Assay Detail
Binding
CHEMBL5253118
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Agonist activity at human kappa opioid receptor expressed in CHO-K1 cells assessed as ERK phosphorylation incubated for 2 hrs by Alphascreen surefire method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conopeptide-Derived κ-Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 6.79 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5281912 | — | — | 1 | 9.44 |
| CHEMBL5282326 | — | — | 1 | 9.21 |
| CHEMBL5273273 | — | — | 1 | 9.02 |
| CHEMBL5289642 | — | — | 1 | 6.35 |
| CHEMBL5268886 | — | — | 1 | 5.96 |
| CHEMBL5267287 | — | — | 1 | 5.80 |
| CHEMBL5281790 | — | — | 1 | 5.23 |
| CHEMBL5283510 | — | — | 1 | 5.13 |
| CHEMBL5282726 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5281912 | — | EC50 | = | 0.36 | nM | 9.44 |
| CHEMBL5282326 | — | EC50 | = | 0.62 | nM | 9.21 |
| CHEMBL5273273 | — | EC50 | = | 0.95 | nM | 9.02 |
| CHEMBL5289642 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5268886 | — | EC50 | = | 1105.0 | nM | 5.96 |
| CHEMBL5267287 | — | EC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL5281790 | — | EC50 | = | 5864.0 | nM | 5.23 |
| CHEMBL5283510 | — | EC50 | = | 7486.0 | nM | 5.13 |
| CHEMBL5282726 | — | EC50 | = | 9848.0 | nM | 5.01 |