Assay Detail
Functional
CHEMBL863310
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
44
Total Activities
11
Compounds Tested
4
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 | 8.28 | 9.10 |
| Imax | 11 | - | - |
| IC50 | 11 | 7.18 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 4 | 9.10 |
| CHEMBL301160 | BUTORPHAN | — | 4 | 8.80 |
| CHEMBL199931 | — | — | 4 | 8.60 |
| CHEMBL201271 | — | — | 4 | 8.54 |
| CHEMBL383320 | — | — | 4 | 8.52 |
| CHEMBL200881 | — | — | 4 | 8.36 |
| CHEMBL199827 | — | — | 4 | 8.29 |
| CHEMBL369919 | — | — | 4 | 7.92 |
| CHEMBL381750 | — | — | 4 | 7.72 |
| CHEMBL38874 | DAMGO | — | 4 | 6.96 |
| CHEMBL193039 | — | — | 4 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL301160 | BUTORPHAN | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL49269 | CYCLORPHAN | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL199931 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL201271 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL383320 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL200881 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL199827 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL369919 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL381750 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL301160 | BUTORPHAN | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL201271 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL38874 | DAMGO | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL200881 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL369919 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL193039 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL199827 | — | Imax | - | — | - | |
| CHEMBL199827 | — | IC50 | - | — | - | |
| CHEMBL199931 | — | Emax | = | 110.0 | % | - |
| CHEMBL199931 | — | Imax | - | — | - | |
| CHEMBL199931 | — | IC50 | - | — | - | |
| CHEMBL201271 | — | Emax | = | 41.0 | % | - |
| CHEMBL200881 | — | Imax | = | 61.0 | % | - |
| CHEMBL201271 | — | Imax | = | 64.0 | % | - |
| CHEMBL200881 | — | Emax | = | 56.0 | % | - |
| CHEMBL193039 | — | Emax | = | 28.0 | % | - |
| CHEMBL193039 | — | EC50 | - | — | - | |
| CHEMBL193039 | — | Imax | = | 71.0 | % | - |
| CHEMBL199827 | — | Emax | = | 93.0 | % | - |
| CHEMBL49269 | CYCLORPHAN | Imax | = | 50.0 | % | - |
| CHEMBL38874 | DAMGO | Emax | = | 120.0 | % | - |
| CHEMBL301160 | BUTORPHAN | Imax | = | 50.0 | % | - |
| CHEMBL38874 | DAMGO | Imax | - | — | - | |
| CHEMBL301160 | BUTORPHAN | Emax | = | 50.0 | % | - |
| CHEMBL369919 | — | Imax | = | 48.0 | % | - |
| CHEMBL383320 | — | Emax | = | 110.0 | % | - |
| CHEMBL369919 | — | Emax | = | 69.0 | % | - |
| CHEMBL381750 | — | IC50 | - | — | - | |
| CHEMBL381750 | — | Imax | - | — | - | |
| CHEMBL49269 | CYCLORPHAN | Emax | = | 40.0 | % | - |
| CHEMBL381750 | — | Emax | = | 96.0 | % | - |
| CHEMBL383320 | — | IC50 | - | — | - | |
| CHEMBL383320 | — | Imax | - | — | - | |
| CHEMBL38874 | DAMGO | IC50 | - | — | - |