Assay Detail
Functional
CHEMBL4123778
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Antagonist activity at alpha1D adrenergic receptor in Wistar rat thoracic aorta assessed as inhibition of noradrenaline-induced contraction measured after 30 mins in presence of cocaine hydrochloride and beta-adrenoceptor blocker propranolol 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 | 11 | 7.52 | 10.12 |
| pKb | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL342062 | — | — | 1 | 10.12 |
| CHEMBL4128084 | — | — | 1 | 9.28 |
| CHEMBL4129461 | — | — | 1 | 8.66 |
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 7.27 |
| CHEMBL4129291 | — | — | 1 | 7.23 |
| CHEMBL4126860 | — | — | 1 | 7.23 |
| CHEMBL4125846 | — | — | 1 | 6.87 |
| CHEMBL4128460 | — | — | 1 | 6.85 |
| CHEMBL4127078 | — | — | 1 | 6.81 |
| CHEMBL4125981 | — | — | 1 | 6.62 |
| CHEMBL4128311 | — | — | 1 | 5.77 |
| CHEMBL564481 | CYCLODOXAZOSIN | — | 1 | - |
| CHEMBL4127483 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL342062 | — | Kd | = | 0.07586 | nM | 10.12 |
| CHEMBL4128084 | — | Kd | = | 0.5248 | nM | 9.28 |
| CHEMBL4129461 | — | Kd | = | 2.188 | nM | 8.66 |
| CHEMBL423294 | CYCLAZOSIN | Kd | = | 53.7 | nM | 7.27 |
| CHEMBL4129291 | — | Kd | = | 58.88 | nM | 7.23 |
| CHEMBL4126860 | — | Kd | = | 58.88 | nM | 7.23 |
| CHEMBL4125846 | — | Kd | = | 134.9 | nM | 6.87 |
| CHEMBL4128460 | — | Kd | = | 141.25 | nM | 6.85 |
| CHEMBL4127078 | — | Kd | = | 154.88 | nM | 6.81 |
| CHEMBL4125981 | — | Kd | = | 239.88 | nM | 6.62 |
| CHEMBL4128311 | — | Kd | = | 1698.24 | nM | 5.77 |
| CHEMBL564481 | CYCLODOXAZOSIN | pKb | = | 7.1 | — | - |
| CHEMBL4127483 | — | pKb | = | 6.22 | — | - |