Assay Detail
Binding
CHEMBL865437
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Inhibition of COX1 in canine whole blood
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Prostaglandin G/H synthase 1 (CHEMBL4133) ↗| Type | SINGLE PROTEIN |
| Organism | Canis lupus familiaris |
Publication
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.04 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL205308 | — | — | 1 | 5.70 |
| CHEMBL205351 | — | — | 1 | 5.70 |
| CHEMBL205938 | — | — | 1 | 5.57 |
| CHEMBL378649 | — | — | 1 | 5.47 |
| CHEMBL380457 | — | — | 1 | 5.42 |
| CHEMBL383409 | — | — | 1 | 5.30 |
| CHEMBL380148 | — | — | 1 | 5.26 |
| CHEMBL205331 | — | — | 1 | 4.96 |
| CHEMBL208450 | — | — | 1 | 4.92 |
| CHEMBL381834 | — | — | 1 | 4.90 |
| CHEMBL383272 | — | — | 1 | 4.81 |
| CHEMBL377797 | — | — | 1 | 4.80 |
| CHEMBL206359 | — | — | 1 | 4.74 |
| CHEMBL207702 | — | — | 1 | 4.64 |
| CHEMBL206207 | — | — | 1 | 4.63 |
| CHEMBL378875 | — | — | 1 | 4.55 |
| CHEMBL383210 | — | — | 1 | 4.30 |
| CHEMBL383064 | — | — | 1 | - |
| CHEMBL377284 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL205308 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL205351 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL205938 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL378649 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL380457 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL383409 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL380148 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL205331 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL208450 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL381834 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL383272 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL377797 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL206359 | — | IC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL207702 | — | IC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL206207 | — | IC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL378875 | — | IC50 | = | 27900.0 | nM | 4.55 |
| CHEMBL383210 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL383064 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL377284 | — | IC50 | > | 50000.0 | nM | - |