Assay Detail
Binding
CHEMBL4139219
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Displacement of [3H]prazosin from human alpha1B 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 | 7.96 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4161165 | — | — | 1 | 9.55 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.39 |
| CHEMBL4163587 | — | — | 1 | 9.28 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 1 | 9.20 |
| CHEMBL4160032 | — | — | 1 | 8.13 |
| CHEMBL4171491 | — | — | 1 | 7.60 |
| CHEMBL4171710 | — | — | 1 | 7.37 |
| CHEMBL4159468 | — | — | 1 | 7.33 |
| CHEMBL4163810 | — | — | 1 | 7.26 |
| CHEMBL4170675 | — | — | 1 | 7.20 |
| CHEMBL4174168 | — | — | 1 | 6.75 |
| CHEMBL4167693 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4161165 | — | Ki | = | 0.2818 | nM | 9.55 |
| CHEMBL2 | PRAZOSIN | Ki | = | 0.4074 | nM | 9.39 |
| CHEMBL4163587 | — | Ki | = | 0.5248 | nM | 9.28 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL4160032 | — | Ki | = | 7.413 | nM | 8.13 |
| CHEMBL4171491 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL4171710 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL4159468 | — | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL4163810 | — | Ki | = | 54.95 | nM | 7.26 |
| CHEMBL4170675 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4174168 | — | Ki | = | 177.83 | nM | 6.75 |
| CHEMBL4167693 | — | Ki | = | 316.23 | nM | 6.50 |