Assay Detail
Binding
CHEMBL1059941
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human COX2 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.97 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL551829 | — | — | 1 | 9.60 |
| CHEMBL551148 | — | — | 1 | 9.55 |
| CHEMBL561891 | — | — | 1 | 9.30 |
| CHEMBL549393 | — | — | 1 | 8.89 |
| CHEMBL539663 | — | — | 1 | 8.70 |
| CHEMBL561609 | — | — | 1 | 8.62 |
| CHEMBL559613 | — | — | 1 | 8.52 |
| CHEMBL558728 | — | — | 1 | 8.30 |
| CHEMBL563322 | — | — | 1 | 8.30 |
| CHEMBL561950 | — | — | 1 | 8.25 |
| CHEMBL561086 | — | — | 1 | 8.14 |
| CHEMBL560887 | — | — | 1 | 7.96 |
| CHEMBL560284 | — | — | 1 | 7.80 |
| CHEMBL559886 | — | — | 1 | 7.75 |
| CHEMBL550473 | — | — | 1 | 7.54 |
| CHEMBL122 | ROFECOXIB | 4.0 | 1 | 7.50 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 7.17 |
| CHEMBL865 | VALDECOXIB | 4.0 | 1 | 6.74 |
| CHEMBL558727 | — | — | 1 | 6.57 |
| CHEMBL416146 | ETORICOXIB | 4.0 | 1 | 6.46 |
| CHEMBL540166 | — | — | 1 | 5.77 |
| CHEMBL563759 | — | — | 1 | - |
| CHEMBL563262 | — | — | 1 | - |
| CHEMBL570773 | — | — | 1 | - |
| CHEMBL551830 | — | — | 1 | - |
| CHEMBL549927 | — | — | 1 | - |
| CHEMBL557874 | — | — | 1 | - |
| CHEMBL560285 | — | — | 1 | - |
| CHEMBL538418 | — | — | 1 | - |
| CHEMBL559812 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL551829 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL551148 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL561891 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL549393 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL539663 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL561609 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL559613 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL558728 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL563322 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL561950 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL561086 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL560887 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL560284 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL559886 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL550473 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL122 | ROFECOXIB | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL118 | CELECOXIB | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL865 | VALDECOXIB | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL558727 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL416146 | ETORICOXIB | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL540166 | — | IC50 | = | 1683.0 | nM | 5.77 |
| CHEMBL563759 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL563262 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL570773 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL551830 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL549927 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL557874 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL560285 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL538418 | — | IC50 | < | 1.4 | nM | - |
| CHEMBL559812 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL549519 | — | IC50 | > | 10000.0 | nM | - |