Assay Detail
Binding
CHEMBL4137785
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DTG from sigma2 receptor in rat liver 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 |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| 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 | 7.18 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1229211 | DOLUTEGRAVIR | 4.0 | 1 | 7.50 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.36 |
| CHEMBL1929421 | — | — | 1 | 7.30 |
| CHEMBL408867 | [11C]SA4503 | — | 1 | 7.21 |
| CHEMBL20943 | — | — | 1 | 7.20 |
| CHEMBL4173258 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1229211 | DOLUTEGRAVIR | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 43.9 | nM | 7.36 |
| CHEMBL1929421 | — | Ki | = | 50.3 | nM | 7.30 |
| CHEMBL408867 | [11C]SA4503 | Ki | = | 62.2 | nM | 7.21 |
| CHEMBL20943 | — | Ki | = | 63.4 | nM | 7.20 |
| CHEMBL4173258 | — | Ki | = | 326.0 | nM | 6.49 |