Assay Detail
Binding
CHEMBL4202145
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human VMAT2 expressed in HEK293 cell membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 6 mins
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Synaptic vesicular amine transporter (CHEMBL1893) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.67 | 7.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL772 | RESERPINE | 4.0 | 1 | 7.88 |
| CHEMBL4205254 | — | — | 2 | 7.80 |
| CHEMBL4207658 | — | — | 1 | 7.71 |
| CHEMBL4206824 | — | — | 1 | 7.55 |
| CHEMBL4202787 | — | — | 1 | 7.41 |
| CHEMBL4214975 | — | — | 1 | 7.07 |
| CHEMBL4208250 | — | — | 1 | 7.00 |
| CHEMBL4208779 | — | — | 1 | 6.90 |
| CHEMBL4213176 | — | — | 1 | 6.85 |
| CHEMBL213814 | — | — | 1 | 6.81 |
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 6.75 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 5.84 |
| CHEMBL4216117 | — | — | 1 | 5.57 |
| CHEMBL4203894 | — | — | 1 | 5.54 |
| CHEMBL508 | — | — | 1 | 5.44 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 5.38 |
| CHEMBL4204449 | — | — | 1 | 5.24 |
| CHEMBL4212633 | — | — | 1 | - |
| CHEMBL4217581 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL772 | RESERPINE | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4205254 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4207658 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL4206824 | — | IC50 | = | 28.1 | nM | 7.55 |
| CHEMBL4202787 | — | IC50 | = | 39.4 | nM | 7.41 |
| CHEMBL4205254 | — | IC50 | = | 51.1 | nM | 7.29 |
| CHEMBL4214975 | — | IC50 | = | 85.5 | nM | 7.07 |
| CHEMBL4208250 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4208779 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4213176 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL213814 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL51 | KETANSERIN | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL39 | SEROTONIN | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL4216117 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4203894 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL508 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL122270 | LOBELINE | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4204449 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4212633 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4217581 | — | IC50 | > | 10000.0 | nM | - |