Assay Detail
Binding
CHEMBL4349904
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 after 120 mins by scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.68 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3355379 | — | — | 1 | 7.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL4439555 | — | — | 1 | 7.10 |
| CHEMBL113830 | (S,R)-IFENPRODIL | — | 1 | 7.01 |
| CHEMBL4521578 | — | — | 1 | 6.40 |
| CHEMBL4553195 | — | — | 1 | 6.25 |
| CHEMBL4464273 | — | — | 1 | 6.23 |
| CHEMBL4472450 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3355379 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4439555 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL113830 | (S,R)-IFENPRODIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4521578 | — | Ki | = | 397.0 | nM | 6.40 |
| CHEMBL4553195 | — | Ki | = | 562.0 | nM | 6.25 |
| CHEMBL4464273 | — | Ki | = | 593.0 | nM | 6.23 |
| CHEMBL4472450 | — | Ki | = | 878.0 | nM | 6.06 |