Assay Detail
Binding
CHEMBL677366
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Binding affinity at dopamine transporter in rat brain by [3H]WIN-35428 displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.46 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112280 | — | — | 1 | 9.05 |
| CHEMBL543876 | — | — | 1 | 8.43 |
| CHEMBL2308105 | — | — | 1 | 8.07 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.93 |
| CHEMBL112528 | — | — | 1 | 7.90 |
| CHEMBL115253 | — | — | 1 | 7.88 |
| CHEMBL3085021 | — | — | 1 | 7.86 |
| CHEMBL3084884 | — | — | 1 | 7.70 |
| CHEMBL115311 | — | — | 1 | 7.58 |
| CHEMBL3085020 | — | — | 1 | 7.56 |
| CHEMBL324518 | — | — | 1 | 7.44 |
| CHEMBL326706 | — | — | 1 | 7.37 |
| CHEMBL115370 | — | — | 1 | 7.32 |
| CHEMBL325826 | — | — | 1 | 7.31 |
| CHEMBL327055 | — | — | 1 | 7.18 |
| CHEMBL326604 | — | — | 1 | 6.74 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.54 |
| CHEMBL111928 | — | — | 1 | 6.15 |
| CHEMBL115710 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112280 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL543876 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL2308105 | — | Ki | = | 8.51 | nM | 8.07 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL112528 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL115253 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL3085021 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL3084884 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL115311 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3085020 | — | Ki | = | 27.6 | nM | 7.56 |
| CHEMBL324518 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL326706 | — | Ki | = | 42.6 | nM | 7.37 |
| CHEMBL115370 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL325826 | — | Ki | = | 48.5 | nM | 7.31 |
| CHEMBL327055 | — | Ki | = | 65.9 | nM | 7.18 |
| CHEMBL326604 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL370805 | COCAINE | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL111928 | — | Ki | = | 703.0 | nM | 6.15 |
| CHEMBL115710 | — | Ki | = | 1620.0 | nM | 5.79 |