Assay Detail
Binding
CHEMBL972418
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane by solid scintillation analysis
9
Total Activities
9
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 of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.66 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL466289 | — | — | 1 | 9.74 |
| CHEMBL511587 | — | — | 1 | 9.10 |
| CHEMBL468929 | — | — | 1 | 9.07 |
| CHEMBL138809 | — | — | 1 | 8.96 |
| CHEMBL468930 | — | — | 1 | 8.85 |
| CHEMBL466096 | — | — | 1 | 8.48 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.41 |
| CHEMBL513470 | — | — | 1 | 8.11 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL466289 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL511587 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL468929 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL138809 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL468930 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL466096 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL513470 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 61.0 | nM | 7.21 |