Assay Detail
Binding
CHEMBL2209608
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain membranes without cerebellum
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.09 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2205419 | — | — | 1 | 9.49 |
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | 4.0 | 1 | 9.37 |
| CHEMBL519367 | — | — | 1 | 9.25 |
| CHEMBL2204730 | — | — | 1 | 8.28 |
| CHEMBL2205412 | — | — | 1 | 8.26 |
| CHEMBL2205420 | — | — | 1 | 8.19 |
| CHEMBL2205417 | — | — | 1 | 8.06 |
| CHEMBL2205418 | — | — | 1 | 8.05 |
| CHEMBL2205421 | — | — | 1 | 7.91 |
| CHEMBL2205414 | — | — | 1 | 7.58 |
| CHEMBL2205413 | — | — | 1 | 7.46 |
| CHEMBL2205415 | — | — | 1 | 7.29 |
| CHEMBL2204731 | — | — | 1 | 7.24 |
| CHEMBL2205416 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2205419 | — | Ki | = | 0.324 | nM | 9.49 |
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | Ki | = | 0.431 | nM | 9.37 |
| CHEMBL519367 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL2204730 | — | Ki | = | 5.26 | nM | 8.28 |
| CHEMBL2205412 | — | Ki | = | 5.49 | nM | 8.26 |
| CHEMBL2205420 | — | Ki | = | 6.52 | nM | 8.19 |
| CHEMBL2205417 | — | Ki | = | 8.62 | nM | 8.06 |
| CHEMBL2205418 | — | Ki | = | 8.88 | nM | 8.05 |
| CHEMBL2205421 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL2205414 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2205413 | — | Ki | = | 34.7 | nM | 7.46 |
| CHEMBL2205415 | — | Ki | = | 51.1 | nM | 7.29 |
| CHEMBL2204731 | — | Ki | = | 57.6 | nM | 7.24 |
| CHEMBL2205416 | — | Ki | = | 147.0 | nM | 6.83 |