Assay Detail
Functional
CHEMBL887396
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding
24
Total Activities
12
Compounds Tested
2
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
High-affinity carbamate analogues of morphinan at opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Emax | 12 | - | - |
| EC50 | 12 | 8.26 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL397035 | — | — | 2 | 9.36 |
| CHEMBL49269 | CYCLORPHAN | — | 2 | 9.10 |
| CHEMBL242048 | — | — | 2 | 8.89 |
| CHEMBL301160 | BUTORPHAN | — | 2 | 8.80 |
| CHEMBL263096 | — | — | 2 | 8.66 |
| CHEMBL427862 | — | — | 2 | 8.62 |
| CHEMBL394624 | — | — | 2 | 8.15 |
| CHEMBL242046 | — | — | 2 | 7.96 |
| CHEMBL241824 | — | — | 2 | 7.85 |
| CHEMBL242047 | — | — | 2 | 7.41 |
| CHEMBL245049 | — | — | 2 | 7.30 |
| CHEMBL38874 | DAMGO | — | 2 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL397035 | — | EC50 | = | 0.44 | nM | 9.36 |
| CHEMBL49269 | CYCLORPHAN | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL242048 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL301160 | BUTORPHAN | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL263096 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL427862 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL394624 | — | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL242046 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL241824 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL242047 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL245049 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL38874 | DAMGO | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL38874 | DAMGO | Emax | = | 120.0 | % | - |
| CHEMBL245049 | — | Emax | = | 71.0 | % | - |
| CHEMBL394624 | — | Emax | = | 54.0 | % | - |
| CHEMBL49269 | CYCLORPHAN | Emax | = | 40.0 | % | - |
| CHEMBL242048 | — | Emax | = | 80.0 | % | - |
| CHEMBL241824 | — | Emax | = | 44.0 | % | - |
| CHEMBL242047 | — | Emax | = | 32.0 | % | - |
| CHEMBL427862 | — | Emax | = | 40.0 | % | - |
| CHEMBL242046 | — | Emax | = | 60.0 | % | - |
| CHEMBL397035 | — | Emax | = | 39.0 | % | - |
| CHEMBL301160 | BUTORPHAN | Emax | = | 50.0 | % | - |
| CHEMBL263096 | — | Emax | = | 39.0 | % | - |