Assay Detail
Binding
CHEMBL755496
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dynorphin A from Opioid receptor kappa 1 of rat brain membranes (DAMGO/DADLE quenching of mu/delta receptor binding)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.98 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333357 | ENDOMORPHIN 2 | — | 1 | 7.97 |
| CHEMBL436039 | — | — | 1 | 7.92 |
| CHEMBL163334 | — | — | 1 | 7.55 |
| CHEMBL166312 | — | — | 1 | 7.47 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 1 | 7.28 |
| CHEMBL423794 | — | — | 1 | 7.25 |
| CHEMBL351976 | — | — | 1 | 7.18 |
| CHEMBL423466 | — | — | 1 | 7.08 |
| CHEMBL349738 | — | — | 1 | 7.03 |
| CHEMBL355141 | — | — | 1 | 6.74 |
| CHEMBL163871 | — | — | 1 | 6.50 |
| CHEMBL355153 | — | — | 1 | 6.33 |
| CHEMBL355367 | — | — | 1 | 6.00 |
| CHEMBL166108 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333357 | ENDOMORPHIN 2 | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL436039 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL163334 | — | Ki | = | 28.1 | nM | 7.55 |
| CHEMBL166312 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL316446 | ENDOMORPHIN-1 | Ki | = | 52.7 | nM | 7.28 |
| CHEMBL423794 | — | Ki | = | 55.7 | nM | 7.25 |
| CHEMBL351976 | — | Ki | = | 65.4 | nM | 7.18 |
| CHEMBL423466 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL349738 | — | Ki | = | 94.3 | nM | 7.03 |
| CHEMBL355141 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL163871 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL355153 | — | Ki | = | 467.0 | nM | 6.33 |
| CHEMBL355367 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL166108 | — | Ki | = | 4470.0 | nM | 5.35 |