Assay Detail
Binding
CHEMBL678074
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Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
6
Total Activities
6
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 |
|---|---|---|---|
| Ki | 6 | 9.11 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL109648 | CLAZOSENTAN | 3.0 | 1 | 9.89 |
| CHEMBL25438 | PD-156707 SODIUM | — | 1 | 9.77 |
| CHEMBL326059 | — | — | 1 | 9.37 |
| CHEMBL111612 | ABT-546 | — | 1 | 9.34 |
| CHEMBL431651 | ENRASENTAN | 2.0 | 1 | 8.96 |
| CHEMBL267458 | BMS-182874 | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL109648 | CLAZOSENTAN | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL25438 | PD-156707 SODIUM | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL326059 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL111612 | ABT-546 | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL431651 | ENRASENTAN | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL267458 | BMS-182874 | Ki | = | 48.0 | nM | 7.32 |