Assay Detail
Binding
CHEMBL4046313
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Inhibition of re-uptake of [3H]-DA at human DAT expressed in HEK293 cells by liquid scintillation counting
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 dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.52 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.40 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.92 |
| CHEMBL4068516 | — | — | 1 | 5.70 |
| CHEMBL4063974 | — | — | 1 | 5.48 |
| CHEMBL4083042 | — | — | 1 | 5.43 |
| CHEMBL4061167 | — | — | 1 | 5.40 |
| CHEMBL4099475 | — | — | 1 | 5.30 |
| CHEMBL4101959 | — | — | 1 | 5.29 |
| CHEMBL4071385 | — | — | 1 | 5.22 |
| CHEMBL4083969 | — | — | 1 | 5.18 |
| CHEMBL4073602 | — | — | 1 | 5.08 |
| CHEMBL4074417 | — | — | 1 | 4.84 |
| CHEMBL4072566 | — | — | 1 | - |
| CHEMBL4091738 | — | — | 1 | - |
| CHEMBL4094228 | — | — | 1 | - |
| CHEMBL4081927 | — | — | 1 | - |
| CHEMBL4060019 | — | — | 1 | - |
| CHEMBL4095847 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL894 | BUPROPION | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4068516 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL4063974 | — | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL4083042 | — | IC50 | = | 3740.0 | nM | 5.43 |
| CHEMBL4061167 | — | IC50 | = | 4020.0 | nM | 5.40 |
| CHEMBL4099475 | — | IC50 | = | 5040.0 | nM | 5.30 |
| CHEMBL4101959 | — | IC50 | = | 5180.0 | nM | 5.29 |
| CHEMBL4071385 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4083969 | — | IC50 | = | 6550.0 | nM | 5.18 |
| CHEMBL4073602 | — | IC50 | = | 8320.0 | nM | 5.08 |
| CHEMBL4074417 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL4072566 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4091738 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4094228 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4081927 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4060019 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4095847 | — | IC50 | > | 10000.0 | nM | - |