Assay Detail
Binding
CHEMBL872897
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Affinity for dopamine transporter was assessed by the ability to displace [3H]WIN-35428 from rat caudate-putamen tissue
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.22 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19944 | — | — | 1 | 7.96 |
| CHEMBL2079577 | — | — | 1 | 7.85 |
| CHEMBL279074 | — | — | 1 | 7.77 |
| CHEMBL2079656 | — | — | 1 | 7.60 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.50 |
| CHEMBL2112763 | — | — | 1 | 7.07 |
| CHEMBL276332 | — | — | 1 | 6.91 |
| CHEMBL19715 | — | — | 1 | 6.87 |
| CHEMBL2112762 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19944 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2079577 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL279074 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2079656 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL370805 | COCAINE | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2112763 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL276332 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL19715 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL2112762 | — | Ki | = | 3490.0 | nM | 5.46 |