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 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]