Assay Detail
Binding
CHEMBL652819
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand
34
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 | 34 | 9.09 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL304591 | — | — | 1 | 9.96 |
| CHEMBL836 | TAMSULOSIN | 4.0 | 2 | 9.89 |
| CHEMBL304132 | — | — | 1 | 9.80 |
| CHEMBL69264 | — | — | 1 | 9.74 |
| CHEMBL70892 | — | — | 1 | 9.70 |
| CHEMBL68203 | — | — | 1 | 9.64 |
| CHEMBL431362 | — | — | 1 | 9.54 |
| CHEMBL309106 | — | — | 2 | 9.48 |
| CHEMBL67552 | — | — | 1 | 9.39 |
| CHEMBL304977 | — | — | 1 | 9.34 |
| CHEMBL69295 | — | — | 1 | 9.18 |
| CHEMBL71580 | — | — | 1 | 9.12 |
| CHEMBL302940 | — | — | 1 | 9.11 |
| CHEMBL67648 | — | — | 1 | 9.10 |
| CHEMBL68604 | — | — | 1 | 9.06 |
| CHEMBL303248 | — | — | 1 | 9.05 |
| CHEMBL69143 | — | — | 1 | 9.05 |
| CHEMBL68601 | — | — | 1 | 9.02 |
| CHEMBL70095 | — | — | 1 | 9.01 |
| CHEMBL303627 | — | — | 1 | 8.99 |
| CHEMBL302092 | — | — | 1 | 8.92 |
| CHEMBL68913 | — | — | 1 | 8.91 |
| CHEMBL68565 | — | — | 1 | 8.83 |
| CHEMBL302246 | — | — | 1 | 8.82 |
| CHEMBL308671 | — | — | 1 | 8.82 |
| CHEMBL68746 | — | — | 1 | 8.74 |
| CHEMBL302942 | — | — | 1 | 8.68 |
| CHEMBL68699 | — | — | 1 | 8.52 |
| CHEMBL419624 | — | — | 1 | 8.37 |
| CHEMBL69245 | — | — | 1 | 8.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL304591 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL836 | TAMSULOSIN | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL836 | TAMSULOSIN | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL304132 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL69264 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL70892 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL68203 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL431362 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL309106 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL309106 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL67552 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL304977 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL69295 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL71580 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL302940 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL67648 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL68604 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL303248 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL69143 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL68601 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL70095 | — | Ki | = | 0.98 | nM | 9.01 |
| CHEMBL303627 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL302092 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL68913 | — | Ki | = | 1.22 | nM | 8.91 |
| CHEMBL68565 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL302246 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL308671 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL68746 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL302942 | — | Ki | = | 2.09 | nM | 8.68 |
| CHEMBL68699 | — | Ki | = | 3.05 | nM | 8.52 |
| CHEMBL419624 | — | Ki | = | 4.25 | nM | 8.37 |
| CHEMBL69245 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL71473 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL68045 | — | Ki | = | 22.0 | nM | 7.66 |