Assay Detail
Binding
CHEMBL804965
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Compound was evaluated for binding affinity towards sigma opioid receptor using [3H](+)-3-PPP in guinea pig ileum
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.39 | 7.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60547 | — | — | 1 | 7.09 |
| CHEMBL301867 | — | — | 1 | 6.66 |
| CHEMBL58033 | (-)-U-50488 | — | 1 | 6.23 |
| CHEMBL290543 | — | — | 2 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60547 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL301867 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL58033 | (-)-U-50488 | Ki | = | 594.0 | nM | 6.23 |
| CHEMBL290543 | — | Ki | = | 874.0 | nM | 6.06 |
| CHEMBL290543 | — | Ki | = | 1270.0 | nM | 5.90 |