Assay Detail
Binding
CHEMBL756072
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at kappa opioid receptor in guinea pig brain by [3H]U-69593 displacement.
19
Total Activities
19
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
Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.11 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411338 | — | — | 1 | 9.28 |
| CHEMBL216640 | — | — | 1 | 9.24 |
| CHEMBL2370618 | — | — | 1 | 9.15 |
| CHEMBL2112652 | — | — | 1 | 9.00 |
| CHEMBL2370611 | — | — | 1 | 9.00 |
| CHEMBL2370629 | — | — | 1 | 8.96 |
| CHEMBL2370622 | — | — | 1 | 8.70 |
| CHEMBL2370627 | — | — | 1 | 8.64 |
| CHEMBL2370612 | — | — | 1 | 8.51 |
| CHEMBL2370626 | — | — | 1 | 7.82 |
| CHEMBL374268 | — | — | 1 | 7.82 |
| CHEMBL404929 | — | — | 1 | 7.75 |
| CHEMBL2370610 | — | — | 1 | 7.58 |
| CHEMBL2370631 | — | — | 1 | 7.37 |
| CHEMBL263509 | — | — | 1 | 7.15 |
| CHEMBL2370628 | — | — | 1 | 7.06 |
| CHEMBL2369128 | — | — | 1 | 7.02 |
| CHEMBL414713 | — | — | 1 | 7.00 |
| CHEMBL2111843 | — | — | 1 | 6.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411338 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL216640 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL2370618 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL2112652 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2370611 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2370629 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2370622 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2370627 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2370612 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2370626 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL374268 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL404929 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2370610 | — | IC50 | = | 26.1 | nM | 7.58 |
| CHEMBL2370631 | — | IC50 | = | 42.6 | nM | 7.37 |
| CHEMBL263509 | — | IC50 | = | 70.5 | nM | 7.15 |
| CHEMBL2370628 | — | IC50 | = | 87.1 | nM | 7.06 |
| CHEMBL2369128 | — | IC50 | = | 96.2 | nM | 7.02 |
| CHEMBL414713 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2111843 | — | IC50 | = | 104.0 | nM | 6.98 |