Assay Detail
Binding
CHEMBL5157900
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 membrane by competitive radioligand receptor binding assay
7
Total Activities
7
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 of tropane-based σ<sub>1</sub> receptor antagonists with antiallodynic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.51 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5187130 | — | — | 1 | 8.00 |
| CHEMBL5175714 | — | — | 1 | 7.96 |
| CHEMBL5186790 | — | — | 1 | 7.57 |
| CHEMBL5185178 | — | — | 1 | 7.54 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL28564 | ELIPRODIL | 2.0 | 1 | 7.15 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5187130 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5175714 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5186790 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL5185178 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL28564 | ELIPRODIL | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |