Assay Detail
Functional
CHEMBL785171
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]dopamine uptake in rat caudate putamen.
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.53 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3084896 | — | — | 1 | 7.62 |
| CHEMBL3084882 | — | — | 1 | 7.54 |
| CHEMBL3084897 | — | — | 1 | 7.47 |
| CHEMBL3084892 | — | — | 1 | 7.33 |
| CHEMBL3084883 | — | — | 1 | 7.32 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.15 |
| CHEMBL3084884 | — | — | 1 | 7.12 |
| CHEMBL310310 | — | — | 2 | 6.94 |
| CHEMBL3084899 | — | — | 1 | 6.66 |
| CHEMBL3084900 | — | — | 1 | 6.65 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 6.39 |
| CHEMBL3084880 | — | — | 1 | 6.33 |
| CHEMBL3084881 | — | — | 1 | 6.29 |
| CHEMBL3084872 | — | — | 1 | 6.17 |
| CHEMBL3084898 | — | — | 1 | 6.01 |
| CHEMBL3084873 | — | — | 1 | 5.67 |
| CHEMBL3084888 | — | — | 1 | 5.60 |
| CHEMBL3084867 | — | — | 1 | 5.54 |
| CHEMBL3084866 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3084896 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3084882 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3084897 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3084892 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3084883 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3084884 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL310310 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3084899 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL3084900 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL3084880 | — | IC50 | = | 468.0 | nM | 6.33 |
| CHEMBL3084881 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL3084872 | — | IC50 | = | 677.0 | nM | 6.17 |
| CHEMBL3084898 | — | IC50 | = | 984.0 | nM | 6.01 |
| CHEMBL3084873 | — | IC50 | = | 2155.0 | nM | 5.67 |
| CHEMBL3084888 | — | IC50 | = | 2536.0 | nM | 5.60 |
| CHEMBL3084867 | — | IC50 | = | 2876.0 | nM | 5.54 |
| CHEMBL310310 | — | IC50 | = | 3519.0 | nM | 5.45 |
| CHEMBL3084866 | — | IC50 | = | 4456.0 | nM | 5.35 |