Assay Detail
Functional
CHEMBL5377579
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Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A Novel Bifunctional μOR Agonist and σ<sub>1</sub>R Antagonist with Potent Analgesic Responses and Reduced Adverse Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 7.09 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5415173 | — | — | 1 | 9.22 |
| CHEMBL596 | FENTANYL | 4.0 | 1 | 8.72 |
| CHEMBL5402310 | — | — | 1 | 7.78 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.68 |
| CHEMBL5425299 | — | — | 1 | 7.08 |
| CHEMBL5429304 | — | — | 1 | 6.98 |
| CHEMBL5439322 | — | — | 1 | 6.96 |
| CHEMBL5427406 | — | — | 1 | 6.88 |
| CHEMBL5412869 | — | — | 1 | 6.87 |
| CHEMBL5425711 | — | — | 1 | 6.78 |
| CHEMBL5412750 | — | — | 1 | 6.72 |
| CHEMBL5424782 | — | — | 1 | 6.70 |
| CHEMBL5424620 | — | — | 1 | 6.59 |
| CHEMBL5418375 | — | — | 1 | 6.56 |
| CHEMBL5398451 | — | — | 1 | 6.40 |
| CHEMBL5414844 | — | — | 1 | 6.34 |
| CHEMBL5408125 | — | — | 1 | 6.20 |
| CHEMBL5423809 | — | — | 1 | - |
| CHEMBL5431794 | — | — | 1 | - |
| CHEMBL5434425 | — | — | 1 | - |
| CHEMBL5404249 | — | — | 1 | - |
| CHEMBL5399099 | — | — | 1 | - |
| CHEMBL5404883 | — | — | 1 | - |
| CHEMBL5427357 | — | — | 1 | - |
| CHEMBL5418407 | — | — | 1 | - |
| CHEMBL5395334 | — | — | 1 | - |
| CHEMBL5424850 | — | — | 1 | - |
| CHEMBL5397375 | — | — | 1 | - |
| CHEMBL5402116 | — | — | 1 | - |
| CHEMBL5440830 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5415173 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL596 | FENTANYL | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5402310 | — | EC50 | = | 16.6 | nM | 7.78 |
| CHEMBL70 | MORPHINE | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5425299 | — | EC50 | = | 84.2 | nM | 7.08 |
| CHEMBL5429304 | — | EC50 | = | 104.6 | nM | 6.98 |
| CHEMBL5439322 | — | EC50 | = | 110.3 | nM | 6.96 |
| CHEMBL5427406 | — | EC50 | = | 130.7 | nM | 6.88 |
| CHEMBL5412869 | — | EC50 | = | 134.4 | nM | 6.87 |
| CHEMBL5425711 | — | EC50 | = | 165.2 | nM | 6.78 |
| CHEMBL5412750 | — | EC50 | = | 191.7 | nM | 6.72 |
| CHEMBL5424782 | — | EC50 | = | 200.6 | nM | 6.70 |
| CHEMBL5424620 | — | EC50 | = | 254.4 | nM | 6.59 |
| CHEMBL5418375 | — | EC50 | = | 275.2 | nM | 6.56 |
| CHEMBL5398451 | — | EC50 | = | 394.3 | nM | 6.40 |
| CHEMBL5414844 | — | EC50 | = | 453.4 | nM | 6.34 |
| CHEMBL5408125 | — | EC50 | = | 632.8 | nM | 6.20 |
| CHEMBL5423809 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5431794 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5434425 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5404249 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5399099 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5404883 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5427357 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5418407 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5395334 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5424850 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5397375 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5402116 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5440830 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5423068 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5414314 | — | EC50 | > | 1000.0 | nM | - |