danirixin [Ligand Id: 8500] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3039531 (Danirixin, Gsk1325756, GSK1325756, GSK1325756B, GSK-1325756B)
  • CXCR1/Interleukin-8 receptor A in Human [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
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  • CXCR2/Interleukin-8 receptor B in Human [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CXCR1/Interleukin-8 receptor A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
ChEMBL Displacement of [125I]IL8 from recombinant human CXCR1 expressed in CHO cell membranes measured after 1 hr by TopCount scintillation counting method B 4.52 pIC50 <30000 nM IC50 US-20070249672-A1. IL-8 Receptor Antagonists (2007)
CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
ChEMBL Displacement of [125I]IL8 from recombinant human CXCR2 expressed in CHO cell membranes measured after 1 hr by TopCount scintillation counting method B 4.52 pIC50 <30000 nM IC50 US-20070249672-A1. IL-8 Receptor Antagonists (2007)
GtoPdb - - 7.9 pIC50 12.5 nM IC50 BMC Pharmacol Toxicol (2015) 16: 18 [PMID:26092545]
ChEMBL Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay F 8.3 pIC50 5 nM IC50 US-20070249672-A1. IL-8 Receptor Antagonists (2007)

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]