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 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]