Assay Detail
Binding
CHEMBL754623
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Binding affinity was measured on opioid receptor kappa 1
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
[2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.84 | 10.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216640 | — | — | 1 | 10.06 |
| CHEMBL436911 | — | — | 1 | 9.49 |
| CHEMBL506821 | — | — | 1 | 9.09 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.09 |
| CHEMBL407124 | — | — | 1 | 8.61 |
| CHEMBL414502 | — | — | 1 | 8.46 |
| CHEMBL414068 | — | — | 1 | 8.42 |
| CHEMBL216899 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216640 | — | Ki | = | 0.0869 | nM | 10.06 |
| CHEMBL436911 | — | Ki | = | 0.322 | nM | 9.49 |
| CHEMBL506821 | — | Ki | = | 0.823 | nM | 9.09 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL407124 | — | Ki | = | 2.47 | nM | 8.61 |
| CHEMBL414502 | — | Ki | = | 3.49 | nM | 8.46 |
| CHEMBL414068 | — | Ki | = | 3.84 | nM | 8.42 |
| CHEMBL216899 | — | Ki | = | 30.7 | nM | 7.51 |