Assay Detail
Binding
CHEMBL1780875
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-iodovinyl-TBZ from VMAT2 in rat striatal homogenate after 60 mins by gamma counting
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Synaptic vesicular amine transporter (CHEMBL4828) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.05 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL579217 | FLORBENAZINE | 2.0 | 1 | 10.00 |
| CHEMBL576222 | DIHYDROTETRABENAZINE | -1.0 | 1 | 8.99 |
| CHEMBL1780005 | — | — | 1 | 8.22 |
| CHEMBL1780006 | — | — | 1 | 7.57 |
| CHEMBL1780008 | — | — | 1 | 6.86 |
| CHEMBL1780007 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL579217 | FLORBENAZINE | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL576222 | DIHYDROTETRABENAZINE | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL1780005 | — | Ki | = | 5.98 | nM | 8.22 |
| CHEMBL1780006 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL1780008 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL1780007 | — | Ki | = | 227.0 | nM | 6.64 |