Assay Detail
Binding
CHEMBL4274855
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins by 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
Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.86 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4288091 | — | — | 1 | 7.17 |
| CHEMBL4276754 | — | — | 1 | 7.17 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 7.01 |
| CHEMBL4284692 | — | — | 1 | 6.94 |
| CHEMBL4280186 | — | — | 1 | 6.56 |
| CHEMBL4284122 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4288091 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4276754 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4284692 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL4280186 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL4284122 | — | Ki | = | 490.0 | nM | 6.31 |