [PMID:29736245]
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb	Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM5 receptor, and displacement of [3H]NMS tracer.	-	8.2	pKi	6.31	nM	Ki	Pharmacol Res Perspect (2018) 6: e00400 [PMID:29736245]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]