Assay Detail
Binding
CHEMBL4426320
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Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
2
Total Activities
2
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 | 2 | 6.59 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1628620 | — | — | 1 | 7.16 |
| CHEMBL2103873 | MACITENTAN | 4.0 | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1628620 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2103873 | MACITENTAN | IC50 | = | 987.0 | nM | 6.01 |