Assay Detail
Binding
CHEMBL5035602
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 incubated for 90 mins by liquid scintillation counting method
28
Total Activities
28
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
Optimization of bifunctional piperidinamide derivatives as σ<sub>1</sub>R Antagonists/MOR agonists for treating neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.04 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5079619 | — | — | 1 | 8.26 |
| CHEMBL5094951 | — | — | 1 | 7.79 |
| CHEMBL5087973 | — | — | 1 | 7.71 |
| CHEMBL5078411 | — | — | 1 | 7.64 |
| CHEMBL5078392 | — | — | 1 | 7.52 |
| CHEMBL5075339 | — | — | 1 | 7.46 |
| CHEMBL4788719 | — | — | 1 | 7.41 |
| CHEMBL5093427 | — | — | 1 | 7.38 |
| CHEMBL5087369 | — | — | 1 | 7.22 |
| CHEMBL5086596 | — | — | 1 | 7.17 |
| CHEMBL5079004 | — | — | 1 | 7.10 |
| CHEMBL5092754 | — | — | 1 | 6.95 |
| CHEMBL5082953 | — | — | 1 | 6.95 |
| CHEMBL5082165 | — | — | 1 | 6.91 |
| CHEMBL5087716 | — | — | 1 | 6.81 |
| CHEMBL5092506 | — | — | 1 | 6.77 |
| CHEMBL5086252 | — | — | 1 | 6.75 |
| CHEMBL5087044 | — | — | 1 | 6.73 |
| CHEMBL5078787 | — | — | 1 | 6.72 |
| CHEMBL5094800 | — | — | 1 | 6.66 |
| CHEMBL5080562 | — | — | 1 | 6.65 |
| CHEMBL5081955 | — | — | 1 | 6.62 |
| CHEMBL5092130 | — | — | 1 | 6.58 |
| CHEMBL5079255 | — | — | 1 | 6.57 |
| CHEMBL5094445 | — | — | 1 | 6.39 |
| CHEMBL5078652 | — | — | 1 | 6.24 |
| CHEMBL5087894 | — | — | 1 | - |
| CHEMBL5081685 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5079619 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL5094951 | — | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL5087973 | — | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL5078411 | — | Ki | = | 22.8 | nM | 7.64 |
| CHEMBL5078392 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL5075339 | — | Ki | = | 34.9 | nM | 7.46 |
| CHEMBL4788719 | — | Ki | = | 38.6 | nM | 7.41 |
| CHEMBL5093427 | — | Ki | = | 41.5 | nM | 7.38 |
| CHEMBL5087369 | — | Ki | = | 59.8 | nM | 7.22 |
| CHEMBL5086596 | — | Ki | = | 67.1 | nM | 7.17 |
| CHEMBL5079004 | — | Ki | = | 79.7 | nM | 7.10 |
| CHEMBL5092754 | — | Ki | = | 113.4 | nM | 6.95 |
| CHEMBL5082953 | — | Ki | = | 112.4 | nM | 6.95 |
| CHEMBL5082165 | — | Ki | = | 122.9 | nM | 6.91 |
| CHEMBL5087716 | — | Ki | = | 155.9 | nM | 6.81 |
| CHEMBL5092506 | — | Ki | = | 168.1 | nM | 6.77 |
| CHEMBL5086252 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL5087044 | — | Ki | = | 186.7 | nM | 6.73 |
| CHEMBL5078787 | — | Ki | = | 191.2 | nM | 6.72 |
| CHEMBL5094800 | — | Ki | = | 218.6 | nM | 6.66 |
| CHEMBL5080562 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL5081955 | — | Ki | = | 242.0 | nM | 6.62 |
| CHEMBL5092130 | — | Ki | = | 262.8 | nM | 6.58 |
| CHEMBL5079255 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL5094445 | — | Ki | = | 409.5 | nM | 6.39 |
| CHEMBL5078652 | — | Ki | = | 572.4 | nM | 6.24 |
| CHEMBL5087894 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5081685 | — | Ki | > | 1000.0 | nM | - |