Assay Detail
Binding
CHEMBL4432466
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Inhibition of VMAT2 in rat striatal homogenate assessed as reduction in [3H]DA uptake after 8 mins by liquid scintillation spectrometric analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Synaptic vesicular amine transporter (CHEMBL4828) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and in vitro evaluation of water-soluble 1,4-diphenethylpiperazine analogs as novel inhibitors of the vesicular monoamine transporter-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.12 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4443407 | — | — | 1 | 7.46 |
| CHEMBL4519939 | — | — | 1 | 7.43 |
| CHEMBL4442303 | — | — | 1 | 7.32 |
| CHEMBL4518586 | — | — | 1 | 7.24 |
| CHEMBL4531091 | — | — | 1 | 7.22 |
| CHEMBL4444122 | — | — | 1 | 7.20 |
| CHEMBL4444692 | — | — | 1 | 7.06 |
| CHEMBL4452875 | — | — | 1 | 7.01 |
| CHEMBL4532351 | — | — | 1 | 7.00 |
| CHEMBL4473454 | — | — | 1 | 6.96 |
| CHEMBL4444796 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4443407 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4519939 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL4442303 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL4518586 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL4531091 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4444122 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4444692 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL4452875 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4532351 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4473454 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4444796 | — | Ki | = | 410.0 | nM | 6.39 |