Assay Detail
Binding
CHEMBL861055
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from rat mu opioid receptor in brain P2 synaptosomes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.78 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL354392 | — | — | 1 | 9.36 |
| CHEMBL322300 | — | — | 1 | 9.31 |
| CHEMBL109390 | — | — | 1 | 9.30 |
| CHEMBL173884 | — | — | 1 | 9.28 |
| CHEMBL422547 | — | — | 1 | 9.08 |
| CHEMBL436063 | — | — | 1 | 8.99 |
| CHEMBL278789 | DERMORPHIN | — | 1 | 8.91 |
| CHEMBL197183 | — | — | 1 | 8.85 |
| CHEMBL354966 | — | — | 1 | 8.16 |
| CHEMBL317956 | DELTORPHIN C | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL354392 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL322300 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL109390 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL173884 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL422547 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL436063 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL278789 | DERMORPHIN | Ki | = | 1.22 | nM | 8.91 |
| CHEMBL197183 | — | Ki | = | 1.42 | nM | 8.85 |
| CHEMBL354966 | — | Ki | = | 6.92 | nM | 8.16 |
| CHEMBL317956 | DELTORPHIN C | Ki | = | 272.0 | nM | 6.57 |