Assay Detail
Binding
CHEMBL673259
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Inhibition of [3H]WIN-35428 binding to the dopamine transporter in cynomolgus (macaca fascicularis) monkey caudate putamen.
22
Total Activities
17
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 | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.72 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL87031 | — | — | 3 | 9.40 |
| CHEMBL87567 | — | — | 1 | 9.31 |
| CHEMBL318138 | — | — | 1 | 9.24 |
| CHEMBL322923 | — | — | 1 | 8.15 |
| CHEMBL2111614 | — | — | 2 | 8.02 |
| CHEMBL103152 | — | — | 1 | 7.96 |
| CHEMBL2079586 | — | — | 2 | 7.96 |
| CHEMBL2111613 | — | — | 2 | 7.92 |
| CHEMBL388545 | — | — | 1 | 7.85 |
| CHEMBL322605 | — | — | 1 | 7.60 |
| CHEMBL2112412 | — | — | 1 | 7.57 |
| CHEMBL103919 | — | — | 1 | 7.38 |
| CHEMBL103936 | — | — | 1 | 6.84 |
| CHEMBL319523 | — | — | 1 | 6.47 |
| CHEMBL327963 | — | — | 1 | 6.41 |
| CHEMBL317714 | — | — | 1 | 6.26 |
| CHEMBL102144 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL87031 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL87567 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL318138 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL87031 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL87031 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL322923 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL2111614 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL103152 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2079586 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2111613 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2111614 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL388545 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2111613 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL322605 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2112412 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL103919 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL103936 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL319523 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL327963 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL317714 | — | IC50 | = | 548.0 | nM | 6.26 |
| CHEMBL2079586 | — | IC50 | = | 633.0 | nM | 6.20 |
| CHEMBL102144 | — | IC50 | = | 1000.0 | nM | 6.00 |