Assay Detail
Binding
CHEMBL807586
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In vitro binding affinity at opioid sigma-2 receptor in rat liver membranes by [3H]-DTG displacement in the presence of 1 uM (+)-pentazocine.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
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 | 20 | 8.35 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53325 | — | — | 1 | 9.47 |
| CHEMBL306365 | — | — | 1 | 9.46 |
| CHEMBL75372 | — | — | 1 | 9.24 |
| CHEMBL75608 | — | — | 1 | 9.17 |
| CHEMBL75480 | — | — | 1 | 9.16 |
| CHEMBL73964 | — | — | 1 | 8.95 |
| CHEMBL75444 | — | — | 1 | 8.91 |
| CHEMBL73854 | — | — | 1 | 8.68 |
| CHEMBL74723 | — | — | 1 | 8.57 |
| CHEMBL77220 | — | — | 1 | 8.45 |
| CHEMBL77906 | — | — | 1 | 8.27 |
| CHEMBL74080 | — | — | 1 | 8.11 |
| CHEMBL419822 | — | — | 1 | 8.06 |
| CHEMBL75286 | — | — | 1 | 8.03 |
| CHEMBL76758 | — | — | 1 | 7.84 |
| CHEMBL75878 | — | — | 1 | 7.79 |
| CHEMBL74858 | — | — | 1 | 7.68 |
| CHEMBL306133 | — | — | 1 | 7.52 |
| CHEMBL74811 | — | — | 1 | 6.99 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53325 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL306365 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL75372 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL75608 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL75480 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL73964 | — | Ki | = | 1.12 | nM | 8.95 |
| CHEMBL75444 | — | Ki | = | 1.22 | nM | 8.91 |
| CHEMBL73854 | — | Ki | = | 2.09 | nM | 8.68 |
| CHEMBL74723 | — | Ki | = | 2.66 | nM | 8.57 |
| CHEMBL77220 | — | Ki | = | 3.58 | nM | 8.45 |
| CHEMBL77906 | — | Ki | = | 5.42 | nM | 8.27 |
| CHEMBL74080 | — | Ki | = | 7.85 | nM | 8.11 |
| CHEMBL419822 | — | Ki | = | 8.65 | nM | 8.06 |
| CHEMBL75286 | — | Ki | = | 9.24 | nM | 8.03 |
| CHEMBL76758 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL75878 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL74858 | — | Ki | = | 21.1 | nM | 7.68 |
| CHEMBL306133 | — | Ki | = | 30.5 | nM | 7.52 |
| CHEMBL74811 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL75228 | 1-PHENETHYLPIPERIDINE | Ki | = | 194.0 | nM | 6.71 |