Assay Detail
Binding
CHEMBL921788
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Inhibition of human COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
22
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 12 | - | - |
| IC50 | 10 | 7.11 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL76084 | — | — | 2 | 7.70 |
| CHEMBL139 | DICLOFENAC | 4.0 | 2 | 7.55 |
| CHEMBL407109 | — | — | 2 | 7.55 |
| CHEMBL76154 | — | — | 2 | 7.33 |
| CHEMBL259218 | — | — | 2 | 7.33 |
| CHEMBL407368 | — | — | 2 | 7.22 |
| CHEMBL404108 | LUMIRACOXIB | 4.0 | 2 | 6.97 |
| CHEMBL258738 | — | — | 2 | 6.78 |
| CHEMBL259842 | — | — | 2 | 6.49 |
| CHEMBL408156 | — | — | 2 | 6.20 |
| CHEMBL258969 | — | — | 1 | - |
| CHEMBL260111 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL76084 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL407109 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL139 | DICLOFENAC | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL259218 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL76154 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL407368 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL404108 | LUMIRACOXIB | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL258738 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL259842 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL408156 | — | IC50 | = | 629.0 | nM | 6.20 |
| CHEMBL404108 | LUMIRACOXIB | Inhibition | = | 50.0 | % | - |
| CHEMBL259218 | — | Inhibition | = | 90.0 | % | - |
| CHEMBL258969 | — | Inhibition | = | 30.0 | % | - |
| CHEMBL407109 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL259842 | — | Inhibition | = | 85.0 | % | - |
| CHEMBL407368 | — | Inhibition | = | 95.0 | % | - |
| CHEMBL139 | DICLOFENAC | Inhibition | = | 90.0 | % | - |
| CHEMBL260111 | — | Inhibition | = | 40.0 | % | - |
| CHEMBL76154 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL76084 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL408156 | — | Inhibition | = | 60.0 | % | - |
| CHEMBL258738 | — | Inhibition | = | 100.0 | % | - |