Assay Detail
Functional
CHEMBL1060374
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Antagonist activity at rat Alpha-1D adrenoceptor assessed as inhibition if norepenephrine-induced contraction of thoracic aorta
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Thoracic aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 8.52 | 9.21 |
| pKb | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 9.21 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 1 | 8.97 |
| CHEMBL564481 | CYCLODOXAZOSIN | — | 1 | 7.39 |
| CHEMBL549764 | — | — | 1 | - |
| CHEMBL561851 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423294 | CYCLAZOSIN | Kd | = | 0.6166 | nM | 9.21 |
| CHEMBL707 | DOXAZOSIN | Kd | = | 1.072 | nM | 8.97 |
| CHEMBL564481 | CYCLODOXAZOSIN | Kd | = | 40.74 | nM | 7.39 |
| CHEMBL549764 | — | pKb | = | 6.88 | — | - |
| CHEMBL561851 | — | pKb | = | 8.64 | — | - |