Assay Detail
Binding
CHEMBL4007286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by microbeta liquid scintillation counting method
31
Total Activities
31
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 dopamine transporter (CHEMBL238) ↗| 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 | 31 | 5.98 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.37 |
| CHEMBL4073939 | — | — | 1 | 7.03 |
| CHEMBL4083724 | — | — | 1 | 7.01 |
| CHEMBL3613151 | — | — | 1 | 6.72 |
| CHEMBL4074999 | — | — | 1 | 6.53 |
| CHEMBL4092998 | — | — | 1 | 6.51 |
| CHEMBL4103183 | — | — | 1 | 6.50 |
| CHEMBL4100713 | — | — | 1 | 6.23 |
| CHEMBL4081753 | — | — | 1 | 6.22 |
| CHEMBL3613152 | — | — | 1 | 6.20 |
| CHEMBL4085259 | — | — | 1 | 6.17 |
| CHEMBL4091502 | — | — | 1 | 6.16 |
| CHEMBL4101722 | — | — | 1 | 6.03 |
| CHEMBL4082902 | — | — | 1 | 6.00 |
| CHEMBL288826 | — | — | 1 | 5.97 |
| CHEMBL4099773 | — | — | 1 | 5.95 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.92 |
| CHEMBL3612830 | — | — | 1 | 5.87 |
| CHEMBL4091567 | — | — | 1 | 5.86 |
| CHEMBL4063684 | — | — | 1 | 5.79 |
| CHEMBL4105112 | — | — | 1 | 5.77 |
| CHEMBL4060900 | — | — | 1 | 5.65 |
| CHEMBL4095430 | — | — | 1 | 5.64 |
| CHEMBL4086279 | — | — | 1 | 5.56 |
| CHEMBL4063764 | — | — | 1 | 5.52 |
| CHEMBL4082767 | — | — | 1 | 5.44 |
| CHEMBL4101780 | — | — | 1 | 5.39 |
| CHEMBL4064805 | — | — | 1 | 5.25 |
| CHEMBL4073400 | — | — | 1 | 5.17 |
| CHEMBL4083782 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4073939 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4083724 | — | IC50 | = | 97.5 | nM | 7.01 |
| CHEMBL3613151 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4074999 | — | IC50 | = | 292.3 | nM | 6.53 |
| CHEMBL4092998 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4103183 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL4100713 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4081753 | — | IC50 | = | 608.0 | nM | 6.22 |
| CHEMBL3613152 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4085259 | — | IC50 | = | 679.8 | nM | 6.17 |
| CHEMBL4091502 | — | IC50 | = | 692.1 | nM | 6.16 |
| CHEMBL4101722 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4082902 | — | IC50 | = | 989.5 | nM | 6.00 |
| CHEMBL288826 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4099773 | — | IC50 | = | 1115.0 | nM | 5.95 |
| CHEMBL894 | BUPROPION | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3612830 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4091567 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL4063684 | — | IC50 | = | 1636.0 | nM | 5.79 |
| CHEMBL4105112 | — | IC50 | = | 1704.0 | nM | 5.77 |
| CHEMBL4060900 | — | IC50 | = | 2231.0 | nM | 5.65 |
| CHEMBL4095430 | — | IC50 | = | 2289.0 | nM | 5.64 |
| CHEMBL4086279 | — | IC50 | = | 2749.0 | nM | 5.56 |
| CHEMBL4063764 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4082767 | — | IC50 | = | 3640.0 | nM | 5.44 |
| CHEMBL4101780 | — | IC50 | = | 4098.0 | nM | 5.39 |
| CHEMBL4064805 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4073400 | — | IC50 | = | 6816.0 | nM | 5.17 |
| CHEMBL4083782 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4094047 | — | IC50 | = | 10000.0 | nM | 5.00 |