Assay Detail
Functional
CHEMBL676580
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Evaluation for functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 13 | 8.32 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70293 | — | — | 1 | 10.00 |
| CHEMBL70385 | — | — | 1 | 9.70 |
| CHEMBL70303 | — | — | 1 | 9.00 |
| CHEMBL70203 | — | — | 1 | 9.00 |
| CHEMBL70895 | — | — | 1 | 8.30 |
| CHEMBL70365 | — | — | 1 | 8.00 |
| CHEMBL70339 | — | — | 1 | 8.00 |
| CHEMBL303428 | — | — | 1 | 7.90 |
| CHEMBL71070 | — | — | 1 | 7.80 |
| CHEMBL70487 | — | — | 1 | 7.70 |
| CHEMBL303649 | — | — | 1 | 7.60 |
| CHEMBL308088 | — | — | 1 | 6.80 |
| CHEMBL72037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70293 | — | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL70385 | — | Kd | = | 0.1995 | nM | 9.70 |
| CHEMBL70303 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL70203 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL70895 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL70365 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL70339 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL303428 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL71070 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL70487 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL303649 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL308088 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL72037 | — | Kd | = | 125892541.18 | nM | - |