Assay Detail
Binding
CHEMBL4182982
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 after 120 mins by scintillation counting analysis
9
Total Activities
9
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
2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.94 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL4218465 | — | — | 1 | 7.22 |
| CHEMBL3753409 | — | — | 1 | 7.12 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 7.01 |
| CHEMBL4204621 | — | — | 1 | 6.90 |
| CHEMBL4206913 | — | — | 1 | 6.83 |
| CHEMBL4205955 | — | — | 1 | 6.05 |
| CHEMBL1289626 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL4218465 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL3753409 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4204621 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL4206913 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL4205955 | — | Ki | = | 894.0 | nM | 6.05 |
| CHEMBL1289626 | — | Ki | > | 10000.0 | nM | - |