Assay Detail
Binding
CHEMBL672387
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inhibition of [3H]WIN-35428 binding to the dopamine transporter (DAT) in monkey caudate-putamen.
10
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-Carbomethoxy-3-aryl-8-oxabicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.36 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL87031 | — | — | 2 | 9.40 |
| CHEMBL14391 | — | — | 2 | 8.90 |
| CHEMBL306208 | — | — | 2 | 8.85 |
| CHEMBL2079586 | — | — | 2 | 7.96 |
| CHEMBL1790051 | — | — | 2 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL87031 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL87031 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL14391 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL306208 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL306208 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL14391 | — | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL2079586 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2079586 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1790051 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1790051 | — | IC50 | = | 101.0 | nM | 7.00 |