Assay Detail
Binding
CHEMBL647467
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Alpha-1-adrenolytic activity was assessed in vitro from the ability to inhibit clonidine binding to rat aorta preparation
16
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Aorta |
| 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 | 13 | 4.62 | 5.00 |
| Kd | 3 | 8.49 | 10.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 10.99 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 8.01 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 6.46 |
| CHEMBL3350238 | — | — | 3 | 5.00 |
| CHEMBL284056 | — | — | 1 | 5.00 |
| CHEMBL554455 | — | — | 1 | 4.40 |
| CHEMBL542812 | — | — | 1 | 4.16 |
| CHEMBL553942 | — | — | 1 | - |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | - |
| CHEMBL554235 | — | — | 1 | - |
| CHEMBL2093965 | — | — | 1 | - |
| CHEMBL540511 | — | — | 1 | - |
| CHEMBL30911 | — | — | 1 | - |
| CHEMBL542814 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Kd | = | 0.01023 | nM | 10.99 |
| CHEMBL597 | PHENTOLAMINE | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL15245 | YOHIMBINE | Kd | = | 346.74 | nM | 6.46 |
| CHEMBL3350238 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL284056 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3350238 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL554455 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL542812 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL553942 | — | IC50 | >> | 100000.0 | nM | - |
| CHEMBL1484 | NICARDIPINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL554235 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2093965 | — | IC50 | >> | 10000.0 | nM | - |
| CHEMBL540511 | — | IC50 | >> | 30000.0 | nM | - |
| CHEMBL30911 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3350238 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL542814 | — | IC50 | >> | 30000.0 | nM | - |