Assay Detail
Functional
CHEMBL4123777
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Antagonist activity at alpha1B adrenergic receptor in Wistar rat spleen assessed as inhibition of phenylephrine-induced contraction incubated for 30 mins in presence of 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 |
|---|---|---|---|
| pKb | 9 | - | - |
| Kd | 4 | 8.30 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129461 | — | — | 1 | 9.21 |
| CHEMBL4128084 | — | — | 1 | 8.74 |
| CHEMBL4128311 | — | — | 1 | 8.52 |
| CHEMBL4129291 | — | — | 1 | 6.72 |
| CHEMBL423294 | CYCLAZOSIN | — | 1 | - |
| CHEMBL4125846 | — | — | 1 | - |
| CHEMBL4125981 | — | — | 1 | - |
| CHEMBL564481 | CYCLODOXAZOSIN | — | 1 | - |
| CHEMBL4128460 | — | — | 1 | - |
| CHEMBL4127078 | — | — | 1 | - |
| CHEMBL4127483 | — | — | 1 | - |
| CHEMBL342062 | — | — | 1 | - |
| CHEMBL4126860 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129461 | — | Kd | = | 0.6166 | nM | 9.21 |
| CHEMBL4128084 | — | Kd | = | 1.82 | nM | 8.74 |
| CHEMBL4128311 | — | Kd | = | 3.02 | nM | 8.52 |
| CHEMBL4129291 | — | Kd | = | 190.55 | nM | 6.72 |
| CHEMBL423294 | CYCLAZOSIN | pKb | = | 8.86 | — | - |
| CHEMBL4125846 | — | pKb | = | 8.05 | — | - |
| CHEMBL4125981 | — | pKb | = | 8.77 | — | - |
| CHEMBL564481 | CYCLODOXAZOSIN | pKb | = | 8.61 | — | - |
| CHEMBL4128460 | — | pKb | = | 8.26 | — | - |
| CHEMBL4127078 | — | pKb | = | 7.99 | — | - |
| CHEMBL4127483 | — | pKb | = | 7.86 | — | - |
| CHEMBL342062 | — | pKb | = | 9.67 | — | - |
| CHEMBL4126860 | — | pKb | = | 7.17 | — | - |