Assay Detail
Binding
CHEMBL2349698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]pentazocine from sigma 1 receptor in Dunkin guinea pig brain membrane without cerebellum by competition binding assay
13
Total Activities
13
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
Investigation of σ receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.34 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.39 |
| CHEMBL1189823 | — | — | 1 | 8.21 |
| CHEMBL2349069 | — | — | 1 | 8.13 |
| CHEMBL2349072 | — | — | 1 | 8.06 |
| CHEMBL2349068 | — | — | 1 | 7.73 |
| CHEMBL1195399 | — | — | 1 | 7.65 |
| CHEMBL2349070 | — | — | 1 | 7.45 |
| CHEMBL2349066 | — | — | 1 | 7.05 |
| CHEMBL2349073 | — | — | 1 | 6.96 |
| CHEMBL1188789 | — | — | 1 | 6.75 |
| CHEMBL2349067 | — | — | 1 | 6.63 |
| CHEMBL2349071 | — | — | 1 | 6.43 |
| CHEMBL1190213 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL1189823 | — | Ki | = | 6.16 | nM | 8.21 |
| CHEMBL2349069 | — | Ki | = | 7.43 | nM | 8.13 |
| CHEMBL2349072 | — | Ki | = | 8.67 | nM | 8.06 |
| CHEMBL2349068 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL1195399 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL2349070 | — | Ki | = | 35.9 | nM | 7.45 |
| CHEMBL2349066 | — | Ki | = | 88.6 | nM | 7.05 |
| CHEMBL2349073 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1188789 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL2349067 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL2349071 | — | Ki | = | 373.0 | nM | 6.43 |
| CHEMBL1190213 | — | Ki | = | 1060.0 | nM | 5.97 |