Assay Detail
Binding
CHEMBL845230
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]U-69593 binding to kappa opioid receptor of guinea pig brain homogenate
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 9.22 | 10.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL438274 | — | — | 1 | 10.46 |
| CHEMBL265241 | — | — | 1 | 10.33 |
| CHEMBL438223 | DYNORPHIN A (1-11) | — | 1 | 10.11 |
| CHEMBL405618 | ANALOG OF DYNORPHIN A | — | 1 | 9.94 |
| CHEMBL409793 | — | — | 1 | 9.94 |
| CHEMBL411196 | — | — | 1 | 9.68 |
| CHEMBL411557 | DYNORPHIN A (1-17) | — | 1 | 9.64 |
| CHEMBL414494 | — | — | 1 | 9.28 |
| CHEMBL444626 | — | — | 1 | 9.23 |
| CHEMBL386722 | — | — | 1 | 9.06 |
| CHEMBL408497 | — | — | 1 | 7.82 |
| CHEMBL2371443 | — | — | 1 | 7.29 |
| CHEMBL384566 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL438274 | — | IC50 | = | 0.035 | nM | 10.46 |
| CHEMBL265241 | — | IC50 | = | 0.047 | nM | 10.33 |
| CHEMBL438223 | DYNORPHIN A (1-11) | IC50 | = | 0.077 | nM | 10.11 |
| CHEMBL405618 | ANALOG OF DYNORPHIN A | IC50 | = | 0.114 | nM | 9.94 |
| CHEMBL409793 | — | IC50 | = | 0.116 | nM | 9.94 |
| CHEMBL411196 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL411557 | DYNORPHIN A (1-17) | IC50 | = | 0.231 | nM | 9.64 |
| CHEMBL414494 | — | IC50 | = | 0.522 | nM | 9.28 |
| CHEMBL444626 | — | IC50 | = | 0.593 | nM | 9.23 |
| CHEMBL386722 | — | IC50 | = | 0.868 | nM | 9.06 |
| CHEMBL408497 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL2371443 | — | IC50 | = | 51.5 | nM | 7.29 |
| CHEMBL384566 | — | IC50 | = | 81.2 | nM | 7.09 |