Assay Detail
Binding
CHEMBL1059944
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Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 16 | 7.27 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL539663 | — | — | 1 | 7.92 |
| CHEMBL550126 | — | — | 1 | 7.67 |
| CHEMBL551419 | — | — | 1 | 7.66 |
| CHEMBL550537 | — | — | 1 | 7.48 |
| CHEMBL564729 | — | — | 1 | 7.35 |
| CHEMBL551017 | — | — | 1 | 7.20 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 7.20 |
| CHEMBL122 | ROFECOXIB | 4.0 | 1 | 6.97 |
| CHEMBL558929 | — | — | 1 | 5.99 |
| CHEMBL552082 | — | — | 1 | - |
| CHEMBL561005 | — | — | 1 | - |
| CHEMBL552081 | — | — | 1 | - |
| CHEMBL551418 | — | — | 1 | - |
| CHEMBL562791 | — | — | 1 | - |
| CHEMBL550737 | — | — | 1 | - |
| CHEMBL564993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL539663 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL550126 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL551419 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL550537 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL564729 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL551017 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL118 | CELECOXIB | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL122 | ROFECOXIB | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL558929 | — | IC50 | = | 1034.0 | nM | 5.99 |
| CHEMBL552082 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL561005 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL552081 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL551418 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL562791 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL550737 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL564993 | — | IC50 | < | 10.0 | nM | - |