Assay Detail
Binding
CHEMBL3873577
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min in presence of GSH
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 33 | 7.74 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL412099 | — | — | 1 | 8.72 |
| CHEMBL3961834 | — | — | 1 | 8.49 |
| CHEMBL3916119 | — | — | 1 | 8.45 |
| CHEMBL3931344 | — | — | 1 | 8.41 |
| CHEMBL3944077 | — | — | 1 | 8.38 |
| CHEMBL3926181 | — | — | 1 | 8.18 |
| CHEMBL3984373 | — | — | 1 | 8.14 |
| CHEMBL3898125 | — | — | 1 | 8.10 |
| CHEMBL3897959 | — | — | 1 | 8.10 |
| CHEMBL3935630 | — | — | 1 | 8.07 |
| CHEMBL3925606 | — | — | 1 | 8.04 |
| CHEMBL3895356 | — | — | 1 | 7.98 |
| CHEMBL3920280 | — | — | 1 | 7.97 |
| CHEMBL3926203 | — | — | 1 | 7.96 |
| CHEMBL3932436 | — | — | 1 | 7.95 |
| CHEMBL3935105 | — | — | 1 | 7.90 |
| CHEMBL3909776 | — | — | 1 | 7.87 |
| CHEMBL3949380 | — | — | 1 | 7.83 |
| CHEMBL3987179 | — | — | 1 | 7.82 |
| CHEMBL3891935 | — | — | 1 | 7.79 |
| CHEMBL3956753 | — | — | 1 | 7.73 |
| CHEMBL3955759 | — | — | 1 | 7.68 |
| CHEMBL3918689 | — | — | 1 | 7.65 |
| CHEMBL3908580 | — | — | 1 | 7.33 |
| CHEMBL3961512 | — | — | 1 | 7.31 |
| CHEMBL3934012 | — | — | 1 | 7.15 |
| CHEMBL3976312 | — | — | 1 | 7.15 |
| CHEMBL3925125 | — | — | 1 | 7.14 |
| CHEMBL3952826 | — | — | 1 | 7.11 |
| CHEMBL3947032 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL412099 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3961834 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3916119 | — | IC50 | = | 3.56 | nM | 8.45 |
| CHEMBL3931344 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3944077 | — | IC50 | = | 4.19 | nM | 8.38 |
| CHEMBL3926181 | — | IC50 | = | 6.59 | nM | 8.18 |
| CHEMBL3984373 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3898125 | — | IC50 | = | 7.99 | nM | 8.10 |
| CHEMBL3897959 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3935630 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3925606 | — | IC50 | = | 9.09 | nM | 8.04 |
| CHEMBL3895356 | — | IC50 | = | 10.41 | nM | 7.98 |
| CHEMBL3920280 | — | IC50 | = | 10.79 | nM | 7.97 |
| CHEMBL3926203 | — | IC50 | = | 11.04 | nM | 7.96 |
| CHEMBL3932436 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL3935105 | — | IC50 | = | 12.53 | nM | 7.90 |
| CHEMBL3909776 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL3949380 | — | IC50 | = | 14.65 | nM | 7.83 |
| CHEMBL3987179 | — | IC50 | = | 15.25 | nM | 7.82 |
| CHEMBL3891935 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL3956753 | — | IC50 | = | 18.66 | nM | 7.73 |
| CHEMBL3955759 | — | IC50 | = | 20.69 | nM | 7.68 |
| CHEMBL3918689 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL3908580 | — | IC50 | = | 46.6 | nM | 7.33 |
| CHEMBL3961512 | — | IC50 | = | 49.47 | nM | 7.31 |
| CHEMBL3934012 | — | IC50 | = | 70.85 | nM | 7.15 |
| CHEMBL3976312 | — | IC50 | = | 70.96 | nM | 7.15 |
| CHEMBL3925125 | — | IC50 | = | 71.82 | nM | 7.14 |
| CHEMBL3952826 | — | IC50 | = | 77.55 | nM | 7.11 |
| CHEMBL3947032 | — | IC50 | = | 103.3 | nM | 6.99 |
| CHEMBL3929200 | — | IC50 | = | 141.2 | nM | 6.85 |
| CHEMBL3900544 | — | IC50 | = | 154.2 | nM | 6.81 |
| CHEMBL3971684 | — | IC50 | = | 415.1 | nM | 6.38 |