Assay Detail
Binding
CHEMBL5033452
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DAMGO from human MOR expressed in CHO-K1 cell membranes incubated for 60 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 | CHO-K1 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 7.21 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5087472 | — | — | 1 | 8.70 |
| CHEMBL5084344 | — | — | 1 | 8.30 |
| CHEMBL5089000 | — | — | 1 | 8.22 |
| CHEMBL5081133 | — | — | 1 | 8.22 |
| CHEMBL5076404 | — | — | 1 | 8.10 |
| CHEMBL5075502 | — | — | 1 | 8.05 |
| CHEMBL5089489 | — | — | 1 | 8.05 |
| CHEMBL656 | OXYCODONE | 4.0 | 1 | 7.92 |
| CHEMBL5070613 | — | — | 1 | 7.85 |
| CHEMBL5079816 | — | — | 1 | 7.72 |
| CHEMBL5094899 | — | — | 1 | 7.55 |
| CHEMBL5089766 | — | — | 1 | 7.55 |
| CHEMBL5073189 | — | — | 1 | 7.50 |
| CHEMBL5083736 | — | — | 1 | 7.48 |
| CHEMBL5090595 | — | — | 1 | 7.43 |
| CHEMBL5077829 | — | — | 1 | 7.37 |
| CHEMBL5092587 | — | — | 1 | 7.34 |
| CHEMBL5087458 | — | — | 1 | 7.31 |
| CHEMBL5078587 | — | — | 1 | 7.19 |
| CHEMBL5070185 | — | — | 1 | 7.14 |
| CHEMBL5083271 | — | — | 1 | 7.14 |
| CHEMBL5089365 | — | — | 1 | 7.09 |
| CHEMBL5085771 | — | — | 1 | 7.08 |
| CHEMBL5084697 | — | — | 1 | 7.02 |
| CHEMBL5080086 | — | — | 1 | 6.97 |
| CHEMBL5080761 | — | — | 1 | 6.86 |
| CHEMBL5084395 | — | — | 1 | 6.80 |
| CHEMBL5090993 | — | — | 1 | 6.78 |
| CHEMBL5093833 | — | — | 1 | 6.77 |
| CHEMBL5082031 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5087472 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL5084344 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL5081133 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5089000 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5076404 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5075502 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL5089489 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL656 | OXYCODONE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5070613 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5079816 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL5094899 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL5089766 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL5073189 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL5083736 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL5090595 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL5077829 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL5092587 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL5087458 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL5078587 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL5070185 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL5083271 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL5089365 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL5085771 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL5084697 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL5080086 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL5080761 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL5084395 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL5090993 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL5093833 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL5082031 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL5076707 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL5093051 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL5086571 | — | Ki | = | 251.0 | nM | 6.60 |
| CHEMBL5091094 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL5081159 | — | Ki | = | 279.0 | nM | 6.55 |
| CHEMBL5082661 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL5094913 | — | Ki | = | 437.0 | nM | 6.36 |
| CHEMBL5081183 | — | Ki | = | 452.0 | nM | 6.34 |
| CHEMBL5079087 | — | Ki | = | 754.0 | nM | 6.12 |
| CHEMBL5085710 | — | Ki | = | 1005.0 | nM | 6.00 |
| CHEMBL5072099 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5079310 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5074927 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5075152 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5077038 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2170062 | — | Ki | > | 10000.0 | nM | - |