Assay Detail
Binding
CHEMBL677974
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Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Potent and selective ET-A antagonists. 2. Discovery and evaluation of potent and water soluble N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 9.44 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL114298 | — | — | 1 | 10.40 |
| CHEMBL324184 | — | — | 1 | 10.40 |
| CHEMBL115147 | — | — | 1 | 8.85 |
| CHEMBL175616 | BOSENTAN SODIUM | — | 1 | 8.12 |
| CHEMBL116046 | — | — | 1 | - |
| CHEMBL324613 | — | — | 1 | - |
| CHEMBL115372 | — | — | 1 | - |
| CHEMBL112531 | — | — | 1 | - |
| CHEMBL115871 | — | — | 1 | - |
| CHEMBL112624 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL114298 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL324184 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL115147 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL175616 | BOSENTAN SODIUM | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL116046 | — | IC50 | < | 0.001 | nM | - |
| CHEMBL324613 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL115372 | — | IC50 | = | 0.0026 | nM | - |
| CHEMBL112531 | — | IC50 | < | 0.001 | nM | - |
| CHEMBL115871 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL112624 | — | IC50 | = | 0.0062 | nM | - |