Assay Detail
Binding
CHEMBL677372
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Binding affinity towards dopamine transporter using [3H]- mazindol as radioligand in rat striatal membranes
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 5.27 | 6.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.55 |
| CHEMBL301281 | — | — | 1 | 6.27 |
| CHEMBL301941 | — | — | 2 | 5.51 |
| CHEMBL53436 | — | — | 2 | 5.33 |
| CHEMBL2310930 | PSEUDOCOCAINE | — | 1 | 4.98 |
| CHEMBL299297 | — | — | 1 | 4.47 |
| CHEMBL50518 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370805 | COCAINE | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL301281 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL301941 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL301941 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL53436 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL2310930 | PSEUDOCOCAINE | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL53436 | — | Ki | = | 29400.0 | nM | 4.53 |
| CHEMBL299297 | — | Ki | = | 34000.0 | nM | 4.47 |
| CHEMBL50518 | — | Ki | = | 38000.0 | nM | 4.42 |