Assay Detail
Binding
CHEMBL747866
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for mu opioid receptors by displacement of [3H]-DAMGO from rat brain membrane binding site
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.14 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15100 | — | — | 1 | 9.05 |
| CHEMBL14887 | — | — | 1 | 8.68 |
| CHEMBL280264 | — | — | 1 | 8.56 |
| CHEMBL278891 | — | — | 1 | 8.47 |
| CHEMBL2370199 | — | — | 1 | 8.40 |
| CHEMBL275670 | — | — | 1 | 8.23 |
| CHEMBL278889 | — | — | 1 | 8.19 |
| CHEMBL8234 | ENKEPHALIN | — | 1 | 8.03 |
| CHEMBL274012 | — | — | 1 | 7.77 |
| CHEMBL557035 | — | — | 1 | 7.10 |
| CHEMBL2370207 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15100 | — | Ki | = | 0.881 | nM | 9.05 |
| CHEMBL14887 | — | Ki | = | 2.09 | nM | 8.68 |
| CHEMBL280264 | — | Ki | = | 2.74 | nM | 8.56 |
| CHEMBL278891 | — | Ki | = | 3.42 | nM | 8.47 |
| CHEMBL2370199 | — | Ki | = | 3.99 | nM | 8.40 |
| CHEMBL275670 | — | Ki | = | 5.89 | nM | 8.23 |
| CHEMBL278889 | — | Ki | = | 6.41 | nM | 8.19 |
| CHEMBL8234 | ENKEPHALIN | Ki | = | 9.43 | nM | 8.03 |
| CHEMBL274012 | — | Ki | = | 17.1 | nM | 7.77 |
| CHEMBL557035 | — | Ki | = | 78.8 | nM | 7.10 |
| CHEMBL2370207 | — | Ki | = | 81.3 | nM | 7.09 |