Assay Detail
Binding
CHEMBL3583976
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Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes after 120 mins by scintillation counting analysis
13
Total Activities
13
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
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 9.15 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3580743 | — | — | 1 | 9.38 |
| CHEMBL3580749 | — | — | 1 | 9.31 |
| CHEMBL3580746 | — | — | 1 | 9.27 |
| CHEMBL3580745 | — | — | 1 | 9.26 |
| CHEMBL3580748 | — | — | 1 | 9.21 |
| CHEMBL3582485 | — | — | 1 | 9.16 |
| CHEMBL3582484 | — | — | 1 | 9.14 |
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 9.10 |
| CHEMBL3580750 | — | — | 1 | 9.04 |
| CHEMBL3582487 | — | — | 1 | 9.01 |
| CHEMBL3580744 | — | — | 1 | 8.80 |
| CHEMBL3580747 | — | — | 1 | - |
| CHEMBL3582486 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3580743 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL3580749 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL3580746 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL3580745 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL3580748 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL3582485 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL3582484 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL333357 | ENDOMORPHIN 2 | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL3580750 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL3582487 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL3580744 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3580747 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3582486 | — | IC50 | > | 1000.0 | nM | - |