Assay Detail
Functional
CHEMBL2050641
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Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting
14
Total Activities
14
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 |
|---|---|---|---|
| EC50 | 14 | 8.02 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 9.10 |
| CHEMBL2048767 | — | — | 1 | 8.96 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 8.80 |
| CHEMBL2048770 | — | — | 1 | 8.44 |
| CHEMBL2048764 | — | — | 1 | 8.44 |
| CHEMBL2048761 | — | — | 1 | 8.42 |
| CHEMBL2048774 | — | — | 1 | 8.19 |
| CHEMBL568877 | — | — | 1 | 8.17 |
| CHEMBL2048762 | — | — | 1 | 8.11 |
| CHEMBL2048771 | — | — | 1 | 8.06 |
| CHEMBL2048768 | — | — | 1 | 7.42 |
| CHEMBL38874 | DAMGO | — | 1 | 7.26 |
| CHEMBL2048782 | — | — | 1 | 6.68 |
| CHEMBL2048786 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2048767 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL301160 | BUTORPHAN | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2048770 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2048764 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2048761 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2048774 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL568877 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2048762 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL2048771 | — | EC50 | = | 8.8 | nM | 8.06 |
| CHEMBL2048768 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL38874 | DAMGO | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL2048782 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2048786 | — | EC50 | = | 550.0 | nM | 6.26 |