Assay Detail
Binding
CHEMBL4202146
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VMAT2 in C57Bl/6J mouse striatal membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 8 mins
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Synaptic vesicular amine transporter (CHEMBL4295886) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.56 | 8.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL772 | RESERPINE | 4.0 | 1 | 8.75 |
| CHEMBL4205254 | — | — | 2 | 8.47 |
| CHEMBL4202787 | — | — | 1 | 8.46 |
| CHEMBL4207658 | — | — | 1 | 8.04 |
| CHEMBL4208779 | — | — | 1 | 7.89 |
| CHEMBL4206824 | — | — | 1 | 7.70 |
| CHEMBL4214975 | — | — | 1 | 7.61 |
| CHEMBL4208250 | — | — | 1 | 7.50 |
| CHEMBL213814 | — | — | 1 | 7.30 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 7.01 |
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 7.00 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 6.42 |
| CHEMBL508 | — | — | 1 | 5.56 |
| CHEMBL4203894 | — | — | 1 | - |
| CHEMBL4216117 | — | — | 1 | - |
| CHEMBL4204449 | — | — | 1 | - |
| CHEMBL4212633 | — | — | 1 | - |
| CHEMBL4217581 | — | — | 1 | - |
| CHEMBL4213176 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL772 | RESERPINE | IC50 | = | 1.79 | nM | 8.75 |
| CHEMBL4205254 | — | IC50 | = | 3.39 | nM | 8.47 |
| CHEMBL4202787 | — | IC50 | = | 3.46 | nM | 8.46 |
| CHEMBL4205254 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4207658 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4208779 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL4206824 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL4214975 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL4208250 | — | IC50 | = | 31.5 | nM | 7.50 |
| CHEMBL213814 | — | IC50 | = | 49.56 | nM | 7.30 |
| CHEMBL39 | SEROTONIN | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL51 | KETANSERIN | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL122270 | LOBELINE | IC50 | = | 381.0 | nM | 6.42 |
| CHEMBL508 | — | IC50 | = | 2740.0 | nM | 5.56 |
| CHEMBL4203894 | — | IC50 | - | — | - | |
| CHEMBL4216117 | — | IC50 | - | — | - | |
| CHEMBL4204449 | — | IC50 | - | — | - | |
| CHEMBL4212633 | — | IC50 | - | — | - | |
| CHEMBL4217581 | — | IC50 | - | — | - | |
| CHEMBL4213176 | — | IC50 | - | — | - |