Assay Detail
Binding
CHEMBL863450
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Displacement of [3H]WIN-from DAT in rat brain membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.69 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 8.39 |
| CHEMBL3085031 | — | — | 1 | 8.34 |
| CHEMBL3085032 | — | — | 1 | 8.27 |
| CHEMBL3085021 | — | — | 1 | 8.25 |
| CHEMBL3085020 | — | — | 1 | 8.21 |
| CHEMBL3085027 | — | — | 1 | 8.07 |
| CHEMBL3350391 | — | — | 1 | 7.95 |
| CHEMBL3085030 | — | — | 1 | 7.93 |
| CHEMBL3085023 | — | — | 1 | 7.90 |
| CHEMBL3085029 | — | — | 1 | 7.67 |
| CHEMBL3085028 | — | — | 1 | 7.57 |
| CHEMBL3085022 | — | — | 1 | 7.54 |
| CHEMBL3085025 | — | — | 1 | 7.44 |
| CHEMBL3085024 | — | — | 1 | 7.42 |
| CHEMBL3085018 | — | — | 1 | 7.19 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.13 |
| CHEMBL3085033 | — | — | 1 | 6.91 |
| CHEMBL3085019 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 4.11 | nM | 8.39 |
| CHEMBL3085031 | — | Ki | = | 4.61 | nM | 8.34 |
| CHEMBL3085032 | — | Ki | = | 5.35 | nM | 8.27 |
| CHEMBL3085021 | — | Ki | = | 5.59 | nM | 8.25 |
| CHEMBL3085020 | — | Ki | = | 6.22 | nM | 8.21 |
| CHEMBL3085027 | — | Ki | = | 8.45 | nM | 8.07 |
| CHEMBL3350391 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL3085030 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL3085023 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL3085029 | — | Ki | = | 21.5 | nM | 7.67 |
| CHEMBL3085028 | — | Ki | = | 26.8 | nM | 7.57 |
| CHEMBL3085022 | — | Ki | = | 29.2 | nM | 7.54 |
| CHEMBL3085025 | — | Ki | = | 36.5 | nM | 7.44 |
| CHEMBL3085024 | — | Ki | = | 38.1 | nM | 7.42 |
| CHEMBL3085018 | — | Ki | = | 64.5 | nM | 7.19 |
| CHEMBL370805 | COCAINE | Ki | = | 74.3 | nM | 7.13 |
| CHEMBL3085033 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL3085019 | — | Ki | = | 661.0 | nM | 6.18 |