Assay Detail
Binding
CHEMBL3776804
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-NE reuptake in human NET transfected into HEK293 cells by liquid scintillation counting method
12
Total Activities
12
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
Design, synthesis, and biological evaluation of arylpiperazine-benzylpiperidines with dual serotonin and norepinephrine reuptake inhibitory activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.03 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774957 | — | — | 1 | 6.42 |
| CHEMBL3774556 | — | — | 1 | 6.28 |
| CHEMBL3775140 | — | — | 1 | 6.25 |
| CHEMBL3775177 | — | — | 1 | 6.22 |
| CHEMBL3775012 | — | — | 1 | 6.21 |
| CHEMBL3775703 | — | — | 1 | 6.12 |
| CHEMBL3774732 | — | — | 1 | 6.05 |
| CHEMBL3775405 | — | — | 1 | 5.97 |
| CHEMBL3774516 | — | — | 1 | 5.93 |
| CHEMBL3775085 | — | — | 1 | 5.68 |
| CHEMBL3775008 | — | — | 1 | 5.60 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774957 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3774556 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3775140 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3775177 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3775012 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3775703 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3774732 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL3775405 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL3774516 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL3775085 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3775008 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 2550.0 | nM | 5.59 |