Assay Detail
Binding
CHEMBL4615564
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 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
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.05 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4639180 | — | — | 1 | 8.10 |
| CHEMBL4633788 | — | — | 1 | 7.72 |
| CHEMBL4643805 | — | — | 1 | 7.70 |
| CHEMBL4640137 | — | — | 1 | 7.54 |
| CHEMBL4640809 | — | — | 1 | 7.39 |
| CHEMBL4644807 | — | — | 1 | 7.16 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL4644248 | — | — | 1 | 6.94 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 6.90 |
| CHEMBL4638673 | — | — | 1 | 6.83 |
| CHEMBL4643145 | — | — | 1 | 6.59 |
| CHEMBL4636240 | — | — | 1 | 6.57 |
| CHEMBL4636929 | — | — | 1 | 6.48 |
| CHEMBL4636805 | — | — | 1 | 6.47 |
| CHEMBL4638934 | — | — | 1 | 6.16 |
| CHEMBL4636728 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4639180 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4633788 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4643805 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4640137 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4640809 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4644807 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4644248 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL4638673 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL4643145 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL4636240 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL4636929 | — | Ki | = | 333.0 | nM | 6.48 |
| CHEMBL4636805 | — | Ki | = | 336.0 | nM | 6.47 |
| CHEMBL4638934 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL4636728 | — | Ki | = | 849.0 | nM | 6.07 |