Assay Detail
Binding
CHEMBL911772
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Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat brain
18
Total Activities
18
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
Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.00 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214234 | — | — | 1 | 8.74 |
| CHEMBL310650 | — | — | 1 | 8.53 |
| CHEMBL217295 | — | — | 1 | 8.47 |
| CHEMBL384482 | — | — | 1 | 8.43 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 8.39 |
| CHEMBL413927 | — | — | 1 | 8.33 |
| CHEMBL317362 | — | — | 1 | 8.16 |
| CHEMBL217456 | — | — | 1 | 8.09 |
| CHEMBL214923 | — | — | 1 | 8.05 |
| CHEMBL384104 | — | — | 1 | 7.96 |
| CHEMBL386064 | — | — | 1 | 7.90 |
| CHEMBL217022 | — | — | 1 | 7.84 |
| CHEMBL3084884 | — | — | 1 | 7.76 |
| CHEMBL217018 | — | — | 1 | 7.66 |
| CHEMBL216990 | — | — | 1 | 7.63 |
| CHEMBL217160 | — | — | 1 | 7.56 |
| CHEMBL214574 | — | — | 1 | 7.40 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214234 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL310650 | — | Ki | = | 2.94 | nM | 8.53 |
| CHEMBL217295 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL384482 | — | Ki | = | 3.74 | nM | 8.43 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 4.11 | nM | 8.39 |
| CHEMBL413927 | — | Ki | = | 4.69 | nM | 8.33 |
| CHEMBL317362 | — | Ki | = | 6.87 | nM | 8.16 |
| CHEMBL217456 | — | Ki | = | 8.18 | nM | 8.09 |
| CHEMBL214923 | — | Ki | = | 8.87 | nM | 8.05 |
| CHEMBL384104 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL386064 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL217022 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL3084884 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL217018 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL216990 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL217160 | — | Ki | = | 27.6 | nM | 7.56 |
| CHEMBL214574 | — | Ki | = | 39.9 | nM | 7.40 |
| CHEMBL370805 | COCAINE | Ki | = | 71.8 | nM | 7.14 |