Assay Detail
Binding
CHEMBL681519
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| Ki | 3 | 8.96 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1627022 | — | — | 1 | 10.82 |
| CHEMBL175616 | BOSENTAN SODIUM | — | 1 | 7.09 |
| CHEMBL112531 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1627022 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL175616 | BOSENTAN SODIUM | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL112531 | — | Ki | = | 0.0042 | nM | - |