Assay Detail
Binding
CHEMBL809832
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]pentazocine binding to Sigma opioid receptor type 1
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
An aromatic moiety is not essential for pharmacophore binding to sigma binding sites: Synthesis of N-alkylazacycloheptane derivatives as potent sigma ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.53 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.36 |
| CHEMBL308816 | — | — | 1 | 8.97 |
| CHEMBL74803 | — | — | 1 | 8.92 |
| CHEMBL424606 | — | — | 1 | 8.88 |
| CHEMBL77812 | — | — | 1 | 8.87 |
| CHEMBL73633 | — | — | 1 | 8.78 |
| CHEMBL75555 | — | — | 1 | 8.66 |
| CHEMBL306318 | — | — | 1 | 8.60 |
| CHEMBL77817 | — | — | 1 | 8.54 |
| CHEMBL307839 | — | — | 1 | 8.54 |
| CHEMBL74499 | — | — | 1 | 8.52 |
| CHEMBL73818 | — | — | 1 | 8.37 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.56 |
| CHEMBL101510 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL308816 | — | Ki | = | 1.08 | nM | 8.97 |
| CHEMBL74803 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL424606 | — | Ki | = | 1.33 | nM | 8.88 |
| CHEMBL77812 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL73633 | — | Ki | = | 1.67 | nM | 8.78 |
| CHEMBL75555 | — | Ki | = | 2.17 | nM | 8.66 |
| CHEMBL306318 | — | Ki | = | 2.53 | nM | 8.60 |
| CHEMBL77817 | — | Ki | = | 2.87 | nM | 8.54 |
| CHEMBL307839 | — | Ki | = | 2.87 | nM | 8.54 |
| CHEMBL74499 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL73818 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL101510 | — | Ki | = | 157.0 | nM | 6.80 |