Assay Detail
Binding
CHEMBL838762
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Inhibition of [3H]- rauwolscine binding to alpha-2C adrenergic receptor
6
Total Activities
6
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
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 9.08 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL91157 | — | — | 1 | 10.00 |
| CHEMBL419316 | — | — | 1 | 9.70 |
| CHEMBL328114 | — | — | 1 | 9.30 |
| CHEMBL92860 | — | — | 1 | 9.10 |
| CHEMBL268258 | — | — | 1 | 8.68 |
| CHEMBL90997 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL91157 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL419316 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL328114 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL92860 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL268258 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL90997 | — | Ki | = | 19.0 | nM | 7.72 |