Assay Detail
Binding
CHEMBL5251999
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DTG from sigma 2 receptor in Wistar Han rat liver membrane assessed as inhibition constant incubated for 120 mins
11
Total Activities
11
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
Development of Fluorescent 4-[4-(3<i>H</i>-Spiro[isobenzofuran-1,4'-piperidin]-1'-yl)butyl]indolyl Derivatives as High-Affinity Probes to Enable the Study of σ Receptors via Fluorescence-Based Techniques.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.82 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5271751 | — | — | 1 | 9.37 |
| CHEMBL5274668 | — | — | 1 | 8.42 |
| CHEMBL5284531 | — | — | 1 | 8.29 |
| CHEMBL5280109 | — | — | 1 | 8.00 |
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 7.90 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.71 |
| CHEMBL5290452 | — | — | 1 | 7.52 |
| CHEMBL5286943 | — | — | 1 | 7.41 |
| CHEMBL5281223 | — | — | 1 | 7.40 |
| CHEMBL5278003 | — | — | 1 | 7.29 |
| CHEMBL5278417 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5271751 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL5274668 | — | Ki | = | 3.84 | nM | 8.42 |
| CHEMBL5284531 | — | Ki | = | 5.07 | nM | 8.29 |
| CHEMBL5280109 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL61479 | SIRAMESINE | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL5290452 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL5286943 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL5281223 | — | Ki | = | 39.8 | nM | 7.40 |
| CHEMBL5278003 | — | Ki | = | 51.1 | nM | 7.29 |
| CHEMBL5278417 | — | Ki | = | 220.0 | nM | 6.66 |