Assay Detail
Binding
CHEMBL1050554
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Inhibition of mPGES1 in IL-1-beta-stimulated human A549 cells assessed as blockade of PGH2 to PGE2 conversion in presence of 50% fetal bovine serum
27
Total Activities
27
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 | Intermediate |
Publication
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.47 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483900 | — | — | 1 | 7.89 |
| CHEMBL585690 | — | — | 1 | 7.68 |
| CHEMBL585134 | — | — | 1 | 7.57 |
| CHEMBL584930 | — | — | 1 | 7.47 |
| CHEMBL585116 | — | — | 1 | 7.42 |
| CHEMBL585295 | — | — | 1 | 7.35 |
| CHEMBL568565 | — | — | 1 | 7.24 |
| CHEMBL585857 | — | — | 1 | 7.22 |
| CHEMBL567714 | — | — | 1 | 7.12 |
| CHEMBL568546 | — | — | 1 | 6.96 |
| CHEMBL566262 | — | — | 1 | 6.55 |
| CHEMBL568576 | — | — | 1 | 6.48 |
| CHEMBL412099 | — | — | 1 | 6.38 |
| CHEMBL585763 | — | — | 1 | 6.35 |
| CHEMBL568545 | — | — | 1 | 6.15 |
| CHEMBL566446 | — | — | 1 | 6.14 |
| CHEMBL568125 | — | — | 1 | 6.00 |
| CHEMBL585486 | — | — | 1 | 5.96 |
| CHEMBL584932 | — | — | 1 | 5.96 |
| CHEMBL585110 | — | — | 1 | 5.70 |
| CHEMBL568366 | — | — | 1 | 5.64 |
| CHEMBL270347 | — | — | 1 | 5.58 |
| CHEMBL566261 | — | — | 1 | 5.52 |
| CHEMBL567282 | — | — | 1 | 5.37 |
| CHEMBL568551 | — | — | 1 | 5.30 |
| CHEMBL566445 | — | — | 1 | 5.13 |
| CHEMBL565831 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483900 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL585690 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL585134 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL584930 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL585116 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL585295 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL568565 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL585857 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL567714 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL568546 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL566262 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL568576 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL412099 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL585763 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL568545 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL566446 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL568125 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL585486 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL584932 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL585110 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL568366 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL270347 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL566261 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL567282 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL568551 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL566445 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL565831 | — | IC50 | > | 50000.0 | nM | - |