Assay Detail
Binding
CHEMBL828262
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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 |
|---|---|---|---|
| Ki | 16 | 5.67 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 9.80 |
| CHEMBL38874 | DAMGO | — | 1 | 8.80 |
| CHEMBL187369 | — | — | 1 | 7.52 |
| CHEMBL364853 | — | — | 1 | 5.57 |
| CHEMBL359792 | — | — | 1 | 5.54 |
| CHEMBL364764 | — | — | 1 | 5.41 |
| CHEMBL434545 | — | — | 1 | 5.18 |
| CHEMBL365002 | — | — | 1 | 4.96 |
| CHEMBL362739 | — | — | 1 | 4.82 |
| CHEMBL365609 | — | — | 1 | 4.75 |
| CHEMBL365889 | — | — | 1 | 4.64 |
| CHEMBL363714 | — | — | 1 | 4.57 |
| CHEMBL359791 | — | — | 1 | 4.52 |
| CHEMBL365667 | — | — | 1 | 4.50 |
| CHEMBL365003 | — | — | 1 | 4.44 |
| CHEMBL189285 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316446 | ENDOMORPHIN-1 | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL38874 | DAMGO | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL187369 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL364853 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL359792 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL364764 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL434545 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL365002 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL362739 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL365609 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL365889 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL363714 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL359791 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL365667 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL365003 | — | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL189285 | — | Ki | = | 230000.0 | nM | - |