Assay Detail
Binding
CHEMBL1228490
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Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.99 | 9.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267495 | NALFURAFINE | 4.0 | 1 | 9.65 |
| CHEMBL1223834 | — | — | 1 | 9.47 |
| CHEMBL1223831 | — | — | 1 | 9.33 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.06 |
| CHEMBL1223773 | — | — | 1 | 9.03 |
| CHEMBL1223774 | — | — | 1 | 8.95 |
| CHEMBL1223832 | — | — | 1 | 8.94 |
| CHEMBL1223833 | — | — | 1 | 8.91 |
| CHEMBL1223889 | — | — | 1 | 8.42 |
| CHEMBL1223890 | — | — | 1 | 8.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267495 | NALFURAFINE | Ki | = | 0.225 | nM | 9.65 |
| CHEMBL1223834 | — | Ki | = | 0.342 | nM | 9.47 |
| CHEMBL1223831 | — | Ki | = | 0.467 | nM | 9.33 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.861 | nM | 9.06 |
| CHEMBL1223773 | — | Ki | = | 0.935 | nM | 9.03 |
| CHEMBL1223774 | — | Ki | = | 1.13 | nM | 8.95 |
| CHEMBL1223832 | — | Ki | = | 1.15 | nM | 8.94 |
| CHEMBL1223833 | — | Ki | = | 1.24 | nM | 8.91 |
| CHEMBL1223889 | — | Ki | = | 3.79 | nM | 8.42 |
| CHEMBL1223890 | — | Ki | = | 7.38 | nM | 8.13 |