Assay Detail
Binding
CHEMBL641155
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Binding affinity at native Alpha-2 adrenergic receptor in rat cerebral cortex by [3H]rauwolscine displacement.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.75 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341665 | — | — | 1 | 7.72 |
| CHEMBL27013 | — | — | 1 | 7.00 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 6.80 |
| CHEMBL29591 | — | — | 1 | 6.23 |
| CHEMBL13647 | BMY-7378 | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341665 | — | Ki | = | 19.05 | nM | 7.72 |
| CHEMBL27013 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2 | PRAZOSIN | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL29591 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL13647 | BMY-7378 | Ki | = | 1047.13 | nM | 5.98 |