Assay Detail
Binding
CHEMBL3776803
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-5-HT reuptake in human SERT 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 serotonin transporter (CHEMBL228) ↗| 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 | 5.75 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 6.70 |
| CHEMBL3774957 | — | — | 1 | 5.93 |
| CHEMBL3775177 | — | — | 1 | 5.87 |
| CHEMBL3775703 | — | — | 1 | 5.84 |
| CHEMBL3774732 | — | — | 1 | 5.75 |
| CHEMBL3775405 | — | — | 1 | 5.70 |
| CHEMBL3774556 | — | — | 1 | 5.69 |
| CHEMBL3775012 | — | — | 1 | 5.65 |
| CHEMBL3775140 | — | — | 1 | 5.60 |
| CHEMBL3774516 | — | — | 1 | 5.58 |
| CHEMBL3775008 | — | — | 1 | 5.37 |
| CHEMBL3775085 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3774957 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL3775177 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL3775703 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL3774732 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL3775405 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3774556 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL3775012 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL3775140 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL3774516 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL3775008 | — | IC50 | = | 4320.0 | nM | 5.37 |
| CHEMBL3775085 | — | IC50 | = | 4920.0 | nM | 5.31 |