Assay Detail
Functional
CHEMBL3611625
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Agonist activity at rat mu opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay
20
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 7.71 | 8.80 |
| Emax | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3609620 | — | — | 2 | 8.80 |
| CHEMBL3609621 | — | — | 2 | 8.28 |
| CHEMBL3608939 | — | — | 2 | 8.26 |
| CHEMBL3609618 | — | — | 2 | 8.15 |
| CHEMBL3609617 | — | — | 2 | 7.64 |
| CHEMBL3608938 | — | — | 2 | 7.60 |
| CHEMBL3609615 | — | — | 2 | 7.39 |
| CHEMBL3608937 | — | — | 2 | 7.23 |
| CHEMBL3609616 | — | — | 2 | 7.00 |
| CHEMBL3609619 | — | — | 2 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3609620 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3609621 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3608939 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3609618 | — | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3609617 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3608938 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3609615 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3608937 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3609616 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3609619 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3608937 | — | Emax | = | 70.0 | % | - |
| CHEMBL3608938 | — | Emax | = | 38.0 | % | - |
| CHEMBL3608939 | — | Emax | = | 58.0 | % | - |
| CHEMBL3609615 | — | Emax | = | 16.0 | % | - |
| CHEMBL3609616 | — | Emax | = | 14.0 | % | - |
| CHEMBL3609617 | — | Emax | = | 34.0 | % | - |
| CHEMBL3609618 | — | Emax | = | 58.0 | % | - |
| CHEMBL3609619 | — | Emax | = | 26.0 | % | - |
| CHEMBL3609620 | — | Emax | = | 49.0 | % | - |
| CHEMBL3609621 | — | Emax | = | 50.0 | % | - |