Assay Detail
Binding
CHEMBL677557
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Displacement of [3H]WIN-35428 from dopamine transporter (DAT) in Rat Caudate Putamen
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Putamen |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, dopamine transporter affinity, dopamine uptake inhibition, and locomotor stimulant activity of 2-substituted 3 beta-phenyltropane derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.43 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL354879 | — | — | 1 | 7.96 |
| CHEMBL353307 | — | — | 1 | 7.80 |
| CHEMBL353829 | — | — | 1 | 7.70 |
| CHEMBL169971 | — | — | 1 | 7.66 |
| CHEMBL353860 | — | — | 1 | 7.64 |
| CHEMBL353240 | — | — | 1 | 7.55 |
| CHEMBL353112 | — | — | 1 | 7.52 |
| CHEMBL370805 | COCAINE | 4.0 | 2 | 7.50 |
| CHEMBL3085532 | — | — | 2 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL354879 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL353307 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL353829 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL169971 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL353860 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL353240 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL353112 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL370805 | COCAINE | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL3085532 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3085532 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL370805 | COCAINE | Ki | = | 388.0 | nM | 6.41 |