Assay Detail
Binding
CHEMBL3772154
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Inhibition of microsomal PGES1 in ILbeta-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis
9
Total Activities
9
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
Targeting microsomal prostaglandin E2synthase-1 (mPGES-1): the development of inhibitors as an alternative to non-steroidal anti-inflammatory drugs (NSAIDs)
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.06 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140 | CURCUMIN | 3.0 | 1 | 6.70 |
| CHEMBL225421 | ARZANOL | — | 1 | 6.40 |
| CHEMBL3134416 | — | — | 1 | 6.40 |
| CHEMBL171637 | PHYSODIC ACID | — | 1 | 6.37 |
| CHEMBL3770045 | — | — | 1 | 6.10 |
| CHEMBL3770744 | — | — | 1 | 6.00 |
| CHEMBL3770253 | — | — | 1 | 5.94 |
| CHEMBL218693 | CARNOSOL | — | 1 | 5.30 |
| CHEMBL484853 | CARNOSIC ACID | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140 | CURCUMIN | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL225421 | ARZANOL | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3134416 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL171637 | PHYSODIC ACID | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3770045 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3770744 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3770253 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL218693 | CARNOSOL | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL484853 | CARNOSIC ACID | IC50 | = | 5000.0 | nM | 5.30 |