Assay Detail
Binding
CHEMBL2393934
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Inhibition of mPGES-1 (unknown origin) using PGH2 as substrate assessed as PGE2 synthesis by ELISA
26
Total Activities
25
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 |
Publication
Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.11 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2391142 | — | — | 1 | 8.70 |
| CHEMBL2391299 | — | — | 1 | 8.52 |
| CHEMBL2325079 | — | — | 1 | 8.52 |
| CHEMBL2391140 | — | — | 1 | 8.52 |
| CHEMBL2391141 | — | — | 1 | 8.52 |
| CHEMBL2391295 | — | — | 1 | 8.22 |
| CHEMBL2391296 | — | — | 1 | 7.82 |
| CHEMBL2391297 | — | — | 1 | 7.80 |
| CHEMBL2391294 | — | — | 1 | 7.70 |
| CHEMBL2325084 | — | — | 1 | 7.60 |
| CHEMBL2325075 | — | — | 1 | 7.48 |
| CHEMBL2391289 | — | — | 1 | 7.33 |
| CHEMBL2391298 | — | — | 1 | 7.31 |
| CHEMBL2325080 | — | — | 2 | 7.19 |
| CHEMBL2391293 | — | — | 1 | 7.06 |
| CHEMBL2315861 | — | — | 1 | 6.66 |
| CHEMBL2315877 | — | — | 1 | 6.07 |
| CHEMBL521286 | — | — | 1 | 5.89 |
| CHEMBL2391287 | — | — | 1 | 5.82 |
| CHEMBL2315860 | — | — | 1 | 5.44 |
| CHEMBL2391288 | — | — | 1 | 5.31 |
| CHEMBL2391290 | — | — | 1 | 5.24 |
| CHEMBL2325081 | — | — | 1 | 5.17 |
| CHEMBL2391291 | — | — | 1 | - |
| CHEMBL2391292 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2391142 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2391299 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2325079 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2391140 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2391141 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2391295 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2391296 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2391297 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2391294 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2325084 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2325075 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2391289 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2391298 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2325080 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2391293 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL2325080 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL2315861 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2315877 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL521286 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2391287 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2315860 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL2391288 | — | IC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL2391290 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2325081 | — | IC50 | = | 6750.0 | nM | 5.17 |
| CHEMBL2391291 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL2391292 | — | IC50 | > | 33000.0 | nM | - |