Assay Detail
Binding
CHEMBL2176359
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Inhibition of human DAT expressed in HEK293 cells assessed as inhibition of dopamine reuptake after 30 mins by fluorescence assay
8
Total Activities
8
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
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.70 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171415 | — | — | 1 | 7.50 |
| CHEMBL2171417 | — | — | 1 | 7.46 |
| CHEMBL2171418 | — | — | 1 | 7.27 |
| CHEMBL2171416 | — | — | 1 | 7.14 |
| CHEMBL2171419 | — | — | 1 | 6.83 |
| CHEMBL543876 | — | — | 1 | 6.72 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 5.94 |
| CHEMBL1201082 | FLUOXETINE HYDROCHLORIDE | 4.0 | 1 | 4.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171415 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2171417 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2171418 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2171416 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2171419 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL543876 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL295467 | NISOXETINE | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL1201082 | FLUOXETINE HYDROCHLORIDE | IC50 | = | 18400.0 | nM | 4.74 |