Assay Detail
Functional
CHEMBL1060372
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Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| 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 |
|---|---|---|---|
| pKb | 3 | - | - |
| Kd | 2 | 8.80 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 8.91 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 1 | 8.69 |
| CHEMBL564481 | CYCLODOXAZOSIN | — | 1 | - |
| CHEMBL549764 | — | — | 1 | - |
| CHEMBL561851 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423294 | CYCLAZOSIN | Kd | = | 1.23 | nM | 8.91 |
| CHEMBL707 | DOXAZOSIN | Kd | = | 2.042 | nM | 8.69 |
| CHEMBL564481 | CYCLODOXAZOSIN | pKb | = | 7.21 | — | - |
| CHEMBL549764 | — | pKb | = | 5.88 | — | - |
| CHEMBL561851 | — | pKb | = | 8.51 | — | - |