WS-12 [Ligand Id: 4343] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Agonist activity at TRPM8 (unknown origin) by fluorometric imaging plate reader analysis | B | 4.92 | pEC50 | 12000 | nM | EC50 | J Med Chem (2016) 59: 10006-10029 [PMID:27437828] |
| 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 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]
