Assay Detail
Binding
CHEMBL1044341
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DTBZ from VMAT2 in rat striatal membrane homogenates
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Synaptic vesicular amine transporter (CHEMBL4828) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of 2-amino-dihydrotetrabenzine derivatives as probes for imaging vesicular monoamine transporter-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.53 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL579217 | FLORBENAZINE | 2.0 | 1 | 9.44 |
| CHEMBL576222 | DIHYDROTETRABENAZINE | -1.0 | 1 | 8.43 |
| CHEMBL569074 | — | — | 1 | 8.15 |
| CHEMBL571308 | — | — | 3 | 8.06 |
| CHEMBL567232 | — | — | 1 | 6.82 |
| CHEMBL569075 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL579217 | FLORBENAZINE | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL576222 | DIHYDROTETRABENAZINE | Ki | = | 3.75 | nM | 8.43 |
| CHEMBL569074 | — | Ki | = | 7.01 | nM | 8.15 |
| CHEMBL571308 | — | Ki | = | 8.63 | nM | 8.06 |
| CHEMBL567232 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL571308 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL569075 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL571308 | — | Ki | = | 686.0 | nM | 6.16 |