ML351 [Ligand Id: 10263] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1548353
  • 15-LOX-1/Arachidonate 15-lipoxygenase in Human [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
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  • 15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
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  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
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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 Inhibition of recombinant N-terminal His6-tagged human reticulocyte 12/15-lipoxygenase using arachidonic acid as substrate assessed as equilibrium constant of dissociation from secondary site measured 15-HpETE formation by UV-vis spectrometric analysis B 5.92 pKi 1200 nM Ki J Med Chem (2014) 57: 4035-4048 [PMID:24684213]
ChEMBL Inhibition of recombinant N-terminal His6-tagged human reticulocyte 12/15-lipoxygenase using arachidonic acid as substrate assessed as equilibrium constant of dissociation from catalytic site measured 15-HpETE formation by UV-vis spectrometric analysis B 7 pKi 100 nM Ki J Med Chem (2014) 57: 4035-4048 [PMID:24684213]
ChEMBL Inhibition of N-terminal His6-tagged human platelet 12-lipoxygenase using arachidonic acid as substrate by UV-vis spectrometric analysis B 4.3 pIC50 >50000 nM IC50 J Med Chem (2014) 57: 4035-4048 [PMID:24684213]
ChEMBL Inhibition of human N-terminal His6-tagged 15-LOX-1 F414I mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis B 5.39 pIC50 4100 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
ChEMBL Inhibition of human N-terminal His6-tagged 15-LOX-1 E356Q mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis B 6.06 pIC50 870 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
ChEMBL Inhibition of human N-terminal His6-tagged 15-LOX-1 F414W mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis B 6.11 pIC50 770 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
ChEMBL Inhibition of human N-terminal His6-tagged 15-LOX-1 L407A mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis B 6.41 pIC50 390 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
ChEMBL Inhibition of wild type human N-terminal His6-tagged 15-LOX-1 expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis B 6.48 pIC50 330 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
ChEMBL Inhibition of human N-terminal His6-tagged 15-LOX-1 Q547L mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis B 6.52 pIC50 300 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
ChEMBL Inhibition of human N-terminal His6-tagged 15-LOX-1 R404L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis B 6.59 pIC50 260 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
ChEMBL Inhibition of recombinant N-terminal His6-tagged human reticulocyte 12/15-lipoxygenase using arachidonic acid as substrate by UV-vis spectrometric analysis B 6.7 pIC50 200 nM IC50 J Med Chem (2014) 57: 4035-4048 [PMID:24684213]
ChEMBL Inhibition of N-terminal His6-tagged human 12/15-LOX using arachidonic acid as substrate by UV-visible spectrophotometric analysis B 6.7 pIC50 200 nM IC50 Bioorg Med Chem (2016) 24: 1183-1190 [PMID:26899595]
GtoPdb - - 6.7 pIC50 200 nM IC50 Probe Reports from the NIH Molecular Libraries Program (2010) : [PMID:24672829]
ChEMBL Inhibition of human N-terminal His6-tagged 15-LOX-1 I417A mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis B 6.74 pIC50 180 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
ChEMBL Inhibition of human N-terminal His6-tagged 15-LOX-1 R402L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis B 6.92 pIC50 120 nM IC50 Bioorg Med Chem (2016) 24: 5380-5387 [PMID:27647374]
15-LOX-2/Arachidonate 15-lipoxygenase, type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2457] [GtoPdb: 1389] [UniProtKB: O15296]
ChEMBL Inhibition of N-terminal His6-tagged human epithelial 15-lipoxygenase-2 using arachidonic acid as substrate by UV-vis spectrometric analysis B 4.3 pIC50 >50000 nM IC50 J Med Chem (2014) 57: 4035-4048 [PMID:24684213]
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL Inhibition of human 5-lipoxygenase using arachidonic acid as substrate by UV-vis spectrometric analysis B 4.3 pIC50 >50000 nM IC50 J Med Chem (2014) 57: 4035-4048 [PMID:24684213]

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]