Assay Detail
Binding
CHEMBL646115
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace [3H]rauwolscine from cloned human Alpha-2B 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 | 6.57 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 7.89 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 7.58 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.38 |
| CHEMBL290860 | — | — | 1 | 6.24 |
| CHEMBL2051956 | DEXNIGULDIPINE | 2.0 | 1 | 6.18 |
| CHEMBL179334 | — | — | 1 | 6.11 |
| CHEMBL5483012 | — | — | 2 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL611 | TERAZOSIN | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL290860 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL2051956 | DEXNIGULDIPINE | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL179334 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL5483012 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL5483012 | — | Ki | = | 860.0 | nM | 6.07 |