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ChEMBL ligand: CHEMBL1548353 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 32:
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]