Assay Detail
Binding
CHEMBL4123784
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Displacement of [3H]prazosin from human alpha1D adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| Ki | 12 | 8.96 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4128084 | — | — | 1 | 10.40 |
| CHEMBL342062 | — | — | 1 | 10.22 |
| CHEMBL4126860 | — | — | 1 | 10.20 |
| CHEMBL4129461 | — | — | 1 | 9.82 |
| CHEMBL4129291 | — | — | 1 | 9.41 |
| CHEMBL4125846 | — | — | 1 | 8.65 |
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 8.49 |
| CHEMBL4127078 | — | — | 1 | 8.43 |
| CHEMBL4125981 | — | — | 1 | 8.40 |
| CHEMBL4127483 | — | — | 1 | 8.29 |
| CHEMBL4128460 | — | — | 1 | 8.21 |
| CHEMBL4128311 | — | — | 1 | 6.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4128084 | — | Ki | = | 0.03981 | nM | 10.40 |
| CHEMBL342062 | — | Ki | = | 0.06026 | nM | 10.22 |
| CHEMBL4126860 | — | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL4129461 | — | Ki | = | 0.1514 | nM | 9.82 |
| CHEMBL4129291 | — | Ki | = | 0.389 | nM | 9.41 |
| CHEMBL4125846 | — | Ki | = | 2.239 | nM | 8.65 |
| CHEMBL423294 | CYCLAZOSIN | Ki | = | 3.236 | nM | 8.49 |
| CHEMBL4127078 | — | Ki | = | 3.715 | nM | 8.43 |
| CHEMBL4125981 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL4127483 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL4128460 | — | Ki | = | 6.166 | nM | 8.21 |
| CHEMBL4128311 | — | Ki | = | 104.71 | nM | 6.98 |