Assay Detail
Binding
CHEMBL4273598
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-LO in human neutrophils using arachidonic acid as substrate assessed as reduction in 5-LO product formation preincubated for 15 mins followed by substrate addition measured after 10 mins in presence of Ca2+ ionophore A23187 by HPLC analysis
28
Total Activities
28
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
Discovery of a benzenesulfonamide-based dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase that favorably modulates lipid mediator biosynthesis in inflammation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.80 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4277234 | — | — | 1 | 6.52 |
| CHEMBL4288981 | — | — | 1 | 6.52 |
| CHEMBL4287468 | — | — | 1 | 6.40 |
| CHEMBL4279548 | — | — | 1 | 6.30 |
| CHEMBL4283338 | — | — | 1 | 6.30 |
| CHEMBL4277656 | — | — | 1 | 6.16 |
| CHEMBL4287827 | — | — | 1 | 6.10 |
| CHEMBL4285595 | — | — | 1 | 6.05 |
| CHEMBL4290120 | — | — | 1 | 6.00 |
| CHEMBL4286690 | — | — | 1 | 5.96 |
| CHEMBL4284489 | — | — | 1 | 5.96 |
| CHEMBL4281072 | — | — | 1 | 5.89 |
| CHEMBL4293928 | — | — | 1 | 5.82 |
| CHEMBL4287883 | — | — | 1 | 5.77 |
| CHEMBL4278377 | — | — | 1 | 5.75 |
| CHEMBL4289048 | — | — | 1 | 5.68 |
| CHEMBL4293980 | — | — | 1 | 5.62 |
| CHEMBL4279919 | — | — | 1 | 5.58 |
| CHEMBL4292383 | — | — | 1 | 5.50 |
| CHEMBL4286325 | — | — | 1 | 5.50 |
| CHEMBL4290525 | — | — | 1 | 5.48 |
| CHEMBL4278781 | — | — | 1 | 5.47 |
| CHEMBL4278826 | — | — | 1 | 5.46 |
| CHEMBL4279873 | — | — | 1 | 5.40 |
| CHEMBL4289742 | — | — | 1 | 5.36 |
| CHEMBL1774311 | — | — | 1 | 5.35 |
| CHEMBL4286074 | — | — | 1 | 5.32 |
| CHEMBL4282253 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4277234 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4288981 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4287468 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4279548 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4283338 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4277656 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4287827 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4285595 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4290120 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4286690 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4284489 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4281072 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4293928 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4287883 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4278377 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4289048 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4293980 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4279919 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4292383 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4286325 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4290525 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4278781 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4278826 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4279873 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4289742 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL1774311 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4286074 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4282253 | — | IC50 | = | 8400.0 | nM | 5.08 |