Assay Detail
Binding
CHEMBL828094
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Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.56 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 9.30 |
| CHEMBL38874 | DAMGO | — | 1 | 8.00 |
| CHEMBL187369 | — | — | 1 | 7.40 |
| CHEMBL364853 | — | — | 1 | 5.50 |
| CHEMBL359792 | — | — | 1 | 5.42 |
| CHEMBL364764 | — | — | 1 | 5.28 |
| CHEMBL434545 | — | — | 1 | 5.09 |
| CHEMBL365002 | — | — | 1 | 4.85 |
| CHEMBL362739 | — | — | 1 | 4.72 |
| CHEMBL363714 | — | — | 1 | 4.54 |
| CHEMBL365889 | — | — | 1 | 4.54 |
| CHEMBL359791 | — | — | 1 | 4.50 |
| CHEMBL365667 | — | — | 1 | 4.41 |
| CHEMBL365003 | — | — | 1 | 4.35 |
| CHEMBL365609 | — | — | 1 | - |
| CHEMBL189285 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL38874 | DAMGO | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL187369 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL364853 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL359792 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL364764 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL434545 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL365002 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL362739 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL363714 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL365889 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL359791 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL365667 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL365003 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL365609 | — | IC50 | = | 240000.0 | nM | - |
| CHEMBL189285 | — | IC50 | = | 102000.0 | nM | - |