Assay Detail
Binding
CHEMBL673255
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Displacement of [3H]WIN-35428 from monkey dopamine transporter
11
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of an unusually selective and novel cocaine analog: difluoropine. Synthesis and inhibition of binding at cocaine recognition sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.21 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300226 | — | — | 1 | 8.97 |
| CHEMBL310650 | — | — | 1 | 7.96 |
| CHEMBL2079586 | — | — | 1 | 7.89 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 6.51 |
| CHEMBL607377 | — | — | 4 | 5.76 |
| CHEMBL607431 | — | — | 1 | 5.47 |
| CHEMBL607430 | — | — | 2 | 4.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300226 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL310650 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL2079586 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL607377 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL607377 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL607431 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL607377 | — | IC50 | = | 3840.0 | nM | 5.42 |
| CHEMBL607377 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL607430 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL607430 | — | IC50 | = | 21900.0 | nM | 4.66 |