Assay Detail
Functional
CHEMBL958395
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Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Syntheses of novel high affinity ligands for opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 8.03 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL470005 | — | — | 1 | 8.64 |
| CHEMBL511645 | — | — | 1 | 8.57 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.48 |
| CHEMBL471243 | — | — | 1 | 8.48 |
| CHEMBL471048 | — | — | 1 | 8.41 |
| CHEMBL512150 | — | — | 1 | 8.41 |
| CHEMBL470617 | NALTREXONE METHIODIDE | — | 1 | 8.05 |
| CHEMBL398707 | HYDROMORPHONE | 4.0 | 1 | 7.96 |
| CHEMBL290543 | — | — | 1 | 7.44 |
| CHEMBL895 | NALBUPHINE | 4.0 | 1 | 7.25 |
| CHEMBL513762 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL470005 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL511645 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL19019 | NALTREXONE | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL471243 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL471048 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL512150 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL470617 | NALTREXONE METHIODIDE | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL398707 | HYDROMORPHONE | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL290543 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL895 | NALBUPHINE | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL513762 | — | EC50 | = | 220.0 | nM | 6.66 |