Assay Detail
Functional
CHEMBL3268177
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Antagonist activity at kappa opioid receptor in guinea pig caudate assessed as inhibition of U69593-stimulated [35S]-GTP[gammaS] binding
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Antagonists of the kappa opioid receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ke | 8 | - | - |
| Ki | 1 | 10.70 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415247 | JDTIC | 1.0 | 1 | 10.70 |
| CHEMBL10986 | — | — | 1 | - |
| CHEMBL3264437 | — | — | 1 | - |
| CHEMBL2111681 | — | — | 1 | - |
| CHEMBL326471 | — | — | 1 | - |
| CHEMBL10872 | — | — | 1 | - |
| CHEMBL2112472 | — | — | 1 | - |
| CHEMBL3264438 | — | — | 1 | - |
| CHEMBL575508 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415247 | JDTIC | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL10986 | — | Ke | = | 4.7 | nM | - |
| CHEMBL3264437 | — | Ke | = | 44.6 | nM | - |
| CHEMBL2111681 | — | Ke | = | 30.0 | nM | - |
| CHEMBL326471 | — | Ke | = | 4.2 | nM | - |
| CHEMBL10872 | — | Ke | = | 11.5 | nM | - |
| CHEMBL2112472 | — | Ke | = | 19.6 | nM | - |
| CHEMBL3264438 | — | Ke | = | 0.16 | nM | - |
| CHEMBL575508 | — | Ke | = | 0.37 | nM | - |