Assay Detail
Binding
CHEMBL916301
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Inhibition of COX1 in human whole blood assessed as inhibition of calcium ionophore A-23187-stimulated platelet aggregation by measuring TXB2 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 | 5.85 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL147165 | — | — | 1 | 6.85 |
| CHEMBL224400 | — | — | 1 | 6.75 |
| CHEMBL374168 | — | — | 1 | 6.62 |
| CHEMBL225092 | — | — | 1 | 6.58 |
| CHEMBL224640 | — | — | 1 | 6.57 |
| CHEMBL225113 | — | — | 1 | 6.44 |
| CHEMBL148542 | — | — | 1 | 6.39 |
| CHEMBL224612 | — | — | 1 | 6.39 |
| CHEMBL224136 | — | — | 1 | 6.21 |
| CHEMBL388628 | — | — | 1 | 5.99 |
| CHEMBL387879 | — | — | 1 | 5.86 |
| CHEMBL224193 | — | — | 1 | 5.85 |
| CHEMBL388625 | — | — | 1 | 5.84 |
| CHEMBL224624 | — | — | 1 | 5.74 |
| CHEMBL374169 | — | — | 1 | 5.64 |
| CHEMBL224693 | — | — | 1 | 5.64 |
| CHEMBL223655 | — | — | 1 | 5.61 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 5.58 |
| CHEMBL224122 | — | — | 1 | 5.44 |
| CHEMBL56367 | NIMESULIDE | 4.0 | 1 | 5.42 |
| CHEMBL224401 | — | — | 1 | 5.33 |
| CHEMBL376143 | — | — | 1 | 5.27 |
| CHEMBL224192 | — | — | 1 | 4.96 |
| CHEMBL389485 | — | — | 1 | 4.74 |
| CHEMBL224781 | — | — | 1 | 4.59 |
| CHEMBL224201 | — | — | 1 | - |
| CHEMBL390317 | — | — | 1 | - |
| CHEMBL224256 | — | — | 1 | - |
| CHEMBL225236 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL147165 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL224400 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL374168 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL225092 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL224640 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL225113 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL148542 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL224612 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL224136 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL388628 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL387879 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL224193 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL388625 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL224624 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL374169 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL224693 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL223655 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL118 | CELECOXIB | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL224122 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL56367 | NIMESULIDE | IC50 | = | 3760.0 | nM | 5.42 |
| CHEMBL224401 | — | IC50 | = | 4630.0 | nM | 5.33 |
| CHEMBL376143 | — | IC50 | = | 5340.0 | nM | 5.27 |
| CHEMBL224192 | — | IC50 | = | 10860.0 | nM | 4.96 |
| CHEMBL389485 | — | IC50 | = | 18360.0 | nM | 4.74 |
| CHEMBL224781 | — | IC50 | = | 25610.0 | nM | 4.59 |
| CHEMBL224201 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL390317 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL224256 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL225236 | — | IC50 | > | 100000.0 | nM | - |