Assay Detail
Binding
CHEMBL4007285
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method
32
Total Activities
32
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 in vitro activity of 1,4-disubstituted piperazines and piperidines as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 5.90 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4083724 | — | — | 1 | 7.00 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.96 |
| CHEMBL4082767 | — | — | 1 | 6.50 |
| CHEMBL4103183 | — | — | 1 | 6.49 |
| CHEMBL4081753 | — | — | 1 | 6.48 |
| CHEMBL4099773 | — | — | 1 | 6.40 |
| CHEMBL4073939 | — | — | 1 | 6.29 |
| CHEMBL4074999 | — | — | 1 | 6.28 |
| CHEMBL4063684 | — | — | 1 | 6.25 |
| CHEMBL4082902 | — | — | 1 | 6.22 |
| CHEMBL4064805 | — | — | 1 | 5.90 |
| CHEMBL4101780 | — | — | 1 | 5.88 |
| CHEMBL4086279 | — | — | 1 | 5.88 |
| CHEMBL4060900 | — | — | 1 | 5.88 |
| CHEMBL4091502 | — | — | 1 | 5.83 |
| CHEMBL4100713 | — | — | 1 | 5.82 |
| CHEMBL4091567 | — | — | 1 | 5.80 |
| CHEMBL4105112 | — | — | 1 | 5.79 |
| CHEMBL3613151 | — | — | 1 | 5.78 |
| CHEMBL4092998 | — | — | 1 | 5.77 |
| CHEMBL4101722 | — | — | 1 | 5.75 |
| CHEMBL3612830 | — | — | 1 | 5.70 |
| CHEMBL288826 | — | — | 1 | 5.66 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 5.59 |
| CHEMBL4085259 | — | — | 1 | 5.55 |
| CHEMBL4063764 | — | — | 1 | 5.52 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.49 |
| CHEMBL4083782 | — | — | 1 | 5.43 |
| CHEMBL4095430 | — | — | 1 | 5.38 |
| CHEMBL4094047 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4083724 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4082767 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL4103183 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL4081753 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL4099773 | — | IC50 | = | 399.5 | nM | 6.40 |
| CHEMBL4073939 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL4074999 | — | IC50 | = | 521.0 | nM | 6.28 |
| CHEMBL4063684 | — | IC50 | = | 568.9 | nM | 6.25 |
| CHEMBL4082902 | — | IC50 | = | 602.8 | nM | 6.22 |
| CHEMBL4064805 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL4101780 | — | IC50 | = | 1323.0 | nM | 5.88 |
| CHEMBL4086279 | — | IC50 | = | 1313.0 | nM | 5.88 |
| CHEMBL4060900 | — | IC50 | = | 1327.0 | nM | 5.88 |
| CHEMBL4091502 | — | IC50 | = | 1467.0 | nM | 5.83 |
| CHEMBL4100713 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4091567 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL4105112 | — | IC50 | = | 1621.0 | nM | 5.79 |
| CHEMBL3613151 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL4092998 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL4101722 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL3612830 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL288826 | — | IC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL4085259 | — | IC50 | = | 2830.0 | nM | 5.55 |
| CHEMBL4063764 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL894 | BUPROPION | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL4083782 | — | IC50 | = | 3750.0 | nM | 5.43 |
| CHEMBL4095430 | — | IC50 | = | 4218.0 | nM | 5.38 |
| CHEMBL4094047 | — | IC50 | = | 5328.0 | nM | 5.27 |
| CHEMBL4073400 | — | IC50 | = | 5862.0 | nM | 5.23 |
| CHEMBL3613152 | — | IC50 | = | 8030.0 | nM | 5.09 |