Assay Detail
Functional
CHEMBL672997
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Inhibition of dopamine uptake in HEK cells expressing human dopamine transporter (hDAT)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.42 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130477 | — | — | 1 | 8.43 |
| CHEMBL132955 | — | — | 1 | 8.22 |
| CHEMBL336613 | — | — | 1 | 8.22 |
| CHEMBL132082 | — | — | 1 | 7.78 |
| CHEMBL133043 | — | — | 1 | 7.52 |
| CHEMBL336940 | — | — | 1 | 7.38 |
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 7.37 |
| CHEMBL130668 | — | — | 1 | 7.23 |
| CHEMBL132954 | — | — | 1 | 7.22 |
| CHEMBL336100 | — | — | 1 | 7.04 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.53 |
| CHEMBL133902 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130477 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL132955 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL336613 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL132082 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL133043 | — | IC50 | = | 30.4 | nM | 7.52 |
| CHEMBL336940 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL781 | MAZINDOL | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL130668 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL132954 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL336100 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL370805 | COCAINE | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL133902 | — | IC50 | = | 730.0 | nM | 6.14 |