Assay Detail
Binding
CHEMBL758581
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Displacement of [3H]DAMGO 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 | 7.26 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL166312 | — | — | 1 | 9.10 |
| CHEMBL436039 | — | — | 1 | 8.78 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 8.38 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 8.02 |
| CHEMBL351976 | — | — | 1 | 7.58 |
| CHEMBL355153 | — | — | 1 | 7.34 |
| CHEMBL423466 | — | — | 1 | 7.34 |
| CHEMBL163334 | — | — | 1 | 7.16 |
| CHEMBL349738 | — | — | 1 | 6.98 |
| CHEMBL163871 | — | — | 1 | 6.97 |
| CHEMBL423794 | — | — | 1 | 6.97 |
| CHEMBL355141 | — | — | 1 | 6.60 |
| CHEMBL355367 | — | — | 1 | 5.31 |
| CHEMBL166108 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL166312 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL436039 | — | Ki | = | 1.67 | nM | 8.78 |
| CHEMBL316446 | ENDOMORPHIN-1 | Ki | = | 4.21 | nM | 8.38 |
| CHEMBL333357 | ENDOMORPHIN 2 | Ki | = | 9.53 | nM | 8.02 |
| CHEMBL351976 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL355153 | — | Ki | = | 45.3 | nM | 7.34 |
| CHEMBL423466 | — | Ki | = | 45.3 | nM | 7.34 |
| CHEMBL163334 | — | Ki | = | 69.5 | nM | 7.16 |
| CHEMBL349738 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL163871 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL423794 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL355141 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL355367 | — | Ki | = | 4910.0 | nM | 5.31 |
| CHEMBL166108 | — | Ki | = | 7090.0 | nM | 5.15 |