mavatrep [Ligand Id: 12755] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2364618 (JNJ-39439335, Mavatrep) |
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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 | Displacement of [3H]-RTX from human TRPV1 transfected in HEK293 cells after 60 mins by scintillation spectroscopic analysis | B | 8.19 | pKi | 6.5 | nM | Ki | J Med Chem (2015) 58: 3859-3874 [PMID:25850459] |
| ChEMBL | Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced current measured for 150 secs by patch clamp assay | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2015) 58: 3859-3874 [PMID:25850459] |
| GtoPdb | Antagonism of capsaicin-induced hTRPV1 current in HEK293 cells by patch clamp assay | - | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2015) 58: 3859-74 [PMID:25850459] |
| ChEMBL | Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of pH 5-induced current measured for 150 secs by patch clamp assay | B | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (2015) 58: 3859-3874 [PMID:25850459] |
| ChEMBL | Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2015) 58: 3859-3874 [PMID:25850459] |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | Antagonist activity at recombinant rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx preincubated for 5 mins followed by capsaicin challenge | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2015) 58: 3859-3874 [PMID:25850459] |
| GtoPdb | Antagonism of capsaicin-induced rTRPV1 mediated calcium influx in HEK293 cells | - | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2015) 58: 3859-74 [PMID:25850459] |
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]
