Assay Detail
Binding
CHEMBL4046312
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Inhibition of re-uptake of [3H]-NE at human NET expressed in HEK293 cells by liquid scintillation counting
19
Total Activities
19
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
Triple reuptake inhibitors: Design, synthesis and structure-activity relationship of benzylpiperidine-tetrazoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.57 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.96 |
| CHEMBL4068516 | — | — | 1 | 5.87 |
| CHEMBL4063974 | — | — | 1 | 5.64 |
| CHEMBL4071385 | — | — | 1 | 5.60 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 5.59 |
| CHEMBL4073602 | — | — | 1 | 5.59 |
| CHEMBL4061167 | — | — | 1 | 5.52 |
| CHEMBL4099475 | — | — | 1 | 5.52 |
| CHEMBL4074417 | — | — | 1 | 5.51 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.49 |
| CHEMBL4094228 | — | — | 1 | 5.46 |
| CHEMBL4060019 | — | — | 1 | 5.46 |
| CHEMBL4101959 | — | — | 1 | 5.45 |
| CHEMBL4083969 | — | — | 1 | 5.40 |
| CHEMBL4081927 | — | — | 1 | 5.36 |
| CHEMBL4072566 | — | — | 1 | 5.30 |
| CHEMBL4083042 | — | — | 1 | 5.29 |
| CHEMBL4091738 | — | — | 1 | 5.26 |
| CHEMBL4095847 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4068516 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4063974 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL4071385 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL4073602 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL4061167 | — | IC50 | = | 3030.0 | nM | 5.52 |
| CHEMBL4099475 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4074417 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL894 | BUPROPION | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL4094228 | — | IC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL4060019 | — | IC50 | = | 3450.0 | nM | 5.46 |
| CHEMBL4101959 | — | IC50 | = | 3590.0 | nM | 5.45 |
| CHEMBL4083969 | — | IC50 | = | 3960.0 | nM | 5.40 |
| CHEMBL4081927 | — | IC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL4072566 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL4083042 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4091738 | — | IC50 | = | 5520.0 | nM | 5.26 |
| CHEMBL4095847 | — | IC50 | > | 10000.0 | nM | - |