Assay Detail
Binding
CHEMBL4202144
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-syn-Ethyl 1-(2-(2,4-Dioxo-1,2-dihydroquinazolin-3(4H)-yl)ethyl)-4-(4-fluorophenyl)piperidine-3-carboxylate from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
20
Total Activities
19
Compounds Tested
2
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 |
|---|---|---|---|
| Ki | 19 | 5.99 | 6.79 |
| Kd | 1 | 7.03 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4205254 | — | — | 2 | 7.03 |
| CHEMBL4202787 | — | — | 1 | 6.79 |
| CHEMBL4207658 | — | — | 1 | 6.54 |
| CHEMBL4208779 | — | — | 1 | 6.46 |
| CHEMBL772 | RESERPINE | 4.0 | 1 | 6.39 |
| CHEMBL4216117 | — | — | 1 | 6.34 |
| CHEMBL4213176 | — | — | 1 | 6.16 |
| CHEMBL4203894 | — | — | 1 | 6.14 |
| CHEMBL4208250 | — | — | 1 | 6.05 |
| CHEMBL4214975 | — | — | 1 | 5.94 |
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 5.92 |
| CHEMBL4217581 | — | — | 1 | 5.78 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 5.71 |
| CHEMBL213814 | — | — | 1 | 5.71 |
| CHEMBL4204449 | — | — | 1 | 5.71 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 5.64 |
| CHEMBL4212633 | — | — | 1 | 5.42 |
| CHEMBL508 | — | — | 1 | 4.61 |
| CHEMBL4206824 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4205254 | — | Kd | = | 93.0 | nM | 7.03 |
| CHEMBL4202787 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL4205254 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL4207658 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL4208779 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL772 | RESERPINE | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL4216117 | — | Ki | = | 452.0 | nM | 6.34 |
| CHEMBL4213176 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL4203894 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL4208250 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL4214975 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL51 | KETANSERIN | Ki | = | 1190.0 | nM | 5.92 |
| CHEMBL4217581 | — | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL122270 | LOBELINE | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL213814 | — | Ki | = | 1932.0 | nM | 5.71 |
| CHEMBL4204449 | — | Ki | = | 1960.0 | nM | 5.71 |
| CHEMBL39 | SEROTONIN | Ki | = | 2290.0 | nM | 5.64 |
| CHEMBL4212633 | — | Ki | = | 3770.0 | nM | 5.42 |
| CHEMBL508 | — | Ki | = | 24500.0 | nM | 4.61 |
| CHEMBL4206824 | — | Ki | > | 10000.0 | nM | - |