Assay Detail
Binding
CHEMBL4615565
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
16
Total Activities
16
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
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.63 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4643805 | — | — | 1 | 7.55 |
| CHEMBL4640137 | — | — | 1 | 7.46 |
| CHEMBL4639180 | — | — | 1 | 7.33 |
| CHEMBL4633788 | — | — | 1 | 7.33 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 7.01 |
| CHEMBL4644807 | — | — | 1 | 6.99 |
| CHEMBL4640809 | — | — | 1 | 6.73 |
| CHEMBL4638673 | — | — | 1 | 6.53 |
| CHEMBL4636240 | — | — | 1 | 6.30 |
| CHEMBL4636929 | — | — | 1 | 6.25 |
| CHEMBL4636805 | — | — | 1 | 5.75 |
| CHEMBL4643145 | — | — | 1 | 5.70 |
| CHEMBL4638934 | — | — | 1 | 5.41 |
| CHEMBL4636728 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4643805 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4640137 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4639180 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL4633788 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4644807 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL4640809 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL4638673 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL4636240 | — | Ki | = | 495.0 | nM | 6.30 |
| CHEMBL4636929 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL4636805 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL4643145 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL4638934 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL4636728 | — | Ki | = | 3900.0 | nM | 5.41 |