Assay Detail
Binding
CHEMBL4139220
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]prazosin from human alpha1D adrenoceptor expressed in CHO cell membranes after 30 mins
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
Quinazoline based α1-adrenoreceptor antagonists with potent antiproliferative activity in human prostate cancer cell lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.04 | 9.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.65 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 1 | 9.49 |
| CHEMBL4161165 | — | — | 1 | 9.48 |
| CHEMBL4163587 | — | — | 1 | 8.67 |
| CHEMBL4160032 | — | — | 1 | 7.88 |
| CHEMBL4163810 | — | — | 1 | 7.55 |
| CHEMBL4171491 | — | — | 1 | 7.47 |
| CHEMBL4171710 | — | — | 1 | 7.43 |
| CHEMBL4170675 | — | — | 1 | 7.31 |
| CHEMBL4174168 | — | — | 1 | 6.99 |
| CHEMBL4159468 | — | — | 1 | 6.53 |
| CHEMBL4167693 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.2239 | nM | 9.65 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 0.3236 | nM | 9.49 |
| CHEMBL4161165 | — | Ki | = | 0.3311 | nM | 9.48 |
| CHEMBL4163587 | — | Ki | = | 2.138 | nM | 8.67 |
| CHEMBL4160032 | — | Ki | = | 13.18 | nM | 7.88 |
| CHEMBL4163810 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL4171491 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL4171710 | — | Ki | = | 37.15 | nM | 7.43 |
| CHEMBL4170675 | — | Ki | = | 48.98 | nM | 7.31 |
| CHEMBL4174168 | — | Ki | = | 102.33 | nM | 6.99 |
| CHEMBL4159468 | — | Ki | = | 295.12 | nM | 6.53 |
| CHEMBL4167693 | — | Ki | > | 1000.0 | nM | - |