Assay Detail
Binding
CHEMBL4137786
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vesicular acetylcholine transporter (CHEMBL2125) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.88 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1929421 | — | — | 1 | 8.59 |
| CHEMBL4173258 | — | — | 1 | 7.33 |
| CHEMBL20943 | — | — | 1 | 7.31 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.41 |
| CHEMBL408867 | [11C]SA4503 | — | 1 | 6.31 |
| CHEMBL1229211 | DOLUTEGRAVIR | 4.0 | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1929421 | — | Ki | = | 2.58 | nM | 8.59 |
| CHEMBL4173258 | — | Ki | = | 46.3 | nM | 7.33 |
| CHEMBL20943 | — | Ki | = | 48.6 | nM | 7.31 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL408867 | [11C]SA4503 | Ki | = | 492.0 | nM | 6.31 |
| CHEMBL1229211 | DOLUTEGRAVIR | Ki | = | 4523.0 | nM | 5.34 |