Assay Detail
Binding
CHEMBL756652
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Binding affinity against Opioid receptor mu 1 using [3H]DAMGO in rat brain synaptosomes was determined
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.31 | 10.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL278789 | DERMORPHIN | — | 1 | 10.04 |
| CHEMBL168110 | — | — | 1 | 8.35 |
| CHEMBL317956 | DELTORPHIN C | — | 1 | 6.50 |
| CHEMBL169860 | — | — | 1 | 5.96 |
| CHEMBL169439 | — | — | 1 | 5.71 |
| CHEMBL355178 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL278789 | DERMORPHIN | Ki | = | 0.092 | nM | 10.04 |
| CHEMBL168110 | — | Ki | = | 4.43 | nM | 8.35 |
| CHEMBL317956 | DELTORPHIN C | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL169860 | — | Ki | = | 1098.0 | nM | 5.96 |
| CHEMBL169439 | — | Ki | = | 1956.0 | nM | 5.71 |
| CHEMBL355178 | — | Ki | = | 0.00054 | nM | - |