Assay Detail
Functional
CHEMBL861891
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells
50
Total Activities
18
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 32 | 7.47 | 9.34 |
| Emax | 16 | - | - |
| Log EC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL208479 | — | — | 3 | 9.34 |
| CHEMBL382051 | — | — | 3 | 8.85 |
| CHEMBL336381 | — | — | 3 | 8.70 |
| CHEMBL262172 | — | — | 3 | 7.93 |
| CHEMBL382349 | — | — | 3 | 7.75 |
| CHEMBL205306 | — | — | 3 | 7.70 |
| CHEMBL218763 | — | — | 3 | 7.66 |
| CHEMBL38874 | DAMGO | — | 3 | 7.44 |
| CHEMBL206974 | — | — | 3 | 7.42 |
| CHEMBL379405 | — | — | 3 | 7.35 |
| CHEMBL407057 | — | — | 3 | 7.09 |
| CHEMBL408330 | — | — | 3 | 6.96 |
| CHEMBL408083 | — | — | 3 | 6.60 |
| CHEMBL383458 | — | — | 3 | 6.46 |
| CHEMBL218327 | — | — | 3 | 6.28 |
| CHEMBL205965 | — | — | 3 | 6.05 |
| CHEMBL382409 | — | — | 1 | - |
| CHEMBL31421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL208479 | — | EC50 | = | 0.46 | nM | 9.34 |
| CHEMBL208479 | — | EC50 | = | 0.4571 | nM | 9.34 |
| CHEMBL382051 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL382051 | — | EC50 | = | 1.445 | nM | 8.84 |
| CHEMBL336381 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL336381 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL262172 | — | EC50 | = | 11.75 | nM | 7.93 |
| CHEMBL262172 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL382349 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL382349 | — | EC50 | = | 17.78 | nM | 7.75 |
| CHEMBL205306 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL205306 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL218763 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL218763 | — | EC50 | = | 22.39 | nM | 7.65 |
| CHEMBL38874 | DAMGO | EC50 | = | 36.31 | nM | 7.44 |
| CHEMBL38874 | DAMGO | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL206974 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL206974 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL379405 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL379405 | — | EC50 | = | 45.71 | nM | 7.34 |
| CHEMBL407057 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL407057 | — | EC50 | = | 81.28 | nM | 7.09 |
| CHEMBL408330 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL408330 | — | EC50 | = | 109.65 | nM | 6.96 |
| CHEMBL408083 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL408083 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL383458 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL383458 | — | EC50 | = | 354.81 | nM | 6.45 |
| CHEMBL218327 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL218327 | — | EC50 | = | 524.81 | nM | 6.28 |
| CHEMBL205965 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL205965 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL382409 | — | Log EC50 | - | — | - | |
| CHEMBL379405 | — | Emax | = | 160.0 | % | - |
| CHEMBL218327 | — | Emax | = | 50.0 | % | - |
| CHEMBL205965 | — | Emax | = | 210.0 | % | - |
| CHEMBL382051 | — | Emax | = | 180.0 | % | - |
| CHEMBL408083 | — | Emax | = | 47.0 | % | - |
| CHEMBL408330 | — | Emax | = | 70.0 | % | - |
| CHEMBL383458 | — | Emax | = | 110.0 | % | - |
| CHEMBL336381 | — | Emax | = | 100.0 | % | - |
| CHEMBL382349 | — | Emax | = | 73.0 | % | - |
| CHEMBL206974 | — | Emax | = | 44.0 | % | - |
| CHEMBL205306 | — | Emax | = | 110.0 | % | - |
| CHEMBL218763 | — | Emax | = | 300.0 | % | - |
| CHEMBL31421 | — | Log EC50 | - | — | - | |
| CHEMBL407057 | — | Emax | = | 91.0 | % | - |
| CHEMBL208479 | — | Emax | = | 88.0 | % | - |
| CHEMBL38874 | DAMGO | Emax | = | 150.0 | % | - |
| CHEMBL262172 | — | Emax | = | 86.0 | % | - |