Assay Detail
Binding
CHEMBL916302
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Inhibition of COX2 in human whole blood assessed as inhibition of LPS-stimulated PGE2 production
29
Total Activities
29
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 | Intermediate |
Publication
Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.87 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224400 | — | — | 1 | 7.05 |
| CHEMBL224136 | — | — | 1 | 6.92 |
| CHEMBL388628 | — | — | 1 | 6.89 |
| CHEMBL224640 | — | — | 1 | 6.82 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 6.46 |
| CHEMBL225092 | — | — | 1 | 6.36 |
| CHEMBL224612 | — | — | 1 | 6.28 |
| CHEMBL147165 | — | — | 1 | 6.21 |
| CHEMBL56367 | NIMESULIDE | 4.0 | 1 | 6.16 |
| CHEMBL224122 | — | — | 1 | 5.92 |
| CHEMBL225113 | — | — | 1 | 5.82 |
| CHEMBL388625 | — | — | 1 | 5.73 |
| CHEMBL224192 | — | — | 1 | 5.70 |
| CHEMBL224624 | — | — | 1 | 5.63 |
| CHEMBL387879 | — | — | 1 | 5.59 |
| CHEMBL223655 | — | — | 1 | 5.48 |
| CHEMBL224193 | — | — | 1 | 5.12 |
| CHEMBL374169 | — | — | 1 | 5.01 |
| CHEMBL374168 | — | — | 1 | 4.86 |
| CHEMBL376143 | — | — | 1 | 4.85 |
| CHEMBL224401 | — | — | 1 | 4.32 |
| CHEMBL224781 | — | — | 1 | - |
| CHEMBL225236 | — | — | 1 | - |
| CHEMBL389485 | — | — | 1 | - |
| CHEMBL224256 | — | — | 1 | - |
| CHEMBL224693 | — | — | 1 | - |
| CHEMBL224201 | — | — | 1 | - |
| CHEMBL148542 | — | — | 1 | - |
| CHEMBL390317 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224400 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL224136 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL388628 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL224640 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL118 | CELECOXIB | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL225092 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL224612 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL147165 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL56367 | NIMESULIDE | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL224122 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL225113 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL388625 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL224192 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL224624 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL387879 | — | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL223655 | — | IC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL224193 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL374169 | — | IC50 | = | 9690.0 | nM | 5.01 |
| CHEMBL374168 | — | IC50 | = | 13840.0 | nM | 4.86 |
| CHEMBL376143 | — | IC50 | = | 14110.0 | nM | 4.85 |
| CHEMBL224401 | — | IC50 | = | 47620.0 | nM | 4.32 |
| CHEMBL224781 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL225236 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL389485 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL224256 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL224693 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL224201 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL148542 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL390317 | — | IC50 | > | 100000.0 | nM | - |