Assay Detail
Binding
CHEMBL678249
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In vitro dopamine transporter binding affinity using [3H]WIN-35428 as radioligand was determined
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.59 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL330651 | — | — | 1 | 8.26 |
| CHEMBL42553 | — | — | 1 | 8.20 |
| CHEMBL318184 | — | — | 1 | 7.96 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.93 |
| CHEMBL310650 | — | — | 1 | 7.87 |
| CHEMBL317362 | — | — | 1 | 7.79 |
| CHEMBL420084 | — | — | 1 | 7.75 |
| CHEMBL99038 | — | — | 1 | 7.52 |
| CHEMBL328204 | — | — | 1 | 7.46 |
| CHEMBL98279 | — | — | 1 | 7.43 |
| CHEMBL95775 | — | — | 1 | 7.43 |
| CHEMBL101001 | — | — | 1 | 7.37 |
| CHEMBL316634 | — | — | 1 | 7.32 |
| CHEMBL97971 | — | — | 1 | 7.01 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL330651 | — | Ki | = | 5.54 | nM | 8.26 |
| CHEMBL42553 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL318184 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL310650 | — | Ki | = | 13.4 | nM | 7.87 |
| CHEMBL317362 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL420084 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL99038 | — | Ki | = | 30.3 | nM | 7.52 |
| CHEMBL328204 | — | Ki | = | 34.7 | nM | 7.46 |
| CHEMBL98279 | — | Ki | = | 36.7 | nM | 7.43 |
| CHEMBL95775 | — | Ki | = | 36.7 | nM | 7.43 |
| CHEMBL101001 | — | Ki | = | 42.3 | nM | 7.37 |
| CHEMBL316634 | — | Ki | = | 48.4 | nM | 7.32 |
| CHEMBL97971 | — | Ki | = | 97.7 | nM | 7.01 |
| CHEMBL370805 | COCAINE | Ki | = | 285.0 | nM | 6.54 |