Assay Detail
Binding
CHEMBL670050
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In vitro competitive binding versus [N-methyl-3H]WIN-35428 in murine kidney cells transfected with cDNA for human dopamine transporter (DAT)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | kidney |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.59 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL353333 | — | — | 1 | 9.92 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 9.31 |
| CHEMBL814 | FLUVOXAMINE | 4.0 | 1 | 8.84 |
| CHEMBL173427 | — | — | 1 | 8.73 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 7.52 |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL353333 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL814 | FLUVOXAMINE | Ki | = | 1.46 | nM | 8.84 |
| CHEMBL173427 | — | Ki | = | 1.88 | nM | 8.73 |
| CHEMBL295467 | NISOXETINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL14370 | REBOXETINE | Ki | = | 60.0 | nM | 7.22 |