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ChEMBL ligand: CHEMBL2441929 (Acoltremon, AR-15512, AVX-012, FEMA NO. 4681, WS-12) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
ChEMBL | Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay | B | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6118-6122 [PMID:24080460] |
TRPM8 in Rat [GtoPdb: 500] [UniProtKB: Q8R455] | ||||||||
GtoPdb | Whole-cell voltage-clamp recordings or Ca2+-microfluorimetry in heterologous cells (HEK, CHO, and Xenopus oocytes) expressing TRPM8 | - | 4.9 | pEC50 | 12500 | nM | EC50 |
Pak J Pharm Sci (2008) 21: 370-8 [PMID:18930858]; J Pharm Pharm Sci (2010) 13: 242-53 [PMID:20816009] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]