Assay Detail
Binding
CHEMBL969336
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Displacement of [3H]DAMGO from mu opioid receptor in human SH-SY5Y cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 9 | 7.17 | 8.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 8.84 |
| CHEMBL35838 | [LEU5]ENKEPHALIN | — | 1 | 7.94 |
| CHEMBL504973 | — | — | 1 | 7.92 |
| CHEMBL500212 | — | — | 1 | 7.43 |
| CHEMBL512955 | — | — | 1 | 7.14 |
| CHEMBL455502 | — | — | 1 | 6.95 |
| CHEMBL387816 | — | — | 1 | 6.65 |
| CHEMBL466147 | — | — | 1 | 6.15 |
| CHEMBL445690 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL35838 | [LEU5]ENKEPHALIN | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL504973 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL500212 | — | Ki | = | 37.3 | nM | 7.43 |
| CHEMBL512955 | — | Ki | = | 72.7 | nM | 7.14 |
| CHEMBL455502 | — | Ki | = | 112.5 | nM | 6.95 |
| CHEMBL387816 | — | Ki | = | 225.9 | nM | 6.65 |
| CHEMBL466147 | — | Ki | = | 705.0 | nM | 6.15 |
| CHEMBL445690 | — | Ki | = | 3190.0 | nM | 5.50 |