Assay Detail
Functional
CHEMBL670036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]dopamine uptake in rat caudate putamen tissue.
37
Total Activities
37
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
CoMFA study of novel phenyl ring-substituted 3alpha-(diphenylmethoxy)tropane analogues at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.61 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3084896 | — | — | 1 | 7.62 |
| CHEMBL3084868 | — | — | 1 | 7.57 |
| 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 |
| CHEMBL3084879 | — | — | 1 | 6.98 |
| CHEMBL3084894 | — | — | 1 | 6.97 |
| CHEMBL310310 | — | — | 1 | 6.94 |
| CHEMBL3084902 | — | — | 1 | 6.91 |
| CHEMBL3084906 | — | — | 1 | 6.86 |
| CHEMBL3084869 | — | — | 1 | 6.85 |
| CHEMBL3084905 | — | — | 1 | 6.75 |
| CHEMBL3084908 | — | — | 1 | 6.74 |
| CHEMBL3084887 | — | — | 1 | 6.74 |
| CHEMBL3084899 | — | — | 1 | 6.66 |
| CHEMBL3084903 | — | — | 1 | 6.65 |
| CHEMBL3084900 | — | — | 1 | 6.65 |
| CHEMBL3084870 | — | — | 1 | 6.64 |
| CHEMBL3084907 | — | — | 1 | 6.60 |
| CHEMBL3084891 | AMINOBENZTROPINE | — | 1 | 6.43 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 6.39 |
| CHEMBL3084909 | — | — | 1 | 6.39 |
| CHEMBL3084901 | — | — | 1 | 6.34 |
| CHEMBL3084880 | — | — | 1 | 6.33 |
| CHEMBL3084881 | — | — | 1 | 6.29 |
| CHEMBL3084872 | — | — | 1 | 6.17 |
| CHEMBL3084893 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3084896 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3084868 | — | IC50 | = | 27.2 | nM | 7.57 |
| 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 |
| CHEMBL3084879 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3084894 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL310310 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3084902 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL3084906 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL3084869 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3084905 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL3084908 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL3084887 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL3084899 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL3084903 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL3084900 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL3084870 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL3084907 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3084891 | AMINOBENZTROPINE | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL3084909 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL3084901 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL3084880 | — | IC50 | = | 468.0 | nM | 6.33 |
| CHEMBL3084881 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL3084872 | — | IC50 | = | 677.0 | nM | 6.17 |
| CHEMBL3084893 | — | IC50 | = | 795.0 | nM | 6.10 |
| CHEMBL3084910 | — | IC50 | = | 977.0 | nM | 6.01 |
| CHEMBL3084898 | — | IC50 | = | 984.0 | nM | 6.01 |
| CHEMBL3084878 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3084873 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL3084888 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL3084867 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL3084866 | — | IC50 | = | 4460.0 | nM | 5.35 |