Assay Detail
Binding
CHEMBL2389182
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Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
14
Total Activities
9
Compounds Tested
2
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 noradrenaline transporter (CHEMBL222) ↗| 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 | 7.66 | 8.92 |
| IC50 | 5 | 7.02 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386163 | — | — | 2 | 8.92 |
| CHEMBL1175 | DULOXETINE | 4.0 | 2 | 8.17 |
| CHEMBL2386162 | — | — | 1 | 8.16 |
| CHEMBL2386164 | — | — | 1 | 7.52 |
| CHEMBL259209 | MILNACIPRAN | 4.0 | 2 | 7.39 |
| CHEMBL2386166 | — | — | 1 | 6.75 |
| CHEMBL2386165 | — | — | 1 | 6.36 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 2 | 6.17 |
| CHEMBL1118 | DESVENLAFAXINE | 4.0 | 2 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386163 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2386163 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1175 | DULOXETINE | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL2386162 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2386164 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL259209 | MILNACIPRAN | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL259209 | MILNACIPRAN | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL2386166 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL2386165 | — | Ki | = | 438.0 | nM | 6.36 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL1118 | DESVENLAFAXINE | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1118 | DESVENLAFAXINE | Ki | > | 650.0 | nM | - |
| CHEMBL637 | VENLAFAXINE | Ki | > | 553.0 | nM | - |