Assay Detail
Binding
CHEMBL5251998
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane assessed as inhibition constant incubated for 120 mins
12
Total Activities
12
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
Development of Fluorescent 4-[4-(3<i>H</i>-Spiro[isobenzofuran-1,4'-piperidin]-1'-yl)butyl]indolyl Derivatives as High-Affinity Probes to Enable the Study of σ Receptors via Fluorescence-Based Techniques.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.15 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.51 |
| CHEMBL61479 | SIRAMESINE | 2.0 | 1 | 7.98 |
| CHEMBL5271751 | — | — | 1 | 7.56 |
| CHEMBL5274668 | — | — | 1 | 7.42 |
| CHEMBL5280109 | — | — | 1 | 7.41 |
| CHEMBL5290452 | — | — | 1 | 7.29 |
| CHEMBL5281223 | — | — | 1 | 7.05 |
| CHEMBL5284531 | — | — | 1 | 6.53 |
| CHEMBL5278003 | — | — | 1 | 6.35 |
| CHEMBL5278417 | — | — | 1 | 6.33 |
| CHEMBL5286943 | — | — | 1 | 6.25 |
| CHEMBL5272978 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL100116 | PENTAZOCINE | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL61479 | SIRAMESINE | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL5271751 | — | Ki | = | 27.3 | nM | 7.56 |
| CHEMBL5274668 | — | Ki | = | 38.1 | nM | 7.42 |
| CHEMBL5280109 | — | Ki | = | 39.3 | nM | 7.41 |
| CHEMBL5290452 | — | Ki | = | 51.3 | nM | 7.29 |
| CHEMBL5281223 | — | Ki | = | 88.8 | nM | 7.05 |
| CHEMBL5284531 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL5278003 | — | Ki | = | 448.0 | nM | 6.35 |
| CHEMBL5278417 | — | Ki | = | 473.0 | nM | 6.33 |
| CHEMBL5286943 | — | Ki | = | 569.0 | nM | 6.25 |
| CHEMBL5272978 | — | Ki | > | 5000.0 | nM | - |