Assay Detail
Functional
CHEMBL4123776
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Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chiral analogues of (+)-cyclazosin as potent α1B-adrenoceptor selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 7.16 | 9.23 |
| pKb | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL342062 | — | — | 1 | 9.23 |
| CHEMBL4128084 | — | — | 1 | 7.79 |
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 7.77 |
| CHEMBL4129461 | — | — | 1 | 7.35 |
| CHEMBL4129291 | — | — | 1 | 6.82 |
| CHEMBL564481 | CYCLODOXAZOSIN | — | 1 | 6.70 |
| CHEMBL4125981 | — | — | 1 | 6.11 |
| CHEMBL4128311 | — | — | 1 | 5.52 |
| CHEMBL4125846 | — | — | 1 | - |
| CHEMBL4128460 | — | — | 1 | - |
| CHEMBL4127078 | — | — | 1 | - |
| CHEMBL4127483 | — | — | 1 | - |
| CHEMBL4126860 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL342062 | — | Kd | = | 0.5888 | nM | 9.23 |
| CHEMBL4128084 | — | Kd | = | 16.22 | nM | 7.79 |
| CHEMBL423294 | CYCLAZOSIN | Kd | = | 16.98 | nM | 7.77 |
| CHEMBL4129461 | — | Kd | = | 44.67 | nM | 7.35 |
| CHEMBL4129291 | — | Kd | = | 151.36 | nM | 6.82 |
| CHEMBL564481 | CYCLODOXAZOSIN | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL4125981 | — | Kd | = | 776.25 | nM | 6.11 |
| CHEMBL4128311 | — | Kd | = | 3019.95 | nM | 5.52 |
| CHEMBL4125846 | — | pKb | = | 6.56 | — | - |
| CHEMBL4128460 | — | pKb | = | 7.17 | — | - |
| CHEMBL4127078 | — | pKb | = | 7.06 | — | - |
| CHEMBL4127483 | — | pKb | = | 5.89 | — | - |
| CHEMBL4126860 | — | pKb | = | 7.02 | — | - |