MLS000536924 [Ligand Id: 10264] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1452107
  • 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-2/Arachidonate 15-lipoxygenase, type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
GtoPdb - - 5.6 pKi 2500 nM Ki PLoS ONE (2014) 9: e104094 [PMID:25111178]
ChEMBL Competitive inhibition of human 15-LOX-2 assessed as equilibrium dissociation constant from catalytic site by measuring 15-HpETE by Dixon plots and Dixon replots analysis B 5.6 pKi 2.5 uM Kic Bioorg Med Chem (2021) 46: 116349-116349 [PMID:34500187]
ChEMBL Inhibition of human 15-LOX-2 assessed as enzymatic rate using arachidonic acid as substrate by UV/Vis spectrophotometric analysis B 5.51 pIC50 3100 nM IC50 Bioorg Med Chem (2021) 46: 116349-116349 [PMID:34500187]
ChEMBL Inhibition of human 15-LOX-2 expressed in HEK293T cells assessed as a reduction in 15-HETE production using arachidonic acid as substrate incubated for 20 mins B 6.22 pEC50 600 nM EC50 Bioorg Med Chem (2021) 46: 116349-116349 [PMID:34500187]

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]