Assay Detail
Binding
CHEMBL3591145
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DTBZ from VMAT2 in rat whole brain by liquid scintillation spectrometry
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
Quinolyl analogues of norlobelane: novel potent inhibitors of [(3)H]dihydrotetrabenazine binding and [(3)H]dopamine uptake at the vesicular monoamine transporter-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 5.96 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589343 | — | — | 1 | 6.75 |
| CHEMBL3589342 | — | — | 1 | 6.53 |
| CHEMBL3589345 | — | — | 1 | 6.20 |
| CHEMBL3589344 | — | — | 1 | 6.19 |
| CHEMBL333465 | LOBELANE | — | 1 | 6.01 |
| CHEMBL1201201 | METHAMPHETAMINE | 4.0 | 1 | 4.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589343 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL3589342 | — | Ki | = | 293.0 | nM | 6.53 |
| CHEMBL3589345 | — | Ki | = | 627.0 | nM | 6.20 |
| CHEMBL3589344 | — | Ki | = | 647.0 | nM | 6.19 |
| CHEMBL333465 | LOBELANE | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL1201201 | METHAMPHETAMINE | Ki | = | 80100.0 | nM | 4.10 |