Assay Detail
Binding
CHEMBL790105
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of dopamine uptake in rat tissue, was determined using [3H]DAU as radioligand
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
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.66 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11776 | — | — | 1 | 8.01 |
| CHEMBL417249 | — | — | 1 | 7.85 |
| CHEMBL2308105 | — | — | 1 | 7.41 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.15 |
| CHEMBL3084641 | — | — | 1 | 6.89 |
| CHEMBL440272 | — | — | 1 | 6.75 |
| CHEMBL3084927 | — | — | 1 | 6.75 |
| CHEMBL11768 | — | — | 1 | 6.70 |
| CHEMBL12227 | — | — | 1 | 6.64 |
| CHEMBL12375 | — | — | 1 | 6.54 |
| CHEMBL11493 | — | — | 1 | 6.43 |
| CHEMBL3084934 | — | — | 1 | 6.19 |
| CHEMBL3084928 | — | — | 1 | 5.92 |
| CHEMBL137769 | — | — | 1 | 5.34 |
| CHEMBL135982 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11776 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL417249 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2308105 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL3084641 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL440272 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL3084927 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL11768 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL12227 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL12375 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL11493 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL3084934 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL3084928 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL137769 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL135982 | — | Ki | = | 5400.0 | nM | 5.27 |