SB705498 [Ligand Id: 4311] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL207433 (GSK705498, Sb-705498, SB-705498)
  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
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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 Antagonist activity against human TRPM8 expressed in HEK293 cells assessed as inhibition of methanol-gated currents by whole cell patch clamp electrophysiology B 5.8 pIC50 1600 nM IC50 Eur J Med Chem (2022) 233: 114191-114191 [PMID:35263708]
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Displacement of [3H]RTX from human TRPV1 expressed in HEK293 cell membranes after 60 mins by scintillation counting method B 7 pIC50 100 nM IC50 Bioorg Med Chem (2018) 26: 3716-3726 [PMID:29887511]
GtoPdb - - 7.1 pIC50 79.4 nM IC50 J Pharmacol Exp Ther (2007) 321: 1183-92 [PMID:17392405]
ChEMBL Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced Ca2+ influx incubated for 30 mins by FLIPR method B 8.03 pIC50 9.24 nM IC50 Eur J Med Chem (2022) 233: 114191-114191 [PMID:35263708]
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433]
ChEMBL Inhibition of rat TRPV1 B 7.49 pIC50 32 nM IC50 J Med Chem (2010) 53: 3330-3348 [PMID:20307063]

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]