Assay Detail
Binding
CHEMBL677377
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Displacement of [3H]WIN-35428 binding to the dopamine transporter in rat caudate putamen tissue.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
CoMFA study of novel phenyl ring-substituted 3alpha-(diphenylmethoxy)tropane analogues at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 7.04 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.93 |
| CHEMBL3084868 | — | — | 1 | 7.82 |
| CHEMBL3084896 | — | — | 1 | 7.72 |
| CHEMBL3084884 | — | — | 1 | 7.70 |
| CHEMBL3084892 | — | — | 1 | 7.68 |
| CHEMBL3084870 | — | — | 1 | 7.66 |
| CHEMBL3084906 | — | — | 1 | 7.63 |
| CHEMBL3084902 | — | — | 1 | 7.63 |
| CHEMBL3084879 | — | — | 1 | 7.57 |
| CHEMBL3084908 | — | — | 1 | 7.55 |
| CHEMBL310310 | — | — | 1 | 7.52 |
| CHEMBL3084894 | — | — | 1 | 7.51 |
| CHEMBL3084883 | — | — | 1 | 7.49 |
| CHEMBL3084905 | — | — | 1 | 7.42 |
| CHEMBL3084882 | — | — | 1 | 7.42 |
| CHEMBL3084909 | — | — | 1 | 7.32 |
| CHEMBL3084869 | — | — | 1 | 7.30 |
| CHEMBL3084907 | — | — | 1 | 7.16 |
| CHEMBL3084880 | — | — | 1 | 7.11 |
| CHEMBL3084903 | — | — | 1 | 7.11 |
| CHEMBL3084887 | — | — | 1 | 7.05 |
| CHEMBL3084897 | — | — | 1 | 7.04 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 6.93 |
| CHEMBL3084901 | — | — | 1 | 6.73 |
| CHEMBL3084893 | — | — | 1 | 6.73 |
| CHEMBL3084881 | — | — | 1 | 6.73 |
| CHEMBL3084900 | — | — | 1 | 6.71 |
| CHEMBL3084899 | — | — | 1 | 6.71 |
| CHEMBL3084910 | — | — | 1 | 6.64 |
| CHEMBL3084872 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL3084868 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL3084896 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL3084884 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3084892 | — | Ki | = | 21.1 | nM | 7.68 |
| CHEMBL3084870 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3084906 | — | Ki | = | 23.3 | nM | 7.63 |
| CHEMBL3084902 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL3084879 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3084908 | — | Ki | = | 27.9 | nM | 7.55 |
| CHEMBL310310 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3084894 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL3084883 | — | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL3084905 | — | Ki | = | 38.2 | nM | 7.42 |
| CHEMBL3084882 | — | Ki | = | 37.9 | nM | 7.42 |
| CHEMBL3084909 | — | Ki | = | 47.4 | nM | 7.32 |
| CHEMBL3084869 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL3084907 | — | Ki | = | 68.5 | nM | 7.16 |
| CHEMBL3084880 | — | Ki | = | 78.4 | nM | 7.11 |
| CHEMBL3084903 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL3084887 | — | Ki | = | 88.1 | nM | 7.05 |
| CHEMBL3084897 | — | Ki | = | 91.6 | nM | 7.04 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL3084901 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL3084893 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL3084881 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL3084900 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL3084899 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL3084910 | — | Ki | = | 228.0 | nM | 6.64 |
| CHEMBL3084872 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL3084878 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL3084888 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL3084898 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL3084873 | — | Ki | = | 635.0 | nM | 6.20 |
| CHEMBL3084891 | AMINOBENZTROPINE | Ki | = | 1840.0 | nM | 5.74 |
| CHEMBL3084866 | — | Ki | = | 1920.0 | nM | 5.72 |
| CHEMBL3084867 | — | Ki | = | 2000.0 | nM | 5.70 |