Assay Detail
Binding
CHEMBL755978
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Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO 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 |
|---|---|---|---|
| Ki | 7 | 8.04 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 9.80 |
| CHEMBL38874 | DAMGO | — | 1 | 8.80 |
| CHEMBL316447 | — | — | 1 | 8.68 |
| CHEMBL2112324 | — | — | 1 | 7.58 |
| CHEMBL313820 | — | — | 1 | 7.17 |
| CHEMBL87907 | — | — | 1 | 7.14 |
| CHEMBL430643 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL38874 | DAMGO | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL316447 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2112324 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL313820 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL87907 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL430643 | — | Ki | = | 79.0 | nM | 7.10 |