A425619 [Ligand Id: 4117] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL104028 (A-425619)
1 CHEMBL104028_lig_chart_1 Vanilloid receptor HumanRat
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]