Assay Detail
Binding
CHEMBL4273597
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human 5-LO expressed in Escherichia coli BL21 (DE3) using arachidonic acid as substrate preincubated for 10 mins followed by CaCl2 and substrate addition measured after 10 mins by RP-HPLC analysis
11
Total Activities
11
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 | 11 | 5.28 | 5.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4285595 | — | — | 1 | 5.64 |
| CHEMBL4287468 | — | — | 1 | 5.64 |
| CHEMBL4283338 | — | — | 1 | 5.28 |
| CHEMBL4278377 | — | — | 1 | 5.26 |
| CHEMBL4277234 | — | — | 1 | 5.25 |
| CHEMBL1774311 | — | — | 1 | 5.24 |
| CHEMBL4287827 | — | — | 1 | 5.22 |
| CHEMBL4286690 | — | — | 1 | 5.19 |
| CHEMBL4279548 | — | — | 1 | 5.18 |
| CHEMBL4288981 | — | — | 1 | 5.14 |
| CHEMBL4278781 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4285595 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4287468 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4283338 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4278377 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4277234 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL1774311 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4287827 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4286690 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4279548 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4288981 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4278781 | — | IC50 | = | 8700.0 | nM | 5.06 |