compound 21n [PMID: 17656086] [Ligand Id: 8750] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL235920
  • 15-LOX-1/Arachidonate 15-lipoxygenase in Human [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • 15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
15-LOX-1/Arachidonate 15-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
ChEMBL Competitive inhibition of human 15-LOX1 using linoleic acid as substrate after 10 mins by Lineweaver-Burk plot analysis B 7.14 pKi 73 nM Ki J Med Chem (2015) 58: 7850-7862 [PMID:26331552]
ChEMBL Competitive inhibition of human 15-LOX-1 assessed as reduction in conversion of linoleic acid to 13(S)-HpODE incubated for 10 mins followed by linoleic acid addition by Lineweaver-Burk plot analysis B 7.14 pKi 73 nM Ki Eur J Med Chem (2016) 122: 786-801 [PMID:27477687]
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL Inhibition of rabbit 15-lipoxygenase in presence of arachidonic acid B 7.12 pIC50 75 nM IC50 Bioorg Med Chem Lett (2007) 17: 5115-5120 [PMID:17656086]
ChEMBL Inhibition of rabbit 15-lipoxygenase in presence of linoleic acid B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2007) 17: 5115-5120 [PMID:17656086]
15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
GtoPdb - - 7.29 pIC50 51 nM IC50 Bioorg Med Chem Lett (2007) 17: 5115-20 [PMID:17656086]
ChEMBL Inhibition of human recombinant 15-lipoxygenase over-expressed in CHO cells B 7.29 pIC50 51 nM IC50 Bioorg Med Chem Lett (2007) 17: 5115-5120 [PMID:17656086]

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]