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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| ChEMBL | Antagonist activity at human recombinant TRPV1 expressed in HEK293T cells assessed as inhibition of capsaicin-induced TRPV1 channel activation by FLIPR-based Ca2+ assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2023) 245: 114893-114893 [PMID:36395649] |
| 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 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]
