Assay Detail
Binding
CHEMBL4829577
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Inhibition of [3H]DTBZ binding to VMAT2 in rat brain incubated for 30 mins by liquid scintillation spectrometry analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Synaptic vesicular amine transporter (CHEMBL4828) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.47 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874676 | — | — | 1 | 8.31 |
| CHEMBL4854730 | — | — | 1 | 8.29 |
| CHEMBL4859304 | — | — | 1 | 8.22 |
| CHEMBL4873900 | — | — | 1 | 8.10 |
| CHEMBL4871801 | — | — | 1 | 7.90 |
| CHEMBL4874168 | — | — | 1 | 7.89 |
| CHEMBL576222 | DIHYDROTETRABENAZINE | -1.0 | 1 | 7.83 |
| CHEMBL4878776 | — | — | 1 | 7.67 |
| CHEMBL4875286 | — | — | 1 | 7.25 |
| CHEMBL4867332 | — | — | 1 | 7.24 |
| CHEMBL117785 | TETRABENAZINE | 4.0 | 1 | 7.15 |
| CHEMBL4862715 | — | — | 1 | 7.14 |
| CHEMBL4860699 | — | — | 1 | 7.06 |
| CHEMBL567232 | — | — | 1 | 6.99 |
| CHEMBL4869605 | — | — | 1 | 6.70 |
| CHEMBL4857619 | — | — | 1 | 6.68 |
| CHEMBL4864621 | — | — | 1 | 6.55 |
| CHEMBL4871559 | — | — | 1 | - |
| CHEMBL4849938 | — | — | 1 | - |
| CHEMBL4849901 | — | — | 1 | - |
| CHEMBL4877457 | — | — | 1 | - |
| CHEMBL4856324 | — | — | 1 | - |
| CHEMBL4867056 | — | — | 1 | - |
| CHEMBL213814 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874676 | — | IC50 | = | 4.91 | nM | 8.31 |
| CHEMBL4854730 | — | IC50 | = | 5.13 | nM | 8.29 |
| CHEMBL4859304 | — | IC50 | = | 5.99 | nM | 8.22 |
| CHEMBL4873900 | — | IC50 | = | 8.02 | nM | 8.10 |
| CHEMBL4871801 | — | IC50 | = | 12.51 | nM | 7.90 |
| CHEMBL4874168 | — | IC50 | = | 12.91 | nM | 7.89 |
| CHEMBL576222 | DIHYDROTETRABENAZINE | IC50 | = | 14.74 | nM | 7.83 |
| CHEMBL4878776 | — | IC50 | = | 21.45 | nM | 7.67 |
| CHEMBL4875286 | — | IC50 | = | 56.58 | nM | 7.25 |
| CHEMBL4867332 | — | IC50 | = | 58.15 | nM | 7.24 |
| CHEMBL117785 | TETRABENAZINE | IC50 | = | 70.22 | nM | 7.15 |
| CHEMBL4862715 | — | IC50 | = | 73.18 | nM | 7.14 |
| CHEMBL4860699 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL567232 | — | IC50 | = | 102.45 | nM | 6.99 |
| CHEMBL4869605 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4857619 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4864621 | — | IC50 | = | 280.34 | nM | 6.55 |
| CHEMBL4871559 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4849938 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4849901 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4877457 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4856324 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4867056 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL213814 | — | IC50 | > | 500.0 | nM | - |