Assay Detail
Binding
CHEMBL839628
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Inhibition of [3H]-nisoxetine binding to Norepinephrine transporter from rat cortex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 6.77 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL92860 | — | — | 1 | 7.48 |
| CHEMBL91157 | — | — | 1 | 6.75 |
| CHEMBL419316 | — | — | 1 | 6.66 |
| CHEMBL328114 | — | — | 1 | 6.51 |
| CHEMBL90997 | — | — | 1 | 6.44 |
| CHEMBL268258 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL92860 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL91157 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL419316 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL328114 | — | Ki | = | 312.0 | nM | 6.51 |
| CHEMBL90997 | — | Ki | = | 365.0 | nM | 6.44 |
| CHEMBL268258 | — | Ki | > | 1000.0 | nM | - |