Assay Detail
Binding
CHEMBL673260
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Inhibition of [3H]WIN-35428 binding to the dopamine transporter (DAT) in monkey caudate-putamen.
28
Total Activities
14
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-oxabicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.72 | 8.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316342 | — | — | 6 | 8.63 |
| CHEMBL313664 | — | — | 2 | 8.15 |
| CHEMBL88792 | — | — | 2 | 8.05 |
| CHEMBL90903 | — | — | 2 | 8.00 |
| CHEMBL310650 | — | — | 2 | 7.96 |
| CHEMBL88163 | — | — | 1 | 6.28 |
| CHEMBL329454 | — | — | 2 | 6.26 |
| CHEMBL327314 | — | — | 2 | 5.76 |
| CHEMBL314402 | — | — | 2 | 5.72 |
| CHEMBL607377 | — | — | 2 | 5.69 |
| CHEMBL89284 | — | — | 2 | 5.42 |
| CHEMBL327868 | — | — | 1 | 4.69 |
| CHEMBL89324 | — | — | 1 | 4.65 |
| CHEMBL88986 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316342 | — | IC50 | = | 2.34 | nM | 8.63 |
| CHEMBL316342 | — | IC50 | = | 3.08 | nM | 8.51 |
| CHEMBL316342 | — | IC50 | = | 3.27 | nM | 8.48 |
| CHEMBL316342 | — | IC50 | = | 3.35 | nM | 8.47 |
| CHEMBL313664 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL88792 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL90903 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL310650 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL88792 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL90903 | — | IC50 | = | 28.5 | nM | 7.54 |
| CHEMBL313664 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL316342 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL316342 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL88163 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL329454 | — | IC50 | = | 546.0 | nM | 6.26 |
| CHEMBL327314 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL314402 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL607377 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL607377 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL89284 | — | IC50 | = | 3840.0 | nM | 5.42 |
| CHEMBL89284 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL310650 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL327868 | — | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL327314 | — | IC50 | = | 21900.0 | nM | 4.66 |
| CHEMBL89324 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL329454 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL88986 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL314402 | — | IC50 | > | 1000.0 | nM | - |