Assay Detail
Binding
CHEMBL4426313
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Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in 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 | Autocuration |
Publication
From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.46 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989834 | AVOSENTAN | 3.0 | 1 | 8.85 |
| CHEMBL109648 | CLAZOSENTAN | 3.0 | 1 | 8.77 |
| CHEMBL61780 | TEZOSENTAN | 3.0 | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989834 | AVOSENTAN | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL109648 | CLAZOSENTAN | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL61780 | TEZOSENTAN | IC50 | = | 18.0 | nM | 7.75 |