Assay Detail
Binding
CHEMBL679715
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Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
9
Total Activities
9
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
Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.65 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303185 | — | — | 1 | 7.66 |
| CHEMBL293874 | — | — | 1 | 7.50 |
| CHEMBL303204 | — | — | 1 | 7.47 |
| CHEMBL307324 | — | — | 1 | 7.46 |
| CHEMBL302776 | — | — | 1 | 6.96 |
| CHEMBL304756 | — | — | 1 | 6.39 |
| CHEMBL1790499 | — | — | 1 | 5.85 |
| CHEMBL3349461 | — | — | 1 | 5.52 |
| CHEMBL308208 | — | — | 1 | 5.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303185 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL293874 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL303204 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL307324 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL302776 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL304756 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1790499 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3349461 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL308208 | — | IC50 | = | 8500.0 | nM | 5.07 |