Assay Detail
Binding
CHEMBL677555
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Displacement of [3H]WIN-35 428 from the dopamine transporter in rat caudate putamen.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.17 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2308105 | — | — | 1 | 8.07 |
| CHEMBL11776 | — | — | 1 | 7.95 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.93 |
| CHEMBL3084934 | — | — | 1 | 7.70 |
| CHEMBL11493 | — | — | 1 | 7.61 |
| CHEMBL417249 | — | — | 1 | 7.52 |
| CHEMBL440272 | — | — | 1 | 7.49 |
| CHEMBL12227 | — | — | 1 | 7.38 |
| CHEMBL3084928 | — | — | 1 | 7.35 |
| CHEMBL12619 | — | — | 1 | 7.24 |
| CHEMBL11497 | — | — | 1 | 7.22 |
| CHEMBL12375 | — | — | 1 | 7.08 |
| CHEMBL3084927 | — | — | 1 | 7.06 |
| CHEMBL11768 | — | — | 1 | 7.02 |
| CHEMBL3084641 | — | — | 1 | 6.97 |
| CHEMBL323997 | — | — | 1 | 6.20 |
| CHEMBL135982 | — | — | 1 | 5.70 |
| CHEMBL137769 | — | — | 1 | 5.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2308105 | — | Ki | = | 8.51 | nM | 8.07 |
| CHEMBL11776 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL3084934 | — | Ki | = | 20.2 | nM | 7.70 |
| CHEMBL11493 | — | Ki | = | 24.6 | nM | 7.61 |
| CHEMBL417249 | — | Ki | = | 29.9 | nM | 7.52 |
| CHEMBL440272 | — | Ki | = | 32.4 | nM | 7.49 |
| CHEMBL12227 | — | Ki | = | 41.9 | nM | 7.38 |
| CHEMBL3084928 | — | Ki | = | 44.6 | nM | 7.35 |
| CHEMBL12619 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL11497 | — | Ki | = | 60.7 | nM | 7.22 |
| CHEMBL12375 | — | Ki | = | 82.2 | nM | 7.08 |
| CHEMBL3084927 | — | Ki | = | 86.4 | nM | 7.06 |
| CHEMBL11768 | — | Ki | = | 95.6 | nM | 7.02 |
| CHEMBL3084641 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL323997 | — | Ki | = | 634.0 | nM | 6.20 |
| CHEMBL135982 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL137769 | — | Ki | = | 2340.0 | nM | 5.63 |