Assay Detail
Binding
CHEMBL3363899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
18
Total Activities
18
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 noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.12 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3310482 | — | — | 1 | 7.97 |
| CHEMBL3310485 | — | — | 1 | 7.84 |
| CHEMBL3310489 | — | — | 1 | 7.83 |
| CHEMBL3310484 | — | — | 1 | 7.80 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 7.70 |
| CHEMBL3310483 | — | — | 1 | 7.52 |
| CHEMBL3310487 | — | — | 1 | 7.51 |
| CHEMBL3310486 | — | — | 1 | 7.49 |
| CHEMBL3310490 | — | — | 1 | 7.48 |
| CHEMBL3309701 | — | — | 1 | 7.47 |
| CHEMBL3310478 | — | — | 1 | 7.47 |
| CHEMBL3309702 | — | — | 1 | 7.43 |
| CHEMBL3310488 | — | — | 1 | 7.16 |
| CHEMBL592374 | AMITIFADINE | 2.0 | 1 | 6.84 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 6.29 |
| CHEMBL543876 | — | — | 1 | 5.84 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.36 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3310482 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL3310485 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL3310489 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL3310484 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL295467 | NISOXETINE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3310483 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3310487 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL3310486 | — | IC50 | = | 32.5 | nM | 7.49 |
| CHEMBL3310490 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL3309701 | — | IC50 | = | 33.5 | nM | 7.47 |
| CHEMBL3310478 | — | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL3309702 | — | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL3310488 | — | IC50 | = | 68.6 | nM | 7.16 |
| CHEMBL592374 | AMITIFADINE | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL543876 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 4410.0 | nM | 5.36 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 5722.0 | nM | 5.24 |