Assay Detail
Binding
CHEMBL676632
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Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | ovary |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.63 | 5.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL432974 | — | — | 1 | 5.55 |
| CHEMBL111612 | ABT-546 | — | 1 | 4.81 |
| CHEMBL110053 | — | — | 1 | 4.75 |
| CHEMBL109778 | — | — | 1 | 4.50 |
| CHEMBL109926 | — | — | 1 | 4.40 |
| CHEMBL322537 | — | — | 1 | 4.38 |
| CHEMBL323951 | — | — | 1 | 4.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL432974 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL111612 | ABT-546 | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL110053 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL109778 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL109926 | — | IC50 | = | 39700.0 | nM | 4.40 |
| CHEMBL322537 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL323951 | — | IC50 | = | 92700.0 | nM | 4.03 |