Assay Detail
Binding
CHEMBL4254524
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-di-o-tolylguanidine from sigma-2 receptor in rat liver membranes incubated for 120 mins measured for 5 mins by scintillation counting method
7
Total Activities
7
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
Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.95 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4286654 | — | — | 1 | 7.50 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL4284348 | — | — | 1 | 7.02 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 7.01 |
| CHEMBL4287755 | — | — | 1 | 6.57 |
| CHEMBL4294991 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4286654 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4284348 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4287755 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL4294991 | — | Ki | = | 592.0 | nM | 6.23 |