A425619 [Ligand Id: 4117] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL104028 (A-425619) |
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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 TRPV1 assessed as inhibition of capsaicin-induced effect by FLIPR assay | B | 7.74 | pKi | 18.3 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 803-806 [PMID:25597011] |
| ChEMBL | Binding affinity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane using [3H]-RTX as radioligand. | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3053-3056 [PMID:15149643] |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | J Pharmacol Exp Ther (2005) 314: 400-9 [PMID:15837819] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay | F | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| ChEMBL | Inhibition of binding to human vanilloid receptor subtype VR1 | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2005) 48: 744-752 [PMID:15689158] |
| ChEMBL | Antagonist activity at human TRPV1 by calcium influx assay | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3894-3899 [PMID:17507218] |
| ChEMBL | Blockade of human TRPV1 receptor assessed as inhibition of capsaicin-induced calcium flux | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2008) 51: 392-395 [PMID:18183945] |
| ChEMBL | Antagonist activity at human TRPV1 assessed as inhibition of calcium influx | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1338-1341 [PMID:21315587] |
| ChEMBL | Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [Ca2+] levels. | F | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 3053-3056 [PMID:15149643] |
| ChEMBL | Antagonist activity at human TRPV1 receptor by calcium influx assay | F | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (2007) 50: 3651-3660 [PMID:17583335] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay | F | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2007) 50: 2589-2596 [PMID:17489570] |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | Inhibition of binding to rat transient receptor potential vanilloid 1 receptor | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2005) 48: 744-752 [PMID:15689158] |
| ChEMBL | Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay | F | 8.05 | pIC50 | 9 | 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]
