Assay Detail
Binding
CHEMBL647049
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Displacement of [125I]HEAT from human Alpha-1A adrenergic receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.22 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310768 | — | — | 1 | 9.05 |
| CHEMBL309969 | — | — | 1 | 8.96 |
| CHEMBL310890 | — | — | 1 | 8.92 |
| CHEMBL81093 | — | — | 1 | 8.08 |
| CHEMBL81661 | — | — | 1 | 7.82 |
| CHEMBL80109 | — | — | 1 | 7.55 |
| CHEMBL80036 | — | — | 1 | 7.09 |
| CHEMBL79817 | — | — | 1 | 7.07 |
| CHEMBL79990 | — | — | 1 | 6.53 |
| CHEMBL79940 | — | — | 1 | 5.89 |
| CHEMBL80125 | — | — | 1 | 5.82 |
| CHEMBL82480 | — | — | 1 | 5.63 |
| CHEMBL83791 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310768 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL309969 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL310890 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL81093 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL81661 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL80109 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL80036 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL79817 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL79990 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL79940 | — | Ki | = | 1298.0 | nM | 5.89 |
| CHEMBL80125 | — | Ki | = | 1502.0 | nM | 5.82 |
| CHEMBL82480 | — | Ki | = | 2321.0 | nM | 5.63 |
| CHEMBL83791 | — | Ki | = | 3466.0 | nM | 5.46 |