Assay Detail
Binding
CHEMBL3096448
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Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.03 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3094419 | — | — | 1 | 6.52 |
| CHEMBL3094412 | — | — | 1 | 6.40 |
| CHEMBL3094418 | — | — | 1 | 6.40 |
| CHEMBL3094420 | — | — | 1 | 6.40 |
| CHEMBL3094421 | — | — | 1 | 6.40 |
| CHEMBL3091497 | — | — | 1 | 6.30 |
| CHEMBL3094422 | — | — | 1 | 6.30 |
| CHEMBL3094428 | — | — | 1 | 6.22 |
| CHEMBL3094414 | — | — | 1 | 6.22 |
| CHEMBL3094413 | — | — | 1 | 6.22 |
| CHEMBL3094425 | — | — | 1 | 6.16 |
| CHEMBL3094431 | — | — | 1 | 6.16 |
| CHEMBL3091499 | — | — | 1 | 6.16 |
| CHEMBL3091498 | — | — | 1 | 6.10 |
| CHEMBL3091500 | — | — | 1 | 6.10 |
| CHEMBL3094424 | — | — | 1 | 6.05 |
| CHEMBL3094432 | — | — | 1 | 5.92 |
| CHEMBL3094423 | — | — | 1 | 5.89 |
| CHEMBL3094426 | — | — | 1 | 5.89 |
| CHEMBL3094433 | — | — | 1 | 5.85 |
| CHEMBL3091495 | — | — | 1 | 5.85 |
| CHEMBL3094415 | — | — | 1 | 5.80 |
| CHEMBL3094411 | — | — | 1 | 5.77 |
| CHEMBL3094427 | — | — | 1 | 5.77 |
| CHEMBL3094416 | — | — | 1 | 5.75 |
| CHEMBL3094410 | — | — | 1 | 5.72 |
| CHEMBL3091496 | — | — | 1 | 5.64 |
| CHEMBL29097 | — | — | 1 | 5.62 |
| CHEMBL3094417 | — | — | 1 | 5.30 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3094419 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3094412 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3094418 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3094420 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3094421 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3091497 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3094422 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3094428 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3094414 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3094413 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3094425 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3094431 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3091499 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3091498 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3091500 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3094424 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3094432 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3094423 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3094426 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3094433 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3091495 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3094415 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3094411 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3094427 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3094416 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3094410 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3091496 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL29097 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3094417 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL93 | ZILEUTON | IC50 | - | — | - |