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 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]
