Assay Detail
Binding
CHEMBL670588
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Inhibition of [3H]WIN-35428 binding to the dopamine transporter in rat brain
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.87 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL133786 | — | — | 1 | 9.00 |
| CHEMBL130255 | — | — | 1 | 8.82 |
| CHEMBL337510 | — | — | 1 | 8.77 |
| CHEMBL130477 | — | — | 1 | 8.77 |
| CHEMBL133795 | — | — | 1 | 8.70 |
| CHEMBL129899 | — | — | 1 | 8.60 |
| CHEMBL132198 | — | — | 1 | 8.59 |
| CHEMBL336654 | — | — | 1 | 8.49 |
| CHEMBL132241 | — | — | 1 | 8.37 |
| CHEMBL337052 | — | — | 1 | 8.24 |
| CHEMBL129885 | — | — | 1 | 8.23 |
| CHEMBL130394 | — | — | 1 | 8.20 |
| CHEMBL336413 | — | — | 1 | 8.19 |
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 8.09 |
| CHEMBL133355 | — | — | 1 | 7.88 |
| CHEMBL132955 | — | — | 1 | 7.87 |
| CHEMBL335296 | — | — | 1 | 7.76 |
| CHEMBL132206 | — | — | 1 | 7.63 |
| CHEMBL147748 | — | — | 1 | 7.53 |
| CHEMBL337299 | — | — | 1 | 7.30 |
| CHEMBL339169 | — | — | 1 | 7.28 |
| CHEMBL442765 | — | — | 1 | 7.24 |
| CHEMBL133902 | — | — | 1 | 7.18 |
| CHEMBL130198 | — | — | 1 | 7.12 |
| CHEMBL336313 | — | — | 1 | 7.06 |
| CHEMBL2112004 | — | — | 1 | 7.05 |
| CHEMBL339841 | — | — | 1 | 6.53 |
| CHEMBL337634 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL133786 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL130255 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL337510 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL130477 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL133795 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL129899 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL132198 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL336654 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL132241 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL337052 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL129885 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL130394 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL336413 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL781 | MAZINDOL | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL133355 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL132955 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL335296 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL132206 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL147748 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL337299 | — | IC50 | = | 50.4 | nM | 7.30 |
| CHEMBL339169 | — | IC50 | = | 52.8 | nM | 7.28 |
| CHEMBL442765 | — | IC50 | = | 57.2 | nM | 7.24 |
| CHEMBL133902 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL130198 | — | IC50 | = | 76.5 | nM | 7.12 |
| CHEMBL336313 | — | IC50 | = | 86.4 | nM | 7.06 |
| CHEMBL2112004 | — | IC50 | = | 89.1 | nM | 7.05 |
| CHEMBL339841 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL337634 | — | IC50 | = | 1340.0 | nM | 5.87 |