Assay Detail
Functional
CHEMBL4138420
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Agonist activity at mouse KOR expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 90 mins by scintillation spectroscopy
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.48 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL58033 | (-)-U-50488 | — | 1 | 7.77 |
| CHEMBL2437063 | — | — | 1 | 7.44 |
| CHEMBL4165157 | — | — | 1 | 7.23 |
| CHEMBL4167929 | — | — | 1 | - |
| CHEMBL4167519 | — | — | 1 | - |
| CHEMBL4159603 | — | — | 1 | - |
| CHEMBL4173059 | — | — | 1 | - |
| CHEMBL4168572 | — | — | 1 | - |
| CHEMBL38874 | DAMGO | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL58033 | (-)-U-50488 | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2437063 | — | EC50 | = | 36.5 | nM | 7.44 |
| CHEMBL4165157 | — | EC50 | = | 58.83 | nM | 7.23 |
| CHEMBL4167929 | — | EC50 | - | — | - | |
| CHEMBL4167519 | — | EC50 | - | — | - | |
| CHEMBL4159603 | — | EC50 | - | — | - | |
| CHEMBL4173059 | — | EC50 | - | — | - | |
| CHEMBL4168572 | — | EC50 | - | — | - | |
| CHEMBL38874 | DAMGO | EC50 | - | — | - |