Assay Detail
Functional
CHEMBL671631
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In vitro potency for inhibiting [3H]- dopamine uptake was determined
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| IC50 | 13 | 8.23 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310650 | — | — | 1 | 8.82 |
| CHEMBL317362 | — | — | 1 | 8.74 |
| CHEMBL316634 | — | — | 1 | 8.66 |
| CHEMBL95775 | — | — | 1 | 8.59 |
| CHEMBL97971 | — | — | 1 | 8.48 |
| CHEMBL99038 | — | — | 1 | 8.21 |
| CHEMBL98279 | — | — | 1 | 8.10 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.86 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.63 |
| CHEMBL98645 | — | — | 1 | - |
| CHEMBL101001 | — | — | 1 | - |
| CHEMBL432814 | — | — | 1 | - |
| CHEMBL99354 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310650 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL317362 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL316634 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL95775 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL97971 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL99038 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL98279 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL370805 | COCAINE | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL98645 | — | IC50 | = | - | nM | - |
| CHEMBL101001 | — | IC50 | = | - | nM | - |
| CHEMBL432814 | — | IC50 | = | - | nM | - |
| CHEMBL99354 | — | IC50 | = | - | nM | - |