Assay Detail
Binding
CHEMBL5383552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from guinea pig brain membrane sigma 1 receptor assessed as inhibition constant measured after 120 mins by scintillation counting method
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Conformationally Restricted σ<sub>1</sub> Receptor Antagonists from (-)-Isopulegol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.63 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5408176 | — | — | 1 | 9.00 |
| CHEMBL5413704 | — | — | 1 | 8.92 |
| CHEMBL5394456 | — | — | 1 | 8.80 |
| CHEMBL5430693 | — | — | 1 | 8.55 |
| CHEMBL5435693 | — | — | 1 | 8.54 |
| CHEMBL5419345 | — | — | 1 | 8.46 |
| CHEMBL5421431 | — | — | 1 | 8.31 |
| CHEMBL5415339 | — | — | 1 | 8.30 |
| CHEMBL5419756 | — | — | 1 | 8.15 |
| CHEMBL5436332 | — | — | 1 | 8.09 |
| CHEMBL5427418 | — | — | 1 | 8.07 |
| CHEMBL5439989 | — | — | 1 | 8.01 |
| CHEMBL5402137 | — | — | 1 | 7.80 |
| CHEMBL5440135 | — | — | 1 | 7.75 |
| CHEMBL5438476 | — | — | 1 | 7.51 |
| CHEMBL5419171 | — | — | 1 | 7.38 |
| CHEMBL5395928 | — | — | 1 | 7.37 |
| CHEMBL5420805 | — | — | 1 | 7.27 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL5418583 | — | — | 1 | 7.16 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL493054 | — | — | 1 | 7.01 |
| CHEMBL5409031 | — | — | 1 | 6.94 |
| CHEMBL73824 | — | — | 1 | 6.35 |
| CHEMBL5406602 | — | — | 1 | 6.14 |
| CHEMBL5394807 | — | — | 1 | 6.09 |
| CHEMBL5417526 | — | — | 1 | 5.68 |
| CHEMBL2170062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5408176 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5413704 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL5394456 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL5430693 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL5435693 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL5419345 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL5421431 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL5415339 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5419756 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5436332 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL5427418 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL5439989 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL5402137 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5440135 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL5438476 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL5419171 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL5395928 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL5420805 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL5418583 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL493054 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL5409031 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL73824 | — | Ki | = | 449.0 | nM | 6.35 |
| CHEMBL5406602 | — | Ki | = | 725.0 | nM | 6.14 |
| CHEMBL5394807 | — | Ki | = | 805.0 | nM | 6.09 |
| CHEMBL5417526 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL2170062 | — | Ki | > | 1000.0 | nM | - |