Assay Detail
Binding
CHEMBL647045
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Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells
14
Total Activities
14
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
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.51 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3392247 | — | — | 1 | 9.40 |
| CHEMBL279436 | — | — | 1 | 8.89 |
| CHEMBL5483012 | — | — | 1 | 8.89 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 8.74 |
| CHEMBL284103 | — | — | 1 | 8.51 |
| CHEMBL3392246 | — | — | 1 | 8.48 |
| CHEMBL114166 | — | — | 1 | 7.48 |
| CHEMBL25467 | — | — | 1 | 7.44 |
| CHEMBL123448 | — | — | 1 | 7.24 |
| CHEMBL31410 | CORYNANTHEINE | — | 1 | 6.85 |
| CHEMBL123349 | — | — | 1 | 6.35 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 5.98 |
| CHEMBL123138 | — | — | 1 | 5.48 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3392247 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL279436 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL5483012 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL284103 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3392246 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL114166 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL25467 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL123448 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL31410 | CORYNANTHEINE | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL123349 | — | Ki | = | 449.0 | nM | 6.35 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 1057.0 | nM | 5.98 |
| CHEMBL123138 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL10347 | RAUWOLSCINE | Ki | = | 4400.0 | nM | 5.36 |