Assay Detail
Functional
CHEMBL811786
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Compound was tested for TXA2 receptor antagonism by measuring its ability to inhibit contraction of rat aorta induced by the stable TXA2 agonist U-46,619 at 1 umol
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Aorta |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Thromboxane modulating agents. 2. Thromboxane receptor antagonists derived from the thromboxane synthase inhibitor dazmegrel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 8.57 | 9.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43770 | — | — | 1 | 9.76 |
| CHEMBL43772 | — | — | 1 | 9.63 |
| CHEMBL47372 | — | — | 1 | 9.57 |
| CHEMBL48128 | — | — | 1 | 9.32 |
| CHEMBL44660 | — | — | 1 | 9.17 |
| CHEMBL47612 | — | — | 1 | 8.85 |
| CHEMBL47611 | — | — | 1 | 8.56 |
| CHEMBL43768 | — | — | 1 | 8.43 |
| CHEMBL44998 | — | — | 1 | 7.00 |
| CHEMBL45075 | — | — | 1 | 5.42 |
| CHEMBL283656 | DAZMEGREL | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL43770 | — | Kd | = | 0.1738 | nM | 9.76 |
| CHEMBL43772 | — | Kd | = | 0.2344 | nM | 9.63 |
| CHEMBL47372 | — | Kd | = | 0.2692 | nM | 9.57 |
| CHEMBL48128 | — | Kd | = | 0.4786 | nM | 9.32 |
| CHEMBL44660 | — | Kd | = | 0.6761 | nM | 9.17 |
| CHEMBL47612 | — | Kd | = | 1.413 | nM | 8.85 |
| CHEMBL47611 | — | Kd | = | 2.754 | nM | 8.56 |
| CHEMBL43768 | — | Kd | = | 3.715 | nM | 8.43 |
| CHEMBL44998 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL45075 | — | Kd | = | 3801.89 | nM | 5.42 |
| CHEMBL283656 | DAZMEGREL | Kd | > | 1000.0 | nM | - |