Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL1548353 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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]