Assay Detail
Functional
CHEMBL4138418
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Agonist activity at mouse MOR 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 | 8.10 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2437063 | — | — | 1 | 8.86 |
| CHEMBL4165157 | — | — | 1 | 8.55 |
| CHEMBL4159603 | — | — | 1 | 8.34 |
| CHEMBL4168572 | — | — | 1 | 8.10 |
| CHEMBL4173059 | — | — | 1 | 8.09 |
| CHEMBL38874 | DAMGO | — | 1 | 7.72 |
| CHEMBL4167519 | — | — | 1 | 7.59 |
| CHEMBL4167929 | — | — | 1 | 7.58 |
| CHEMBL58033 | (-)-U-50488 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2437063 | — | EC50 | = | 1.38 | nM | 8.86 |
| CHEMBL4165157 | — | EC50 | = | 2.83 | nM | 8.55 |
| CHEMBL4159603 | — | EC50 | = | 4.62 | nM | 8.34 |
| CHEMBL4168572 | — | EC50 | = | 7.98 | nM | 8.10 |
| CHEMBL4173059 | — | EC50 | = | 8.16 | nM | 8.09 |
| CHEMBL38874 | DAMGO | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4167519 | — | EC50 | = | 25.7 | nM | 7.59 |
| CHEMBL4167929 | — | EC50 | = | 26.42 | nM | 7.58 |
| CHEMBL58033 | (-)-U-50488 | EC50 | - | — | - |