Assay Detail
Binding
CHEMBL4426311
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat aortic ring ETA receptor in presence of ET1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 6.76 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448273 | — | — | 1 | 7.70 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 7.40 |
| CHEMBL4438132 | — | — | 1 | 6.90 |
| CHEMBL4525321 | — | — | 1 | 6.02 |
| CHEMBL4590568 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448273 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL957 | BOSENTAN | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL4438132 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL4525321 | — | Kd | = | 954.99 | nM | 6.02 |
| CHEMBL4590568 | — | Kd | = | 1584.89 | nM | 5.80 |