Assay Detail
Binding
CHEMBL4829580
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptosome incubated for 10 mins followed by [3H]DA addition and measured after 20 mins by TopCount scintillation counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Subcellular | Synaptosome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Synaptic vesicular amine transporter (CHEMBL4828) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.82 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4873900 | — | — | 1 | 8.29 |
| CHEMBL4874168 | — | — | 1 | 8.24 |
| CHEMBL4854730 | — | — | 1 | 8.22 |
| CHEMBL117785 | TETRABENAZINE | 4.0 | 1 | 7.96 |
| CHEMBL4859304 | — | — | 1 | 7.75 |
| CHEMBL576222 | DIHYDROTETRABENAZINE | -1.0 | 1 | 7.70 |
| CHEMBL4860699 | — | — | 1 | 7.55 |
| CHEMBL4874676 | — | — | 1 | 7.45 |
| CHEMBL4867332 | — | — | 1 | 7.19 |
| CHEMBL567232 | — | — | 1 | - |
| CHEMBL4867056 | — | — | 1 | - |
| CHEMBL213814 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4873900 | — | IC50 | = | 5.14 | nM | 8.29 |
| CHEMBL4874168 | — | IC50 | = | 5.72 | nM | 8.24 |
| CHEMBL4854730 | — | IC50 | = | 6.04 | nM | 8.22 |
| CHEMBL117785 | TETRABENAZINE | IC50 | = | 10.98 | nM | 7.96 |
| CHEMBL4859304 | — | IC50 | = | 17.83 | nM | 7.75 |
| CHEMBL576222 | DIHYDROTETRABENAZINE | IC50 | = | 20.01 | nM | 7.70 |
| CHEMBL4860699 | — | IC50 | = | 27.89 | nM | 7.55 |
| CHEMBL4874676 | — | IC50 | = | 35.24 | nM | 7.45 |
| CHEMBL4867332 | — | IC50 | = | 64.91 | nM | 7.19 |
| CHEMBL567232 | — | IC50 | - | — | - | |
| CHEMBL4867056 | — | IC50 | - | — | - | |
| CHEMBL213814 | — | IC50 | - | — | - |