Assay Detail
Binding
CHEMBL4368175
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-LOX in human PMNL cells assessed as A23187-stimulated LTB4 production preincubated for 15 mins followed by A23187 addition and measured after 10 mins by HPLC analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Protective effect of piceatannol and bioactive stilbene derivatives against hypoxia-induced toxicity in H9c2 cardiomyocytes and structural elucidation as 5-LOX inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.29 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL332610 | — | — | 1 | 7.30 |
| CHEMBL119576 | — | — | 1 | 7.16 |
| CHEMBL69863 | PICEATANNOL | — | 1 | 6.62 |
| CHEMBL83527 | PTEROSTILBENE | 2.0 | 1 | 6.28 |
| CHEMBL296411 | TRISMETHOXYRESVERATROL | — | 1 | 6.12 |
| CHEMBL165 | RESVERATROL | 3.0 | 1 | 5.31 |
| CHEMBL419378 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL332610 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL119576 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL69863 | PICEATANNOL | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL83527 | PTEROSTILBENE | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL296411 | TRISMETHOXYRESVERATROL | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL165 | RESVERATROL | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL419378 | — | IC50 | = | 5480.0 | nM | 5.26 |