Assay Detail
Binding
CHEMBL5383553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]di-o-tolylguanidine from rat liver membrane sigma 2 receptor assessed as inhibition constant measured after 120 mins by scintillation counting method
22
Total Activities
22
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
Conformationally Restricted σ<sub>1</sub> Receptor Antagonists from (-)-Isopulegol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.65 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL493054 | — | — | 1 | 8.24 |
| CHEMBL5413704 | — | — | 1 | 7.44 |
| CHEMBL5435693 | — | — | 1 | 7.12 |
| CHEMBL5418583 | — | — | 1 | 7.07 |
| CHEMBL5415339 | — | — | 1 | 6.92 |
| CHEMBL5419345 | — | — | 1 | 6.91 |
| CHEMBL5421431 | — | — | 1 | 6.84 |
| CHEMBL5408176 | — | — | 1 | 6.76 |
| CHEMBL5430693 | — | — | 1 | 6.71 |
| CHEMBL5438476 | — | — | 1 | 6.68 |
| CHEMBL5440135 | — | — | 1 | 6.67 |
| CHEMBL5395928 | — | — | 1 | 6.58 |
| CHEMBL5419171 | — | — | 1 | 6.56 |
| CHEMBL5439989 | — | — | 1 | 6.49 |
| CHEMBL5394456 | — | — | 1 | 6.42 |
| CHEMBL5419756 | — | — | 1 | 6.37 |
| CHEMBL5427418 | — | — | 1 | 6.28 |
| CHEMBL5402137 | — | — | 1 | 6.19 |
| CHEMBL5420805 | — | — | 1 | 6.11 |
| CHEMBL5436332 | — | — | 1 | 6.07 |
| CHEMBL5409031 | — | — | 1 | 6.06 |
| CHEMBL5394807 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL493054 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL5413704 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL5435693 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL5418583 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL5415339 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL5419345 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL5421431 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL5408176 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL5430693 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL5438476 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL5440135 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL5395928 | — | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL5419171 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL5439989 | — | Ki | = | 322.0 | nM | 6.49 |
| CHEMBL5394456 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL5419756 | — | Ki | = | 424.0 | nM | 6.37 |
| CHEMBL5427418 | — | Ki | = | 525.0 | nM | 6.28 |
| CHEMBL5402137 | — | Ki | = | 649.0 | nM | 6.19 |
| CHEMBL5420805 | — | Ki | = | 779.0 | nM | 6.11 |
| CHEMBL5436332 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL5409031 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL5394807 | — | Ki | = | 1600.0 | nM | 5.80 |