Assay Detail
Binding
CHEMBL672989
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Ability to displace [3H]WIN-35428 from dopamine transporter on guinea pig striatal membrane.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.80 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL334577 | — | — | 1 | 8.68 |
| CHEMBL337020 | — | — | 1 | 8.57 |
| CHEMBL340281 | — | — | 1 | 8.48 |
| CHEMBL132676 | — | — | 1 | 8.39 |
| CHEMBL130477 | — | — | 1 | 8.38 |
| CHEMBL424627 | — | — | 1 | 8.08 |
| CHEMBL133646 | — | — | 1 | 7.97 |
| CHEMBL130877 | — | — | 1 | 7.44 |
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 7.37 |
| CHEMBL130593 | — | — | 1 | 6.66 |
| CHEMBL132713 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL334577 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL337020 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL340281 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL132676 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL130477 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL424627 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL133646 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL130877 | — | IC50 | = | 36.1 | nM | 7.44 |
| CHEMBL781 | MAZINDOL | IC50 | = | 42.6 | nM | 7.37 |
| CHEMBL130593 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL132713 | — | IC50 | = | 1841.0 | nM | 5.74 |