Assay Detail
Functional
CHEMBL970213
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Agonist activity at mu opioid receptor assessed as inhibition of forskolin-induced cAMP production in human SH-SY5Y cells pretreated for 24 hrs with excess ligand after 15 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.14 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL504973 | — | — | 1 | 7.31 |
| CHEMBL35838 | [LEU5]ENKEPHALIN | — | 1 | 7.24 |
| CHEMBL455502 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL504973 | — | IC50 | = | 49.2 | nM | 7.31 |
| CHEMBL35838 | [LEU5]ENKEPHALIN | IC50 | = | 57.8 | nM | 7.24 |
| CHEMBL455502 | — | IC50 | = | 132.4 | nM | 6.88 |