Assay Detail
Binding
CHEMBL1693237
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane homogenate by liquid scintillation counting
16
Total Activities
16
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 | Autocuration |
Publication
Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.46 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1689552 | — | — | 1 | 9.89 |
| CHEMBL1689548 | — | — | 1 | 9.33 |
| CHEMBL1689546 | — | — | 1 | 9.09 |
| CHEMBL1689541 | — | — | 1 | 9.03 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 8.87 |
| CHEMBL1689550 | — | — | 1 | 8.82 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 8.80 |
| CHEMBL1689551 | — | — | 1 | 8.55 |
| CHEMBL1689543 | — | — | 1 | 8.49 |
| CHEMBL1689542 | — | — | 1 | 8.39 |
| CHEMBL1689539 | — | — | 1 | 8.38 |
| CHEMBL1689549 | — | — | 1 | 8.01 |
| CHEMBL1689545 | — | — | 1 | 7.96 |
| CHEMBL1689547 | — | — | 1 | 7.47 |
| CHEMBL1689540 | — | — | 1 | 7.46 |
| CHEMBL1689544 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1689552 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL1689548 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL1689546 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL1689541 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL333357 | ENDOMORPHIN 2 | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL1689550 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL316446 | ENDOMORPHIN-1 | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1689551 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1689543 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1689542 | — | Ki | = | 4.11 | nM | 8.39 |
| CHEMBL1689539 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL1689549 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL1689545 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL1689547 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL1689540 | — | Ki | = | 34.6 | nM | 7.46 |
| CHEMBL1689544 | — | Ki | = | 143.1 | nM | 6.84 |