ChEMBL ligand: CHEMBL3833319 (GSK-1160724, GSK1160724, Revefenacin, Revefenacina, Revefenacine, 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]
ChEMBL	GPCR PRESTO-Tango dose-response in antagonist mode with target: CHRM2	F	7.33	pIC50	46.88	nM	IC50	EUbOPEN Chemogenomics Library - GPCR Dose-Respose
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]