Assay Detail
Functional
CHEMBL646231
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonistic activity against alpha-1B receptor in rat spleen.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Spleen |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 8.32 | 9.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | 4.0 | 1 | 9.69 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 1 | 9.51 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.60 |
| CHEMBL709 | ALFUZOSIN | 4.0 | 1 | 8.31 |
| CHEMBL293695 | — | — | 1 | 8.15 |
| CHEMBL62033 | — | — | 1 | 7.73 |
| CHEMBL291303 | — | — | 1 | 7.52 |
| CHEMBL445325 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | Kd | = | 0.2042 | nM | 9.69 |
| CHEMBL707 | DOXAZOSIN | Kd | = | 0.309 | nM | 9.51 |
| CHEMBL611 | TERAZOSIN | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL709 | ALFUZOSIN | Kd | = | 4.898 | nM | 8.31 |
| CHEMBL293695 | — | Kd | = | 7.079 | nM | 8.15 |
| CHEMBL62033 | — | Kd | = | 18.62 | nM | 7.73 |
| CHEMBL291303 | — | Kd | = | 30.2 | nM | 7.52 |
| CHEMBL445325 | — | Kd | = | 85.11 | nM | 7.07 |