Assay Detail
Binding
CHEMBL891167
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Displacement of [3H]prazosin from human adrenergic alpha-1b 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 | 9.11 | 9.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 9.87 |
| CHEMBL242724 | — | — | 1 | 9.62 |
| CHEMBL388884 | — | — | 1 | 9.51 |
| CHEMBL242934 | — | — | 1 | 9.31 |
| CHEMBL242508 | — | — | 1 | 9.06 |
| CHEMBL242507 | — | — | 1 | 9.06 |
| CHEMBL242723 | — | — | 1 | 8.86 |
| CHEMBL389978 | — | — | 1 | 8.50 |
| CHEMBL242725 | — | — | 1 | 8.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423294 | CYCLAZOSIN | Ki | = | 0.1349 | nM | 9.87 |
| CHEMBL242724 | — | Ki | = | 0.2399 | nM | 9.62 |
| CHEMBL388884 | — | Ki | = | 0.309 | nM | 9.51 |
| CHEMBL242934 | — | Ki | = | 0.4898 | nM | 9.31 |
| CHEMBL242508 | — | Ki | = | 0.871 | nM | 9.06 |
| CHEMBL242507 | — | Ki | = | 0.871 | nM | 9.06 |
| CHEMBL242723 | — | Ki | = | 1.38 | nM | 8.86 |
| CHEMBL389978 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL242725 | — | Ki | = | 5.888 | nM | 8.23 |