Assay Detail
Binding
CHEMBL922320
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in guinea pig brain membrane
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.21 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL410832 | — | — | 1 | 9.30 |
| CHEMBL406018 | — | — | 1 | 8.96 |
| CHEMBL138809 | — | — | 1 | 8.94 |
| CHEMBL259732 | — | — | 1 | 8.89 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.72 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 6.75 |
| CHEMBL259941 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL410832 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL406018 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL138809 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL259732 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 177.3 | nM | 6.75 |
| CHEMBL259941 | — | Ki | = | 1200.0 | nM | 5.92 |