Assay Detail
Binding
CHEMBL642293
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Binding affinity against native Alpha-2 adrenergic receptor from rat cerebral cortex using radioligand ([3H]rauwolscine) binding assay
6
Total Activities
6
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
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.23 | 6.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 6.87 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 6.83 |
| CHEMBL97698 | — | — | 1 | 6.17 |
| CHEMBL342062 | — | — | 1 | 6.13 |
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 5.86 |
| CHEMBL140450 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL2 | PRAZOSIN | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL97698 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL342062 | — | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL423294 | CYCLAZOSIN | Ki | = | 1380.38 | nM | 5.86 |
| CHEMBL140450 | — | Ki | = | 2884.03 | nM | 5.54 |