Assay Detail
Functional
CHEMBL2050643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [33S]GTPgammaS binding after 60 mins by scintillation counting
19
Total Activities
19
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
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.79 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2048766 | — | — | 1 | 9.68 |
| CHEMBL49269 | CYCLORPHAN | — | 1 | 8.77 |
| CHEMBL2048765 | — | — | 1 | 8.70 |
| CHEMBL2048772 | — | — | 1 | 8.46 |
| CHEMBL2048769 | — | — | 1 | 8.32 |
| CHEMBL2048767 | — | — | 1 | 8.17 |
| CHEMBL2048773 | — | — | 1 | 8.12 |
| CHEMBL568877 | — | — | 1 | 8.00 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 7.70 |
| CHEMBL2048770 | — | — | 1 | 7.12 |
| CHEMBL2048761 | — | — | 1 | 7.10 |
| CHEMBL2048764 | — | — | 1 | 7.03 |
| CHEMBL2048762 | — | — | 1 | 6.82 |
| CHEMBL2048771 | — | — | 1 | 6.80 |
| CHEMBL2048768 | — | — | 1 | 6.09 |
| CHEMBL38874 | DAMGO | — | 1 | - |
| CHEMBL2048774 | — | — | 1 | - |
| CHEMBL2048782 | — | — | 1 | - |
| CHEMBL2048786 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2048766 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL49269 | CYCLORPHAN | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2048765 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2048772 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL2048769 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2048767 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2048773 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL568877 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL301160 | BUTORPHAN | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2048770 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2048761 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2048764 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2048762 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2048771 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2048768 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL38874 | DAMGO | IC50 | - | — | - | |
| CHEMBL2048774 | — | IC50 | - | — | - | |
| CHEMBL2048782 | — | IC50 | - | — | - | |
| CHEMBL2048786 | — | IC50 | - | — | - |