Assay Detail
Functional
CHEMBL863309
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
32
Total Activities
11
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Emax | 11 | - | - |
| EC50 | 11 | 8.38 | 9.72 |
| Imax | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 3 | 9.72 |
| CHEMBL301160 | BUTORPHAN | — | 3 | 8.89 |
| CHEMBL199931 | — | — | 3 | 8.64 |
| CHEMBL201271 | — | — | 3 | 8.60 |
| CHEMBL383320 | — | — | 3 | 8.55 |
| CHEMBL199827 | — | — | 3 | 8.42 |
| CHEMBL193039 | — | — | 3 | 8.10 |
| CHEMBL369919 | — | — | 3 | 8.06 |
| CHEMBL200881 | — | — | 2 | 8.06 |
| CHEMBL381750 | — | — | 3 | 7.77 |
| CHEMBL58033 | (-)-U-50488 | — | 3 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | EC50 | = | 0.19 | nM | 9.72 |
| CHEMBL301160 | BUTORPHAN | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL199931 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL201271 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL383320 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL199827 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL193039 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL369919 | — | EC50 | = | 8.8 | nM | 8.06 |
| CHEMBL200881 | — | EC50 | = | 8.8 | nM | 8.06 |
| CHEMBL381750 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL58033 | (-)-U-50488 | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL58033 | (-)-U-50488 | Imax | - | — | - | |
| CHEMBL49269 | CYCLORPHAN | Emax | = | 90.0 | % | - |
| CHEMBL49269 | CYCLORPHAN | Imax | - | — | - | |
| CHEMBL301160 | BUTORPHAN | Emax | = | 80.0 | % | - |
| CHEMBL301160 | BUTORPHAN | Imax | - | — | - | |
| CHEMBL369919 | — | Emax | = | 140.0 | % | - |
| CHEMBL200881 | — | Emax | = | 55.0 | % | - |
| CHEMBL199827 | — | Emax | = | 170.0 | % | - |
| CHEMBL199827 | — | Imax | - | — | - | |
| CHEMBL199931 | — | Emax | = | 150.0 | % | - |
| CHEMBL199931 | — | Imax | - | — | - | |
| CHEMBL201271 | — | Emax | = | 110.0 | % | - |
| CHEMBL201271 | — | Imax | - | — | - | |
| CHEMBL58033 | (-)-U-50488 | Emax | = | 110.0 | % | - |
| CHEMBL193039 | — | Emax | = | 77.0 | % | - |
| CHEMBL381750 | — | Imax | - | — | - | |
| CHEMBL193039 | — | Imax | - | — | - | |
| CHEMBL381750 | — | Emax | = | 91.0 | % | - |
| CHEMBL383320 | — | Emax | = | 75.0 | % | - |
| CHEMBL369919 | — | Imax | - | — | - | |
| CHEMBL383320 | — | Imax | - | — | - |