Assay Detail
Binding
CHEMBL5377680
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at sigma1 receptor (unknown origin)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A Novel Bifunctional μOR Agonist and σ<sub>1</sub>R Antagonist with Potent Analgesic Responses and Reduced Adverse Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.07 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5179132 | — | — | 1 | 7.44 |
| CHEMBL4439908 | — | — | 1 | 7.24 |
| CHEMBL4461774 | — | — | 1 | 7.24 |
| CHEMBL5086571 | — | — | 1 | 6.97 |
| CHEMBL4781352 | — | — | 1 | 6.93 |
| CHEMBL172155 | — | — | 1 | 6.62 |
| CHEMBL5287561 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5179132 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4439908 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4461774 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL5086571 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL4781352 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL172155 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL5287561 | — | Ki | < | 100.0 | nM | - |