Assay Detail
Functional
CHEMBL4478047
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Agonist activity at human NPY Y4 receptor expressed in HEK293 cells co-expressing CRE-Luc gene assessed as inhibition of forskolin stimulated luciferase activity after 4.5 hrs by luminescence assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
High Affinity Agonists of the Neuropeptide Y (NPY) Y4 Receptor Derived from the C-Terminal Pentapeptide of Human Pancreatic Polypeptide (hPP): Synthesis, Stereochemical Discrimination, and Radiolabeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 7.95 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4540843 | PANCREATIC POLYPEPTIDE | 2.0 | 1 | 9.14 |
| CHEMBL4456247 | — | — | 1 | 8.80 |
| CHEMBL3787712 | — | — | 1 | 8.77 |
| CHEMBL4522438 | — | — | 1 | 8.40 |
| CHEMBL409762 | — | — | 1 | 8.26 |
| CHEMBL3787713 | — | — | 1 | 8.15 |
| CHEMBL4475071 | — | — | 1 | 7.72 |
| CHEMBL4549208 | — | — | 1 | 7.57 |
| CHEMBL3787766 | — | — | 1 | 7.07 |
| CHEMBL4533775 | — | — | 1 | 6.82 |
| CHEMBL4581256 | — | — | 1 | 6.80 |
| CHEMBL4576579 | — | — | 1 | - |
| CHEMBL4581302 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4540843 | PANCREATIC POLYPEPTIDE | EC50 | = | 0.73 | nM | 9.14 |
| CHEMBL4456247 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3787712 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4522438 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL409762 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3787713 | — | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4475071 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4549208 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3787766 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4533775 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4581256 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4576579 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL4581302 | — | EC50 | > | 3000.0 | nM | - |