Assay Detail
Functional
CHEMBL676490
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Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rodentia sp. |
| Cell Type | MMQ |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 9.33 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL109644 | — | — | 1 | 9.85 |
| CHEMBL323464 | — | — | 1 | 9.42 |
| CHEMBL111277 | — | — | 1 | 9.32 |
| CHEMBL325581 | — | — | 1 | 9.26 |
| CHEMBL419367 | — | — | 1 | 8.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL109644 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL323464 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL111277 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL325581 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL419367 | — | IC50 | = | 1.66 | nM | 8.78 |