Assay Detail
Binding
CHEMBL2384262
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Inhibition of COX-1 in human whole blood assessed as inhibition of serum TXB2 level after 1 hr by radioimmunoassay
22
Total Activities
22
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 | Autocuration |
Publication
Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.62 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2380863 | — | — | 1 | 6.57 |
| CHEMBL2380867 | — | — | 1 | 6.50 |
| CHEMBL2380876 | — | — | 1 | 6.48 |
| CHEMBL363228 | — | — | 1 | 6.30 |
| CHEMBL2380864 | — | — | 1 | 6.09 |
| CHEMBL2380862 | — | — | 1 | 5.89 |
| CHEMBL2380865 | — | — | 1 | 5.72 |
| CHEMBL2380866 | — | — | 1 | 5.72 |
| CHEMBL2380874 | — | — | 1 | 5.66 |
| CHEMBL2380870 | — | — | 1 | 5.38 |
| CHEMBL2380871 | — | — | 1 | 5.30 |
| CHEMBL1710350 | — | — | 1 | 4.76 |
| CHEMBL2380877 | — | — | 1 | 4.76 |
| CHEMBL2380869 | — | — | 1 | 4.72 |
| CHEMBL2380861 | — | — | 1 | 4.43 |
| CHEMBL2380868 | — | — | 1 | - |
| CHEMBL2380872 | — | — | 1 | - |
| CHEMBL2380873 | — | — | 1 | - |
| CHEMBL2380875 | — | — | 1 | - |
| CHEMBL2380878 | — | — | 1 | - |
| CHEMBL2380879 | — | — | 1 | - |
| CHEMBL2380880 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2380863 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2380867 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2380876 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL363228 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2380864 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL2380862 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2380865 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2380866 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2380874 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2380870 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL2380871 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1710350 | — | IC50 | = | 17280.0 | nM | 4.76 |
| CHEMBL2380877 | — | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL2380869 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL2380861 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL2380868 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2380872 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2380873 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2380875 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2380878 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2380879 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2380880 | — | IC50 | > | 100000.0 | nM | - |