Assay Detail
Binding
CHEMBL802050
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity at opioid sigma-1 receptor in guinea pig brain membranes by (+)-[3H]pentazocine displacement.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 8.76 | 10.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL76758 | — | — | 1 | 10.44 |
| CHEMBL306133 | — | — | 1 | 9.66 |
| CHEMBL75878 | — | — | 1 | 9.51 |
| CHEMBL77906 | — | — | 1 | 9.44 |
| CHEMBL309064 | — | — | 1 | 9.40 |
| CHEMBL75608 | — | — | 1 | 9.21 |
| CHEMBL73964 | — | — | 1 | 9.16 |
| CHEMBL74080 | — | — | 1 | 8.84 |
| CHEMBL306365 | — | — | 1 | 8.82 |
| CHEMBL77220 | — | — | 1 | 8.81 |
| CHEMBL75286 | — | — | 1 | 8.80 |
| CHEMBL74858 | — | — | 1 | 8.80 |
| CHEMBL75480 | — | — | 1 | 8.67 |
| CHEMBL75372 | — | — | 1 | 8.62 |
| CHEMBL419822 | — | — | 1 | 8.61 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.52 |
| CHEMBL74811 | — | — | 1 | 8.51 |
| CHEMBL74723 | — | — | 1 | 8.27 |
| CHEMBL73854 | — | — | 1 | 8.26 |
| CHEMBL75444 | — | — | 1 | 8.04 |
| CHEMBL53325 | — | — | 1 | 7.87 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL76758 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL306133 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL75878 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL77906 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL309064 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL75608 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL73964 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL74080 | — | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL306365 | — | Ki | = | 1.52 | nM | 8.82 |
| CHEMBL77220 | — | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL75286 | — | Ki | = | 1.57 | nM | 8.80 |
| CHEMBL74858 | — | Ki | = | 1.57 | nM | 8.80 |
| CHEMBL75480 | — | Ki | = | 2.16 | nM | 8.67 |
| CHEMBL75372 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL419822 | — | Ki | = | 2.45 | nM | 8.61 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 3.05 | nM | 8.52 |
| CHEMBL74811 | — | Ki | = | 3.07 | nM | 8.51 |
| CHEMBL74723 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL73854 | — | Ki | = | 5.54 | nM | 8.26 |
| CHEMBL75444 | — | Ki | = | 9.04 | nM | 8.04 |
| CHEMBL53325 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | Ki | = | 309.0 | nM | 6.51 |