Assay Detail
Binding
CHEMBL4329317
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel multitarget-directed ligands targeting acetylcholinesterase and σ<sub>1</sub> receptors as lead compounds for treatment of Alzheimer's disease: Synthesis, evaluation, and structural characterization of their complexes with acetylcholinesterase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.23 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.80 |
| CHEMBL4585990 | — | — | 1 | 8.48 |
| CHEMBL4537101 | — | — | 1 | 8.29 |
| CHEMBL4444843 | — | — | 1 | 8.29 |
| CHEMBL4526050 | — | — | 1 | 8.24 |
| CHEMBL3417009 | — | — | 1 | 7.29 |
| CHEMBL85251 | — | — | 1 | - |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | - |
| CHEMBL4540355 | — | — | 1 | - |
| CHEMBL4562793 | — | — | 1 | - |
| CHEMBL4567394 | — | — | 1 | - |
| CHEMBL4454706 | — | — | 1 | - |
| CHEMBL4559904 | — | — | 1 | - |
| CHEMBL4541090 | — | — | 1 | - |
| CHEMBL4583738 | — | — | 1 | - |
| CHEMBL4578844 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4585990 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4537101 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL4444843 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL4526050 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL3417009 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL85251 | — | Ki | - | — | - | |
| CHEMBL502 | DONEPEZIL | Ki | - | — | - | |
| CHEMBL4540355 | — | Ki | - | — | - | |
| CHEMBL4562793 | — | Ki | - | — | - | |
| CHEMBL4567394 | — | Ki | - | — | - | |
| CHEMBL4454706 | — | Ki | - | — | - | |
| CHEMBL4559904 | — | Ki | - | — | - | |
| CHEMBL4541090 | — | Ki | - | — | - | |
| CHEMBL4583738 | — | Ki | - | — | - | |
| CHEMBL4578844 | — | Ki | - | — | - |