Assay Detail
Binding
CHEMBL816127
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In vitro inhibition of [3H]- Methoxytetrabenazine binding to rat brain vesicular monoamine transporter 2 (VMAT2)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Synaptic vesicular amine transporter (CHEMBL4828) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
In vitro and in vivo studies of benzisoquinoline ligands for the brain synaptic vesicle monoamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.63 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303770 | — | — | 1 | 8.59 |
| CHEMBL61636 | — | — | 1 | 8.09 |
| CHEMBL62154 | — | — | 1 | 7.92 |
| CHEMBL61363 | — | — | 1 | 7.48 |
| CHEMBL441439 | — | — | 1 | 7.38 |
| CHEMBL59443 | — | — | 1 | 7.08 |
| CHEMBL58121 | — | — | 1 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303770 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL61636 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL62154 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL61363 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL441439 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL59443 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL58121 | — | Ki | = | 136.0 | nM | 6.87 |