Assay Detail
Binding
CHEMBL677378
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Affinity for rat dopamine transporter using [3H]WIN-35428 displacement.
22
Total Activities
21
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 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 |
|---|---|---|---|
| Ki | 22 | 6.96 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.94 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.93 |
| CHEMBL3084896 | — | — | 1 | 7.72 |
| CHEMBL3084884 | — | — | 1 | 7.70 |
| CHEMBL3084892 | — | — | 1 | 7.68 |
| CHEMBL310310 | — | — | 2 | 7.52 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.50 |
| CHEMBL3084883 | — | — | 1 | 7.49 |
| CHEMBL3084882 | — | — | 1 | 7.42 |
| CHEMBL3084880 | — | — | 1 | 7.11 |
| CHEMBL3084897 | — | — | 1 | 7.04 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 6.93 |
| CHEMBL3084881 | — | — | 1 | 6.73 |
| CHEMBL3084899 | — | — | 1 | 6.71 |
| CHEMBL3084900 | — | — | 1 | 6.71 |
| CHEMBL3084872 | — | — | 1 | 6.53 |
| CHEMBL3084888 | — | — | 1 | 6.38 |
| CHEMBL3084898 | — | — | 1 | 6.28 |
| CHEMBL3084873 | — | — | 1 | 6.20 |
| CHEMBL3084866 | — | — | 1 | 5.72 |
| CHEMBL3084867 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL3084896 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL3084884 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3084892 | — | Ki | = | 21.1 | nM | 7.68 |
| CHEMBL310310 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL370805 | COCAINE | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL3084883 | — | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL3084882 | — | Ki | = | 37.9 | nM | 7.42 |
| CHEMBL3084880 | — | Ki | = | 78.4 | nM | 7.11 |
| CHEMBL3084897 | — | Ki | = | 91.6 | nM | 7.04 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL3084881 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL3084899 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL3084900 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL3084872 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL3084888 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL3084898 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL3084873 | — | Ki | = | 635.0 | nM | 6.20 |
| CHEMBL310310 | — | Ki | = | 854.0 | nM | 6.07 |
| CHEMBL3084866 | — | Ki | = | 1918.0 | nM | 5.72 |
| CHEMBL3084867 | — | Ki | = | 2000.0 | nM | 5.70 |