Assay Detail
Functional
CHEMBL764629
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ETA receptor antagonist activity was measured by inhibition of ET-1 induced vasoconstriction in isolated porcine coronary artery
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Sus scrofa |
| Tissue | Coronary artery |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 7.03 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2373291 | — | — | 1 | 7.70 |
| CHEMBL1790962 | — | — | 1 | 7.70 |
| CHEMBL2373292 | — | — | 1 | 7.40 |
| CHEMBL411171 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2373291 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL1790962 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL2373292 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL411171 | — | Kd | = | 5011.87 | nM | 5.30 |