Assay Detail
Functional
CHEMBL5033453
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Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 |
|---|---|---|---|
| EC50 | 46 | 6.93 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5089000 | — | — | 1 | 8.40 |
| CHEMBL5090595 | — | — | 1 | 8.22 |
| CHEMBL5081133 | — | — | 1 | 8.22 |
| CHEMBL5084344 | — | — | 1 | 8.05 |
| CHEMBL5094899 | — | — | 1 | 7.92 |
| CHEMBL656 | OXYCODONE | 4.0 | 1 | 7.77 |
| CHEMBL5083736 | — | — | 1 | 7.62 |
| CHEMBL5070613 | — | — | 1 | 7.58 |
| CHEMBL5073189 | — | — | 1 | 7.55 |
| CHEMBL5087458 | — | — | 1 | 7.52 |
| CHEMBL5087472 | — | — | 1 | 7.47 |
| CHEMBL5089489 | — | — | 1 | 7.46 |
| CHEMBL5076404 | — | — | 1 | 7.41 |
| CHEMBL5089766 | — | — | 1 | 7.28 |
| CHEMBL5075502 | — | — | 1 | 7.14 |
| CHEMBL5089365 | — | — | 1 | 7.08 |
| CHEMBL5080761 | — | — | 1 | 7.07 |
| CHEMBL5092587 | — | — | 1 | 6.88 |
| CHEMBL5085771 | — | — | 1 | 6.85 |
| CHEMBL5077829 | — | — | 1 | 6.80 |
| CHEMBL5093051 | — | — | 1 | 6.75 |
| CHEMBL5086571 | — | — | 1 | 6.74 |
| CHEMBL5090993 | — | — | 1 | 6.68 |
| CHEMBL5080086 | — | — | 1 | 6.60 |
| CHEMBL5084697 | — | — | 1 | 6.52 |
| CHEMBL5084395 | — | — | 1 | 6.50 |
| CHEMBL5076707 | — | — | 1 | 6.29 |
| CHEMBL5083271 | — | — | 1 | 6.29 |
| CHEMBL5081159 | — | — | 1 | 6.22 |
| CHEMBL5079087 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5089000 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5090595 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5081133 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5084344 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5094899 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL656 | OXYCODONE | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5083736 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5070613 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5073189 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5087458 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5087472 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5089489 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5076404 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5089766 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5075502 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5089365 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5080761 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5092587 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL5085771 | — | EC50 | = | 142.0 | nM | 6.85 |
| CHEMBL5077829 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL5093051 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5086571 | — | EC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5090993 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5080086 | — | EC50 | = | 253.0 | nM | 6.60 |
| CHEMBL5084697 | — | EC50 | = | 299.0 | nM | 6.52 |
| CHEMBL5084395 | — | EC50 | = | 314.0 | nM | 6.50 |
| CHEMBL5076707 | — | EC50 | = | 515.0 | nM | 6.29 |
| CHEMBL5083271 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL5081159 | — | EC50 | = | 598.0 | nM | 6.22 |
| CHEMBL5079087 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL5081183 | — | EC50 | = | 738.0 | nM | 6.13 |
| CHEMBL5079310 | — | EC50 | = | 869.0 | nM | 6.06 |
| CHEMBL5093833 | — | EC50 | = | 972.0 | nM | 6.01 |
| CHEMBL5082661 | — | EC50 | = | 1167.0 | nM | 5.93 |
| CHEMBL5082031 | — | EC50 | = | 1237.0 | nM | 5.91 |
| CHEMBL5075152 | — | EC50 | = | 1468.0 | nM | 5.83 |
| CHEMBL5085710 | — | EC50 | = | 4527.0 | nM | 5.34 |
| CHEMBL5091094 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5072099 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5078587 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5079816 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5074927 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5094913 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5070185 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5077038 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2170062 | — | EC50 | > | 10000.0 | nM | - |