Assay Detail
Binding
CHEMBL4035574
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 membranes after 120 mins by microbeta scintillation counting method
17
Total Activities
17
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
Lipase-catalyzed kinetic resolution as key step in the synthesis of enantiomerically pure σ ligands with 2-benzopyran structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.66 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077148 | — | — | 1 | 9.24 |
| CHEMBL4064375 | — | — | 1 | 8.64 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.41 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.38 |
| CHEMBL1172685 | — | — | 1 | 8.05 |
| CHEMBL1171916 | — | — | 1 | 8.00 |
| CHEMBL1171865 | — | — | 1 | 8.00 |
| CHEMBL1169962 | — | — | 1 | 7.82 |
| CHEMBL4092162 | — | — | 1 | 7.62 |
| CHEMBL4077547 | — | — | 1 | 7.48 |
| CHEMBL3828752 | — | — | 1 | 7.37 |
| CHEMBL1171917 | — | — | 1 | 7.32 |
| CHEMBL4102372 | — | — | 1 | 7.25 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.21 |
| CHEMBL1169963 | — | — | 1 | 7.17 |
| CHEMBL4060625 | — | — | 1 | 6.25 |
| CHEMBL3827235 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077148 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL4064375 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL1172685 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1171916 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1171865 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1169962 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4092162 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4077547 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3828752 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL1171917 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL4102372 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL1169963 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4060625 | — | Ki | = | 556.0 | nM | 6.25 |
| CHEMBL3827235 | — | Ki | = | 860.0 | nM | 6.07 |