Assay Detail
Binding
CHEMBL758582
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Displacement of [3H]endomorphin-2 from Opioid receptor mu 1 of rat brain membranes
14
Total Activities
14
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
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.65 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL166312 | — | — | 1 | 9.33 |
| CHEMBL436039 | — | — | 1 | 9.01 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 8.79 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 8.40 |
| CHEMBL351976 | — | — | 1 | 7.63 |
| CHEMBL163334 | — | — | 1 | 7.63 |
| CHEMBL423794 | — | — | 1 | 7.46 |
| CHEMBL355153 | — | — | 1 | 7.36 |
| CHEMBL163871 | — | — | 1 | 7.33 |
| CHEMBL349738 | — | — | 1 | 7.32 |
| CHEMBL423466 | — | — | 1 | 7.14 |
| CHEMBL355141 | — | — | 1 | 6.90 |
| CHEMBL166108 | — | — | 1 | 5.16 |
| CHEMBL355367 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL166312 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL436039 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL316446 | ENDOMORPHIN-1 | Ki | = | 1.62 | nM | 8.79 |
| CHEMBL333357 | ENDOMORPHIN 2 | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL351976 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL163334 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL423794 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL355153 | — | Ki | = | 43.6 | nM | 7.36 |
| CHEMBL163871 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL349738 | — | Ki | = | 47.7 | nM | 7.32 |
| CHEMBL423466 | — | Ki | = | 73.1 | nM | 7.14 |
| CHEMBL355141 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL166108 | — | Ki | = | 6980.0 | nM | 5.16 |
| CHEMBL355367 | — | Ki | > | 10000.0 | nM | - |