Assay Detail
Binding
CHEMBL3873579
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Inhibition of mPGES-1 in human whole blood assessed as reduction in LPS-induced PGE2 production preincubated followed by LPS stimulation for 20 to 24 hrs
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2',3':3,4]benzo[1,2-d]imidazole-5-carboxamide as potent, selective and efficacious microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.16 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3897959 | — | — | 1 | 6.60 |
| CHEMBL3916119 | — | — | 1 | 6.56 |
| CHEMBL3987179 | — | — | 1 | 6.27 |
| CHEMBL3926203 | — | — | 1 | 6.20 |
| CHEMBL3984373 | — | — | 1 | 6.08 |
| CHEMBL3895356 | — | — | 1 | 6.02 |
| CHEMBL3925606 | — | — | 1 | 5.95 |
| CHEMBL412099 | — | — | 1 | 5.87 |
| CHEMBL3898125 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3897959 | — | IC50 | = | 249.9 | nM | 6.60 |
| CHEMBL3916119 | — | IC50 | = | 277.3 | nM | 6.56 |
| CHEMBL3987179 | — | IC50 | = | 541.9 | nM | 6.27 |
| CHEMBL3926203 | — | IC50 | = | 632.5 | nM | 6.20 |
| CHEMBL3984373 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL3895356 | — | IC50 | = | 959.6 | nM | 6.02 |
| CHEMBL3925606 | — | IC50 | = | 1127.0 | nM | 5.95 |
| CHEMBL412099 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL3898125 | — | IC50 | = | 1388.0 | nM | 5.86 |