Assay Detail
Binding
CHEMBL2389181
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Displacement of [3H]WIN35428 from human DAT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.36 | 6.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386163 | — | — | 2 | 6.45 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 6.32 |
| CHEMBL259209 | MILNACIPRAN | 4.0 | 1 | - |
| CHEMBL1118 | DESVENLAFAXINE | 4.0 | 1 | - |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | - |
| CHEMBL2386166 | — | — | 1 | - |
| CHEMBL2386165 | — | — | 1 | - |
| CHEMBL2386164 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386163 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL1175 | DULOXETINE | Ki | = | 484.0 | nM | 6.32 |
| CHEMBL2386163 | — | Ki | = | 475.0 | nM | 6.32 |
| CHEMBL259209 | MILNACIPRAN | Ki | > | 854.0 | nM | - |
| CHEMBL1118 | DESVENLAFAXINE | Ki | > | 854.0 | nM | - |
| CHEMBL637 | VENLAFAXINE | Ki | > | 890.0 | nM | - |
| CHEMBL2386166 | — | Ki | > | 890.0 | nM | - |
| CHEMBL2386165 | — | Ki | > | 890.0 | nM | - |
| CHEMBL2386164 | — | Ki | > | 890.0 | nM | - |