Assay Detail
Binding
CHEMBL2209606
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Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebellum membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| 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 | 9.11 | 9.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2205419 | — | — | 1 | 9.79 |
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | 4.0 | 1 | 9.75 |
| CHEMBL2205420 | — | — | 1 | 9.52 |
| CHEMBL2205421 | — | — | 1 | 9.47 |
| CHEMBL2205418 | — | — | 1 | 9.47 |
| CHEMBL2205412 | — | — | 1 | 9.35 |
| CHEMBL519367 | — | — | 1 | 9.15 |
| CHEMBL2205413 | — | — | 1 | 9.15 |
| CHEMBL2204731 | — | — | 1 | 9.13 |
| CHEMBL2204730 | — | — | 1 | 8.96 |
| CHEMBL2205416 | — | — | 1 | 8.69 |
| CHEMBL2205414 | — | — | 1 | 8.65 |
| CHEMBL2205417 | — | — | 1 | 8.64 |
| CHEMBL2205415 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2205419 | — | Ki | = | 0.163 | nM | 9.79 |
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | Ki | = | 0.178 | nM | 9.75 |
| CHEMBL2205420 | — | Ki | = | 0.303 | nM | 9.52 |
| CHEMBL2205421 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL2205418 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL2205412 | — | Ki | = | 0.451 | nM | 9.35 |
| CHEMBL519367 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL2205413 | — | Ki | = | 0.711 | nM | 9.15 |
| CHEMBL2204731 | — | Ki | = | 0.733 | nM | 9.13 |
| CHEMBL2204730 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2205416 | — | Ki | = | 2.06 | nM | 8.69 |
| CHEMBL2205414 | — | Ki | = | 2.23 | nM | 8.65 |
| CHEMBL2205417 | — | Ki | = | 2.28 | nM | 8.64 |
| CHEMBL2205415 | — | Ki | = | 14.5 | nM | 7.84 |