Assay Detail
Binding
CHEMBL911773
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Inhibition of [3H]dopamine uptake at DAT in Sprague-Dawley rat brain
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.21 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310650 | — | — | 1 | 8.82 |
| CHEMBL217022 | — | — | 1 | 8.82 |
| CHEMBL317362 | — | — | 1 | 8.74 |
| CHEMBL386064 | — | — | 1 | 8.61 |
| CHEMBL3084884 | — | — | 1 | 7.63 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.63 |
| CHEMBL216990 | — | — | 1 | - |
| CHEMBL217018 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310650 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL217022 | — | IC50 | = | 1.52 | nM | 8.82 |
| CHEMBL317362 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL386064 | — | IC50 | = | 2.46 | nM | 8.61 |
| CHEMBL3084884 | — | IC50 | = | 23.4 | nM | 7.63 |
| CHEMBL370805 | COCAINE | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL216990 | — | IC50 | - | — | - | |
| CHEMBL217018 | — | IC50 | - | — | - |