Assay Detail
Binding
CHEMBL677376
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Displacement of [3H]WIN-35428 from dopamine transporter of rat brain membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.28 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 8.39 |
| CHEMBL113144 | — | — | 1 | 8.24 |
| CHEMBL112825 | — | — | 1 | 8.20 |
| CHEMBL113195 | — | — | 1 | 7.50 |
| CHEMBL2112508 | — | — | 1 | 7.24 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.13 |
| CHEMBL2112509 | — | — | 1 | 7.12 |
| CHEMBL2112515 | — | — | 1 | 7.09 |
| CHEMBL2112513 | — | — | 1 | 6.97 |
| CHEMBL2112511 | — | — | 1 | 6.92 |
| CHEMBL2112512 | — | — | 1 | 6.83 |
| CHEMBL2112510 | — | — | 1 | 6.82 |
| CHEMBL2112514 | — | — | 1 | 6.77 |
| CHEMBL2112516 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 4.11 | nM | 8.39 |
| CHEMBL113144 | — | Ki | = | 5.81 | nM | 8.24 |
| CHEMBL112825 | — | Ki | = | 6.28 | nM | 8.20 |
| CHEMBL113195 | — | Ki | = | 31.3 | nM | 7.50 |
| CHEMBL2112508 | — | Ki | = | 57.1 | nM | 7.24 |
| CHEMBL370805 | COCAINE | Ki | = | 74.3 | nM | 7.13 |
| CHEMBL2112509 | — | Ki | = | 75.4 | nM | 7.12 |
| CHEMBL2112515 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL2112513 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL2112511 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL2112512 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL2112510 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL2112514 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL2112516 | — | Ki | = | 175.0 | nM | 6.76 |