Assay Detail
Binding
CHEMBL5033451
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from human sigma-1 receptor transfected in HEK293 membranes incubated for 120 mins measured by microBeta scintillation counter method
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ<sub>1</sub> Receptor Antagonists for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 7.18 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5094913 | — | — | 1 | 8.10 |
| CHEMBL5081133 | — | — | 1 | 8.10 |
| CHEMBL5077038 | — | — | 1 | 8.00 |
| CHEMBL5094899 | — | — | 1 | 7.89 |
| CHEMBL5084697 | — | — | 1 | 7.85 |
| CHEMBL2170062 | — | — | 1 | 7.77 |
| CHEMBL5075502 | — | — | 1 | 7.77 |
| CHEMBL5070613 | — | — | 1 | 7.68 |
| CHEMBL5077829 | — | — | 1 | 7.64 |
| CHEMBL5080761 | — | — | 1 | 7.57 |
| CHEMBL5084344 | — | — | 1 | 7.52 |
| CHEMBL5085771 | — | — | 1 | 7.47 |
| CHEMBL5079816 | — | — | 1 | 7.46 |
| CHEMBL5073189 | — | — | 1 | 7.44 |
| CHEMBL5091094 | — | — | 1 | 7.42 |
| CHEMBL5087472 | — | — | 1 | 7.38 |
| CHEMBL5080086 | — | — | 1 | 7.38 |
| CHEMBL5089000 | — | — | 1 | 7.33 |
| CHEMBL5075152 | — | — | 1 | 7.32 |
| CHEMBL5092587 | — | — | 1 | 7.29 |
| CHEMBL5084395 | — | — | 1 | 7.28 |
| CHEMBL5089766 | — | — | 1 | 7.27 |
| CHEMBL5070185 | — | — | 1 | 7.27 |
| CHEMBL5087458 | — | — | 1 | 7.22 |
| CHEMBL5089365 | — | — | 1 | 7.22 |
| CHEMBL5074927 | — | — | 1 | 7.19 |
| CHEMBL5090595 | — | — | 1 | 7.16 |
| CHEMBL5083736 | — | — | 1 | 7.12 |
| CHEMBL5076404 | — | — | 1 | 7.05 |
| CHEMBL5076707 | — | — | 1 | 7.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5094913 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5081133 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5077038 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5094899 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5084697 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2170062 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5075502 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5070613 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5077829 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5080761 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL5084344 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL5085771 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL5079816 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL5073189 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL5091094 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL5087472 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL5080086 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL5089000 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL5075152 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL5092587 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL5084395 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL5089766 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL5070185 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL5087458 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL5089365 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL5074927 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL5090595 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL5083736 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL5076404 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL5076707 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL5086571 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL5079310 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL5090993 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL5083271 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL5081159 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL5089489 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL5093051 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL5079087 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL5081183 | — | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL5078587 | — | Ki | = | 479.0 | nM | 6.32 |
| CHEMBL5072099 | — | Ki | = | 496.0 | nM | 6.30 |
| CHEMBL5093833 | — | Ki | = | 667.0 | nM | 6.18 |
| CHEMBL5085710 | — | Ki | = | 699.0 | nM | 6.16 |
| CHEMBL5082661 | — | Ki | = | 955.0 | nM | 6.02 |
| CHEMBL5082031 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL656 | OXYCODONE | Ki | > | 10000.0 | nM | - |