Assay Detail
Binding
CHEMBL4273596
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mPGES-1 isolated from microsomes of interleukin-1 beta-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 5.61 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4286690 | — | — | 1 | 6.52 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 6.22 |
| CHEMBL4287468 | — | — | 1 | 6.16 |
| CHEMBL4278377 | — | — | 1 | 6.16 |
| CHEMBL4287827 | — | — | 1 | 6.00 |
| CHEMBL4278781 | — | — | 1 | 5.96 |
| CHEMBL4277234 | — | — | 1 | 5.92 |
| CHEMBL4284489 | — | — | 1 | 5.80 |
| CHEMBL4292383 | — | — | 1 | 5.72 |
| CHEMBL4293928 | — | — | 1 | 5.72 |
| CHEMBL4291396 | — | — | 1 | 5.62 |
| CHEMBL4285595 | — | — | 1 | 5.57 |
| CHEMBL4284176 | — | — | 1 | 5.57 |
| CHEMBL4287883 | — | — | 1 | 5.54 |
| CHEMBL4277656 | — | — | 1 | 5.50 |
| CHEMBL4286325 | — | — | 1 | 5.47 |
| CHEMBL1774311 | — | — | 1 | 5.43 |
| CHEMBL4288981 | — | — | 1 | 5.42 |
| CHEMBL4290525 | — | — | 1 | 5.40 |
| CHEMBL4289742 | — | — | 1 | 5.33 |
| CHEMBL4289048 | — | — | 1 | 5.33 |
| CHEMBL4283338 | — | — | 1 | 5.30 |
| CHEMBL4278826 | — | — | 1 | 5.28 |
| CHEMBL4290120 | — | — | 1 | 5.28 |
| CHEMBL4279919 | — | — | 1 | 5.27 |
| CHEMBL4281072 | — | — | 1 | 5.21 |
| CHEMBL4293980 | — | — | 1 | 5.20 |
| CHEMBL4279548 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4286690 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL93 | ZILEUTON | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4287468 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4278377 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4287827 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4278781 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4277234 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4284489 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4292383 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4293928 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4291396 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4285595 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4284176 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4287883 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4277656 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4286325 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1774311 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4288981 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4290525 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4289742 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4289048 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4283338 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4278826 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4290120 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4279919 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4281072 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4293980 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL4279548 | — | IC50 | = | 6500.0 | nM | 5.19 |