Assay Detail
Binding
CHEMBL820600
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TXA2 synthetase inhibition measured by the inhibition of TXB2 formation by human gel-filtered platelets incubated with [14C]arachidonic acid
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
On the bioisosteric potential of diazines: diazine analogues of the combined thromboxane A2 receptor antagonist and synthetase inhibitor Ridogrel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.49 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129867 | — | — | 1 | 8.22 |
| CHEMBL280728 | RIDOGREL | 2.0 | 1 | 8.15 |
| CHEMBL132385 | — | — | 1 | 7.80 |
| CHEMBL129843 | — | — | 1 | 7.41 |
| CHEMBL131949 | — | — | 1 | 7.12 |
| CHEMBL130564 | — | — | 1 | 7.10 |
| CHEMBL130755 | — | — | 1 | 6.58 |
| CHEMBL337048 | — | — | 1 | 6.24 |
| CHEMBL130790 | — | — | 1 | 6.21 |
| CHEMBL336548 | — | — | 1 | 6.16 |
| CHEMBL131415 | — | — | 1 | 5.54 |
| CHEMBL131334 | — | — | 1 | 5.42 |
| CHEMBL422793 | — | — | 1 | 5.21 |
| CHEMBL337607 | — | — | 1 | 5.18 |
| CHEMBL130823 | — | — | 1 | 5.06 |
| CHEMBL129935 | — | — | 1 | - |
| CHEMBL130365 | — | — | 1 | - |
| CHEMBL130236 | — | — | 1 | - |
| CHEMBL341426 | — | — | 1 | - |
| CHEMBL2111862 | — | — | 1 | - |
| CHEMBL335841 | — | — | 1 | - |
| CHEMBL335717 | — | — | 1 | - |
| CHEMBL129995 | — | — | 1 | - |
| CHEMBL435412 | — | — | 1 | - |
| CHEMBL131078 | — | — | 1 | - |
| CHEMBL128188 | — | — | 1 | - |
| CHEMBL341211 | — | — | 1 | - |
| CHEMBL130785 | — | — | 1 | - |
| CHEMBL132043 | — | — | 1 | - |
| CHEMBL130623 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129867 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL280728 | RIDOGREL | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL132385 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL129843 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL131949 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL130564 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL130755 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL337048 | — | IC50 | = | 573.0 | nM | 6.24 |
| CHEMBL130790 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL336548 | — | IC50 | = | 693.0 | nM | 6.16 |
| CHEMBL131415 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL131334 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL422793 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL337607 | — | IC50 | = | 6633.0 | nM | 5.18 |
| CHEMBL130823 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL131088 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL130341 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL129935 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL130365 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL130236 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL341426 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2111862 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL335841 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL335717 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL129995 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL435412 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL131078 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL128188 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL341211 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL130785 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL132043 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL130623 | — | IC50 | > | 10000.0 | nM | - |