Assay Detail
Binding
CHEMBL646864
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Alpha-1-adrenolytic activity was assessed from the ability to inhibit [3H]prazosin binding to rat cerebral cortex preparation
16
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.19 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.22 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 8.00 |
| CHEMBL284056 | — | — | 1 | 7.39 |
| CHEMBL30911 | — | — | 1 | 6.52 |
| CHEMBL542812 | — | — | 1 | 6.42 |
| CHEMBL554455 | — | — | 1 | 6.30 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 6.00 |
| CHEMBL553942 | — | — | 1 | 6.00 |
| CHEMBL3350238 | — | — | 3 | 5.72 |
| CHEMBL2093965 | — | — | 1 | 5.70 |
| CHEMBL540511 | — | — | 1 | 5.46 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 5.44 |
| CHEMBL542814 | — | — | 1 | 5.41 |
| CHEMBL554235 | — | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL597 | PHENTOLAMINE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL284056 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL30911 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL542812 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL554455 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL15245 | YOHIMBINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL553942 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3350238 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2093965 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3350238 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3350238 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL540511 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1484 | NICARDIPINE | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL542814 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL554235 | — | IC50 | = | 75000.0 | nM | 4.12 |