Assay Detail
Binding
CHEMBL905183
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Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells
18
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.64 | 8.85 |
| IC50 | 8 | 7.14 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200199 | BIPHALIN | — | 1 | 8.85 |
| CHEMBL229280 | — | — | 2 | 8.26 |
| CHEMBL439019 | — | — | 2 | 8.01 |
| CHEMBL340032 | DADLE | — | 1 | 7.82 |
| CHEMBL389651 | — | — | 2 | 7.64 |
| CHEMBL426363 | — | — | 2 | 7.57 |
| CHEMBL2371977 | — | — | 2 | 7.55 |
| CHEMBL389652 | — | — | 2 | 7.44 |
| CHEMBL387670 | — | — | 2 | 6.85 |
| CHEMBL2371978 | — | — | 2 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200199 | BIPHALIN | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL229280 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL439019 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL229280 | — | IC50 | = | 12.88 | nM | 7.89 |
| CHEMBL340032 | DADLE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL439019 | — | IC50 | = | 20.42 | nM | 7.69 |
| CHEMBL389651 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL426363 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2371977 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL389652 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL389651 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL426363 | — | IC50 | = | 57.54 | nM | 7.24 |
| CHEMBL2371977 | — | IC50 | = | 60.26 | nM | 7.22 |
| CHEMBL389652 | — | IC50 | = | 77.62 | nM | 7.11 |
| CHEMBL387670 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL387670 | — | IC50 | = | 288.4 | nM | 6.54 |
| CHEMBL2371978 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL2371978 | — | IC50 | = | 812.83 | nM | 6.09 |