Assay Detail
Binding
CHEMBL751067
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Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.65 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 9.30 |
| CHEMBL316447 | — | — | 1 | 8.40 |
| CHEMBL38874 | DAMGO | — | 1 | 8.00 |
| CHEMBL87907 | — | — | 1 | 7.63 |
| CHEMBL313820 | — | — | 1 | 7.10 |
| CHEMBL430643 | — | — | 1 | 7.10 |
| CHEMBL2112324 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL316447 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL38874 | DAMGO | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL87907 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL313820 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL430643 | — | IC50 | = | 80.1 | nM | 7.10 |
| CHEMBL2112324 | — | IC50 | = | 990.0 | nM | 6.00 |