NSC 157449 [Ligand Id: 834] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL280711
  • 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 Inhibition of binding of IL-8 to membranes of cloned CXC chemokine receptor 1 expressed in CHO Cells using [125I]IL-8 radioligand B 4.74 pIC50 18200 nM IC50 J Med Chem (2004) 47: 1319-1321 [PMID:14998320]
ChEMBL Displacement of [125I]IL-8 from CXCR1 (unknown origin) stably expressed in CHO cells B 4.74 pIC50 18200 nM IC50 Eur J Med Chem (2020) 185: 111853-111853 [PMID:31732253]
CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
GtoPdb - - 6.3 pIC50 - - - J Biol Chem (1998) 273: 10095-8 [PMID:9553055]
ChEMBL Inhibition of binding of IL-8 to membranes of cloned CXC chemokine receptor 2 expressed in CHO Cells using [125I]IL-8 radioligand B 6.49 pIC50 320 nM IC50 J Med Chem (2004) 47: 1319-1321 [PMID:14998320]
ChEMBL Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cells B 6.49 pIC50 320 nM IC50 Bioorg Med Chem Lett (2007) 17: 1713-1717 [PMID:17236763]
ChEMBL Displacement of [125I]IL-8 from CXCR2 (unknown origin) stably expressed in CHO cells B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2020) 185: 111853-111853 [PMID:31732253]

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]