revefenacin [Ligand Id: 10129] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL3833319 (GSK-1160724, Yupelri, Revefenacin, GSK1160724, TD-4208)
  • 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 B 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 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 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 B 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 28:

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]