Assay Detail
Functional
CHEMBL671630
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro potency for inhibiting [3H]- dopamine uptake in rat brain was determined
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 5 | 8.47 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42553 | — | — | 1 | 8.85 |
| CHEMBL330651 | — | — | 1 | 8.72 |
| CHEMBL420084 | — | — | 1 | 8.57 |
| CHEMBL318184 | — | — | 1 | 8.49 |
| CHEMBL328204 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42553 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL330651 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL420084 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL318184 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL328204 | — | IC50 | = | 19.0 | nM | 7.72 |