elubirixin [Ligand Id: 8499] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2178579 (Elubrixin, Sb-656933, SB-656933, SB656933, SB-656933-AAF)
  • 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 Binding affinity to CXCR1 B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
ChEMBL Antagonist activity at CXCR2 assessed as inhibition of neutrophil shape change F 6.51 pIC50 310.5 nM IC50 J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
ChEMBL Antagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulation F 6.58 pIC50 260.7 nM IC50 J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
GtoPdb - - 7.66 pIC50 22 nM IC50 Pharmacol Rev (2014) 66: 1-79 [PMID:24218476]
ChEMBL Binding affinity to CXCR2 B 8.29 pIC50 5.1 nM IC50 J Med Chem (2012) 55: 9363-9392 [PMID:22931505]

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]