JNJ17203212 [Ligand Id: 4228] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL254778 (JNJ-17203212)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Antagonist activity at human recombinant TRPV1 assessed as inhibition of capsaicin-induced in intracellular calcium levels by cell-based FLIPR assay F 6.8 pIC50 160 nM IC50 Bioorg Med Chem Lett (2010) 20: 7137-7141 [PMID:20947352]
ChEMBL Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay F 7.19 pIC50 65 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
ChEMBL Inhibition of human TRPV1 B 7.19 pIC50 65 nM IC50 Eur J Med Chem (2023) 245: 114893-114893 [PMID:36395649]
ChEMBL Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay F 7.8 pIC50 16 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
GtoPdb - - 7.8 pIC50 16 nM IC50 J Med Chem (2005) 48: 1857-72 [PMID:15771431]
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433]
ChEMBL Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay F 6.99 pIC50 102 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
ChEMBL Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay F 7.8 pIC50 16 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]

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]