Assay Detail
Binding
CHEMBL648109
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace [3H]prazosin from cloned human Alpha-1B adrenergic receptor
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.49 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.68 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 8.59 |
| CHEMBL290860 | — | — | 1 | 7.30 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 7.26 |
| CHEMBL2051956 | DEXNIGULDIPINE | 2.0 | 1 | 7.25 |
| CHEMBL179334 | — | — | 1 | 6.75 |
| CHEMBL5483012 | — | — | 2 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL611 | TERAZOSIN | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL290860 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2051956 | DEXNIGULDIPINE | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL179334 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL5483012 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL5483012 | — | Ki | = | 410.0 | nM | 6.39 |