Assay Detail
Functional
CHEMBL676578
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Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 2 | 8.30 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL72037 | — | — | 1 | 9.30 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL72037 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL957 | BOSENTAN | Kd | = | 50.12 | nM | 7.30 |