Assay Detail
Functional
CHEMBL958397
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding
30
Total Activities
16
Compounds Tested
2
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
Syntheses of novel high affinity ligands for opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.71 | 9.06 |
| Imax | 14 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL471243 | — | — | 2 | 9.06 |
| CHEMBL470005 | — | — | 2 | 8.42 |
| CHEMBL511816 | — | — | 2 | 8.36 |
| CHEMBL19019 | NALTREXONE | 4.0 | 2 | 8.32 |
| CHEMBL511645 | — | — | 2 | 8.19 |
| CHEMBL512150 | — | — | 2 | 7.58 |
| CHEMBL511302 | — | — | 2 | 7.28 |
| CHEMBL511621 | — | — | 2 | 7.27 |
| CHEMBL895 | NALBUPHINE | 4.0 | 2 | 7.02 |
| CHEMBL470617 | NALTREXONE METHIODIDE | — | 2 | 6.77 |
| CHEMBL56695 | — | — | 2 | 6.57 |
| CHEMBL471049 | — | — | 2 | - |
| CHEMBL398707 | HYDROMORPHONE | 4.0 | 2 | - |
| CHEMBL469815 | — | — | 2 | - |
| CHEMBL38874 | DAMGO | — | 1 | - |
| CHEMBL471048 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL471243 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL470005 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL511816 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL511645 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL512150 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL511302 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL511621 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL895 | NALBUPHINE | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL470617 | NALTREXONE METHIODIDE | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL56695 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL471049 | — | Imax | - | — | - | |
| CHEMBL398707 | HYDROMORPHONE | IC50 | - | — | - | |
| CHEMBL398707 | HYDROMORPHONE | Imax | - | — | - | |
| CHEMBL469815 | — | IC50 | - | — | - | |
| CHEMBL469815 | — | Imax | - | — | - | |
| CHEMBL19019 | NALTREXONE | Imax | = | 93.0 | % | - |
| CHEMBL38874 | DAMGO | IC50 | - | — | - | |
| CHEMBL511816 | — | Imax | = | 89.0 | % | - |
| CHEMBL511621 | — | Imax | = | 93.0 | % | - |
| CHEMBL471048 | — | IC50 | - | — | - | |
| CHEMBL471049 | — | IC50 | - | — | - | |
| CHEMBL470617 | NALTREXONE METHIODIDE | Imax | = | 98.0 | % | - |
| CHEMBL471243 | — | Imax | = | 92.0 | % | - |
| CHEMBL56695 | — | Imax | = | 91.0 | % | - |
| CHEMBL511302 | — | Imax | = | 96.0 | % | - |
| CHEMBL511645 | — | Imax | = | 81.0 | % | - |
| CHEMBL512150 | — | Imax | = | 84.0 | % | - |
| CHEMBL895 | NALBUPHINE | Imax | = | 76.0 | % | - |
| CHEMBL470005 | — | Imax | = | 92.0 | % | - |