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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 |
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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 | 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 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]