Assay Detail
Binding
CHEMBL4480644
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 measured after 120 mins by scintillation counting analysis
6
Total Activities
6
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
Synthesis and receptor binding of thiophene bioisosteres of potent GluN2B ligands with a benzo[7]annulene-scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.77 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4287203 | — | — | 1 | 8.04 |
| CHEMBL4574247 | — | — | 1 | 7.30 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 7.01 |
| CHEMBL4513837 | — | — | 1 | 6.22 |
| CHEMBL4570472 | — | — | 1 | 6.11 |
| CHEMBL4590193 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4287203 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL4574247 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4513837 | — | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL4570472 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL4590193 | — | Ki | = | 1100.0 | nM | 5.96 |