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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]