Assay Detail
Binding
CHEMBL4685220
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method
15
Total Activities
15
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
Negative allosteric modulators of the GluN2B NMDA receptor with phenylethylamine structure embedded in ring-expanded and ring-contracted scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.34 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740593 | — | — | 1 | 8.68 |
| CHEMBL4746028 | — | — | 1 | 8.54 |
| CHEMBL4745685 | — | — | 1 | 7.60 |
| CHEMBL4758763 | — | — | 1 | 7.55 |
| CHEMBL25858 | — | — | 1 | 7.54 |
| CHEMBL55317 | — | — | 1 | 7.42 |
| CHEMBL4778291 | — | — | 1 | 7.30 |
| CHEMBL4759924 | — | — | 1 | 7.30 |
| CHEMBL4744736 | — | — | 1 | 7.19 |
| CHEMBL4745317 | — | — | 1 | 7.16 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 7.01 |
| CHEMBL4800530 | — | — | 1 | 6.82 |
| CHEMBL4754021 | — | — | 1 | 6.75 |
| CHEMBL4759856 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740593 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4746028 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4745685 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4758763 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL25858 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL55317 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4778291 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4759924 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4744736 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL4745317 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4800530 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4754021 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL4759856 | — | Ki | = | 694.0 | nM | 6.16 |