Assay Detail
Binding
CHEMBL891166
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Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.91 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388884 | — | — | 1 | 8.46 |
| CHEMBL242934 | — | — | 1 | 8.38 |
| CHEMBL242724 | — | — | 1 | 8.37 |
| CHEMBL389978 | — | — | 1 | 7.98 |
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 7.91 |
| CHEMBL242507 | — | — | 1 | 7.63 |
| CHEMBL242723 | — | — | 1 | 7.59 |
| CHEMBL242508 | — | — | 1 | 7.56 |
| CHEMBL242725 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388884 | — | Ki | = | 3.467 | nM | 8.46 |
| CHEMBL242934 | — | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL242724 | — | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL389978 | — | Ki | = | 10.47 | nM | 7.98 |
| CHEMBL423294 | CYCLAZOSIN | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL242507 | — | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL242723 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL242508 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL242725 | — | Ki | = | 48.98 | nM | 7.31 |