Assay Detail
Binding
CHEMBL679113
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Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A10 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Selective endothelin A receptor antagonists. 4. Discovery and structure-activity relationships of stilbene acid and alcohol derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.11 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90320 | — | — | 1 | 8.10 |
| CHEMBL328600 | — | — | 1 | 7.10 |
| CHEMBL92842 | — | — | 1 | 6.82 |
| CHEMBL330255 | — | — | 1 | 6.70 |
| CHEMBL433201 | — | — | 1 | 6.70 |
| CHEMBL91810 | — | — | 1 | 6.52 |
| CHEMBL90191 | — | — | 1 | 6.52 |
| CHEMBL93411 | — | — | 1 | 6.40 |
| CHEMBL328786 | — | — | 1 | 6.30 |
| CHEMBL90666 | — | — | 1 | 6.22 |
| CHEMBL330543 | — | — | 1 | 6.22 |
| CHEMBL328580 | — | — | 1 | 6.22 |
| CHEMBL328057 | — | — | 1 | 6.16 |
| CHEMBL328464 | — | — | 1 | 6.16 |
| CHEMBL419694 | — | — | 1 | 6.10 |
| CHEMBL92446 | — | — | 1 | 6.05 |
| CHEMBL328964 | — | — | 1 | 6.00 |
| CHEMBL327861 | — | — | 1 | 5.96 |
| CHEMBL328444 | — | — | 1 | 5.89 |
| CHEMBL91741 | — | — | 1 | 5.89 |
| CHEMBL93596 | — | — | 1 | 5.85 |
| CHEMBL91965 | — | — | 1 | 5.70 |
| CHEMBL92570 | — | — | 1 | 5.70 |
| CHEMBL92876 | — | — | 1 | 5.68 |
| CHEMBL90094 | — | — | 1 | 5.52 |
| CHEMBL92092 | — | — | 1 | 5.51 |
| CHEMBL92402 | — | — | 1 | 5.28 |
| CHEMBL92607 | — | — | 1 | 5.22 |
| CHEMBL96836 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90320 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL328600 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL92842 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL330255 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL433201 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL91810 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL90191 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL93411 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL328786 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL90666 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL330543 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL328580 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL328057 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL328464 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL419694 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL92446 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL328964 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL327861 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL328444 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL91741 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL93596 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL91965 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL92570 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL92876 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL90094 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL92092 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL92402 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL92607 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL96836 | — | IC50 | = | 20000.0 | nM | 4.70 |