Assay Detail
Binding
CHEMBL4137784
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes after 60 mins by liquid scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| 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 | 4 | 7.59 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.27 |
| CHEMBL408867 | [11C]SA4503 | — | 1 | 7.87 |
| CHEMBL20943 | — | — | 1 | 7.56 |
| CHEMBL1229211 | DOLUTEGRAVIR | 4.0 | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 5.39 | nM | 8.27 |
| CHEMBL408867 | [11C]SA4503 | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL20943 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL1229211 | DOLUTEGRAVIR | Ki | = | 217.0 | nM | 6.66 |