Assay Detail
Binding
CHEMBL4202136
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]reserpine from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
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 |
|---|---|---|---|
| Ki | 20 | 6.55 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL772 | RESERPINE | 4.0 | 1 | 8.28 |
| CHEMBL4205254 | — | — | 2 | 7.21 |
| CHEMBL4207658 | — | — | 1 | 7.16 |
| CHEMBL4202787 | — | — | 1 | 7.13 |
| CHEMBL213814 | — | — | 1 | 7.08 |
| CHEMBL4206824 | — | — | 1 | 6.82 |
| CHEMBL4214975 | — | — | 1 | 6.75 |
| CHEMBL51 | KETANSERIN | 3.0 | 1 | 6.45 |
| CHEMBL4208250 | — | — | 1 | 6.35 |
| CHEMBL4213176 | — | — | 1 | 6.19 |
| CHEMBL4208779 | — | — | 1 | 6.00 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 5.74 |
| CHEMBL508 | — | — | 1 | 5.19 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 5.11 |
| CHEMBL4203894 | — | — | 1 | - |
| CHEMBL4216117 | — | — | 1 | - |
| CHEMBL4204449 | — | — | 1 | - |
| CHEMBL4212633 | — | — | 1 | - |
| CHEMBL4217581 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL772 | RESERPINE | Ki | = | 5.26 | nM | 8.28 |
| CHEMBL4205254 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4207658 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4202787 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL213814 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL4206824 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL4214975 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL4205254 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL51 | KETANSERIN | Ki | = | 353.0 | nM | 6.45 |
| CHEMBL4208250 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL4213176 | — | Ki | = | 652.0 | nM | 6.19 |
| CHEMBL4208779 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL122270 | LOBELINE | Ki | = | 1840.0 | nM | 5.74 |
| CHEMBL508 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL39 | SEROTONIN | Ki | = | 7690.0 | nM | 5.11 |
| CHEMBL4203894 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4216117 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4204449 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4212633 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4217581 | — | Ki | > | 10000.0 | nM | - |