Assay Detail
Binding
CHEMBL872385
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Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 |
|---|---|---|---|
| IC50 | 10 | 9.21 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | 2.0 | 1 | 9.82 |
| CHEMBL1790959 | — | — | 1 | 9.74 |
| CHEMBL1790963 | — | — | 1 | 9.72 |
| CHEMBL1790960 | — | — | 1 | 9.70 |
| CHEMBL1790962 | — | — | 1 | 9.38 |
| CHEMBL2373291 | — | — | 1 | 9.21 |
| CHEMBL2373292 | — | — | 1 | 9.15 |
| CHEMBL427748 | — | — | 1 | 9.12 |
| CHEMBL438733 | — | — | 1 | 8.23 |
| CHEMBL411171 | — | — | 1 | 8.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL1790959 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL1790963 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL1790960 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1790962 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL2373291 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL2373292 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL427748 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL438733 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL411171 | — | IC50 | = | 8.6 | nM | 8.07 |