Assay Detail
Binding
CHEMBL1676914
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
17
Total Activities
17
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
Analogues of σ receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with added polar functionality and reduced lipophilicity for potential use as positron emission tomography radiotracers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.25 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419822 | — | — | 1 | 9.89 |
| CHEMBL53325 | — | — | 1 | 9.42 |
| CHEMBL73854 | — | — | 1 | 9.20 |
| CHEMBL1672038 | — | — | 1 | 8.66 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.52 |
| CHEMBL1672039 | — | — | 1 | 8.49 |
| CHEMBL1672037 | — | — | 1 | 8.41 |
| CHEMBL1672036 | — | — | 1 | 8.38 |
| CHEMBL1672042 | — | — | 1 | 8.26 |
| CHEMBL1672040 | — | — | 1 | 7.90 |
| CHEMBL1672030 | — | — | 1 | 7.90 |
| CHEMBL1672034 | — | — | 1 | 7.87 |
| CHEMBL1672031 | — | — | 1 | 7.69 |
| CHEMBL1672035 | — | — | 1 | 7.63 |
| CHEMBL1672033 | — | — | 1 | 7.62 |
| CHEMBL1672041 | — | — | 1 | 7.37 |
| CHEMBL1672032 | — | — | 1 | 7.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419822 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL53325 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL73854 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL1672038 | — | Ki | = | 2.17 | nM | 8.66 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1672039 | — | Ki | = | 3.24 | nM | 8.49 |
| CHEMBL1672037 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1672036 | — | Ki | = | 4.17 | nM | 8.38 |
| CHEMBL1672042 | — | Ki | = | 5.44 | nM | 8.26 |
| CHEMBL1672040 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL1672030 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL1672034 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL1672031 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL1672035 | — | Ki | = | 23.3 | nM | 7.63 |
| CHEMBL1672033 | — | Ki | = | 23.9 | nM | 7.62 |
| CHEMBL1672041 | — | Ki | = | 42.6 | nM | 7.37 |
| CHEMBL1672032 | — | Ki | = | 94.6 | nM | 7.02 |