Assay Detail
Binding
CHEMBL4139218
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Displacement of [3H]prazosin from human alpha1A 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 | 7.95 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.23 |
| CHEMBL4161165 | — | — | 1 | 9.20 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 1 | 9.11 |
| CHEMBL4163587 | — | — | 1 | 8.15 |
| CHEMBL4170675 | — | — | 1 | 7.74 |
| CHEMBL4160032 | — | — | 1 | 7.48 |
| CHEMBL4171710 | — | — | 1 | 6.96 |
| CHEMBL4171491 | — | — | 1 | 6.92 |
| CHEMBL4163810 | — | — | 1 | 6.72 |
| CHEMBL4167693 | — | — | 1 | - |
| CHEMBL4159468 | — | — | 1 | - |
| CHEMBL4174168 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.5888 | nM | 9.23 |
| CHEMBL4161165 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 0.7762 | nM | 9.11 |
| CHEMBL4163587 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL4170675 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL4160032 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL4171710 | — | Ki | = | 109.65 | nM | 6.96 |
| CHEMBL4171491 | — | Ki | = | 120.23 | nM | 6.92 |
| CHEMBL4163810 | — | Ki | = | 190.55 | nM | 6.72 |
| CHEMBL4167693 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4159468 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4174168 | — | Ki | > | 1000.0 | nM | - |