Assay Detail
Binding
CHEMBL646099
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards cloned human alpha-1D 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 | 7.28 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | 4.0 | 1 | 9.74 |
| CHEMBL70892 | — | — | 1 | 8.00 |
| CHEMBL69264 | — | — | 1 | 7.82 |
| CHEMBL304591 | — | — | 1 | 7.80 |
| CHEMBL67552 | — | — | 1 | 7.66 |
| CHEMBL68604 | — | — | 1 | 7.55 |
| CHEMBL304132 | — | — | 1 | 7.43 |
| CHEMBL68746 | — | — | 1 | 7.42 |
| CHEMBL67648 | — | — | 1 | 7.40 |
| CHEMBL71580 | — | — | 1 | 7.39 |
| CHEMBL302092 | — | — | 1 | 7.29 |
| CHEMBL302940 | — | — | 1 | 7.29 |
| CHEMBL309106 | — | — | 1 | 7.28 |
| CHEMBL302942 | — | — | 1 | 7.28 |
| CHEMBL431362 | — | — | 1 | 7.27 |
| CHEMBL68601 | — | — | 1 | 7.26 |
| CHEMBL70095 | — | — | 1 | 7.25 |
| CHEMBL69295 | — | — | 1 | 7.21 |
| CHEMBL71473 | — | — | 1 | 7.20 |
| CHEMBL69143 | — | — | 1 | 7.19 |
| CHEMBL68565 | — | — | 1 | 7.14 |
| CHEMBL303248 | — | — | 1 | 7.14 |
| CHEMBL302246 | — | — | 1 | 7.12 |
| CHEMBL68699 | — | — | 1 | 7.12 |
| CHEMBL308671 | — | — | 1 | 6.96 |
| CHEMBL68203 | — | — | 1 | 6.91 |
| CHEMBL304977 | — | — | 1 | 6.86 |
| CHEMBL419624 | — | — | 1 | 6.86 |
| CHEMBL68913 | — | — | 1 | 6.82 |
| CHEMBL303627 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL836 | TAMSULOSIN | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL70892 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL69264 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL304591 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL67552 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL68604 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL304132 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL68746 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL67648 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL71580 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL302092 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL302940 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL309106 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL302942 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL431362 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL68601 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL70095 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL69295 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL71473 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL69143 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL68565 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL303248 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL302246 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL68699 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL308671 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL68203 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL304977 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL419624 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL68913 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL303627 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL69245 | — | Ki | = | 407.0 | nM | 6.39 |
| CHEMBL68045 | — | Ki | = | 540.0 | nM | 6.27 |