Assay Detail
Binding
CHEMBL4372796
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 120 mins by scintillation counting method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.81 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.27 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.18 |
| CHEMBL4561040 | — | — | 1 | 6.06 |
| CHEMBL4438714 | — | — | 1 | 5.80 |
| CHEMBL4582146 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL100116 | PENTAZOCINE | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL4561040 | — | Ki | = | 876.0 | nM | 6.06 |
| CHEMBL4438714 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4582146 | — | Ki | = | 1800.0 | nM | 5.75 |