Assay Detail
Binding
CHEMBL644759
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Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2B adrenergic receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous 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 | 16 | 7.14 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25467 | — | — | 1 | 8.47 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 8.34 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 8.33 |
| CHEMBL123138 | — | — | 1 | 7.85 |
| CHEMBL3559672 | RAUWOLFIA SERPENTINA | 4.0 | 1 | 7.84 |
| CHEMBL123448 | — | — | 1 | 7.82 |
| CHEMBL123349 | — | — | 1 | 7.80 |
| CHEMBL122404 | AKUAMMIGINE | — | 1 | 6.94 |
| CHEMBL114166 | — | — | 1 | 6.85 |
| CHEMBL279436 | — | — | 1 | 6.56 |
| CHEMBL31410 | CORYNANTHEINE | — | 1 | 6.34 |
| CHEMBL3392246 | — | — | 1 | 6.12 |
| CHEMBL284103 | — | — | 1 | 6.04 |
| CHEMBL5483012 | — | — | 1 | 5.93 |
| CHEMBL3392247 | — | — | 1 | 5.91 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25467 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL10347 | RAUWOLSCINE | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL123138 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3559672 | RAUWOLFIA SERPENTINA | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL123448 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL123349 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL122404 | AKUAMMIGINE | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL114166 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL279436 | — | Ki | = | 275.0 | nM | 6.56 |
| CHEMBL31410 | CORYNANTHEINE | Ki | = | 455.0 | nM | 6.34 |
| CHEMBL3392246 | — | Ki | = | 758.0 | nM | 6.12 |
| CHEMBL284103 | — | Ki | = | 912.0 | nM | 6.04 |
| CHEMBL5483012 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL3392247 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL405355 | NIGULDIPINE | Ki | > | 5000.0 | nM | - |