Assay Detail
Binding
CHEMBL4307198
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes in the presence of sigma1 receptor ligand (+)-pentazocine incubated for 120 mins by scintillation counting method
17
Total Activities
17
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
Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.12 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4581662 | — | — | 1 | 8.82 |
| CHEMBL4446466 | — | — | 1 | 7.80 |
| CHEMBL4449269 | — | — | 1 | 7.68 |
| CHEMBL4446431 | — | — | 1 | 7.68 |
| CHEMBL4533030 | — | — | 1 | 7.50 |
| CHEMBL4459690 | — | — | 1 | 7.47 |
| CHEMBL4439170 | — | — | 1 | 7.35 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL4453315 | — | — | 1 | 7.14 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL4463741 | — | — | 1 | 7.10 |
| CHEMBL4451677 | — | — | 1 | 7.03 |
| CHEMBL4445874 | — | — | 1 | 7.01 |
| CHEMBL4454333 | — | — | 1 | 6.42 |
| CHEMBL4567801 | — | — | 1 | 6.16 |
| CHEMBL4446009 | — | — | 1 | 6.06 |
| CHEMBL4442750 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4581662 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4446466 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4449269 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4446431 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4533030 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4459690 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4439170 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4453315 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4463741 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL4451677 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL4445874 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4454333 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL4567801 | — | Ki | = | 686.0 | nM | 6.16 |
| CHEMBL4446009 | — | Ki | = | 864.0 | nM | 6.06 |
| CHEMBL4442750 | — | Ki | = | 2800.0 | nM | 5.55 |