Assay Detail
Binding
CHEMBL857770
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Hippocampus |
| Confidence | 8 — Homologous single protein target |
| 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 | 7.93 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.03 |
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 8.77 |
| CHEMBL97698 | — | — | 1 | 8.41 |
| CHEMBL342062 | — | — | 1 | 7.73 |
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 7.42 |
| CHEMBL140450 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.9333 | nM | 9.03 |
| CHEMBL423294 | CYCLAZOSIN | Ki | = | 1.698 | nM | 8.77 |
| CHEMBL97698 | — | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL342062 | — | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL267930 | SPIPERONE | Ki | = | 38.02 | nM | 7.42 |
| CHEMBL140450 | — | Ki | = | 645.65 | nM | 6.19 |