Assay Detail
Binding
CHEMBL648995
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards cloned human alpha-1B adrenergic receptor was determined using [125]-HEAT as radioligand
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.50 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | 4.0 | 1 | 8.72 |
| CHEMBL70892 | — | — | 1 | 6.59 |
| CHEMBL304591 | — | — | 1 | 6.44 |
| CHEMBL69264 | — | — | 1 | 6.33 |
| CHEMBL67552 | — | — | 1 | 6.32 |
| CHEMBL68601 | — | — | 1 | 6.22 |
| CHEMBL71580 | — | — | 1 | 6.22 |
| CHEMBL302092 | — | — | 1 | 5.91 |
| CHEMBL68565 | — | — | 1 | 5.79 |
| CHEMBL69143 | — | — | 1 | - |
| CHEMBL304132 | — | — | 1 | - |
| CHEMBL68746 | — | — | 1 | - |
| CHEMBL303627 | — | — | 1 | - |
| CHEMBL68604 | — | — | 1 | - |
| CHEMBL302246 | — | — | 1 | - |
| CHEMBL68203 | — | — | 1 | - |
| CHEMBL308671 | — | — | 1 | - |
| CHEMBL419624 | — | — | 1 | - |
| CHEMBL71473 | — | — | 1 | - |
| CHEMBL67648 | — | — | 1 | - |
| CHEMBL69245 | — | — | 1 | - |
| CHEMBL68699 | — | — | 1 | - |
| CHEMBL68913 | — | — | 1 | - |
| CHEMBL68045 | — | — | 1 | - |
| CHEMBL309106 | — | — | 1 | - |
| CHEMBL302942 | — | — | 1 | - |
| CHEMBL70095 | — | — | 1 | - |
| CHEMBL431362 | — | — | 1 | - |
| CHEMBL69295 | — | — | 1 | - |
| CHEMBL304977 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | Ki | = | 1.92 | nM | 8.72 |
| CHEMBL70892 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL304591 | — | Ki | = | 361.0 | nM | 6.44 |
| CHEMBL69264 | — | Ki | = | 465.0 | nM | 6.33 |
| CHEMBL67552 | — | Ki | = | 482.0 | nM | 6.32 |
| CHEMBL68601 | — | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL71580 | — | Ki | = | 605.0 | nM | 6.22 |
| CHEMBL302092 | — | Ki | = | 1225.0 | nM | 5.91 |
| CHEMBL68565 | — | Ki | = | 1639.0 | nM | 5.79 |
| CHEMBL304132 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL303248 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL68746 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL303627 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL68604 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL302246 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL68203 | — | Ki | > | 1750.0 | nM | - |
| CHEMBL308671 | — | Ki | > | 1658.0 | nM | - |
| CHEMBL419624 | — | Ki | > | 20000.0 | nM | - |
| CHEMBL71473 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL302940 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL69143 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL67648 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL69245 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL68699 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL68913 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL68045 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL309106 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL302942 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL70095 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL431362 | — | Ki | > | 1650.0 | nM | - |
| CHEMBL69295 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL304977 | — | Ki | > | 2000.0 | nM | - |