Assay Detail
Functional
CHEMBL3387010
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glucose-dependent insulinotropic receptor (CHEMBL5652) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 33 | 7.83 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354778 | — | — | 1 | 9.30 |
| CHEMBL3354774 | — | — | 1 | 9.00 |
| CHEMBL3354801 | — | — | 1 | 8.70 |
| CHEMBL3354795 | — | — | 1 | 8.70 |
| CHEMBL3354779 | — | — | 1 | 8.70 |
| CHEMBL3354804 | — | — | 1 | 8.70 |
| CHEMBL3354777 | — | — | 1 | 8.52 |
| CHEMBL3354780 | — | — | 1 | 8.52 |
| CHEMBL3354784 | — | — | 1 | 8.52 |
| CHEMBL3354791 | — | — | 1 | 8.52 |
| CHEMBL3354798 | — | — | 1 | 8.30 |
| CHEMBL3354805 | — | — | 1 | 8.22 |
| CHEMBL3354786 | — | — | 1 | 8.15 |
| CHEMBL3354781 | — | — | 1 | 8.10 |
| CHEMBL3354788 | — | — | 1 | 7.96 |
| CHEMBL3354799 | — | — | 1 | 7.82 |
| CHEMBL3354803 | — | — | 1 | 7.70 |
| CHEMBL3354787 | — | — | 1 | 7.70 |
| CHEMBL3354797 | — | — | 1 | 7.68 |
| CHEMBL3354776 | — | — | 1 | 7.64 |
| CHEMBL3354789 | — | — | 1 | 7.60 |
| CHEMBL3354790 | — | — | 1 | 7.47 |
| CHEMBL3354802 | — | — | 1 | 7.46 |
| CHEMBL3352841 | — | — | 1 | 7.42 |
| CHEMBL3354793 | — | — | 1 | 7.14 |
| CHEMBL3354782 | — | — | 1 | 7.13 |
| CHEMBL3354783 | — | — | 1 | 7.00 |
| CHEMBL3354785 | — | — | 1 | 6.90 |
| CHEMBL3354792 | — | — | 1 | 6.67 |
| CHEMBL3354794 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354778 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3354774 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3354801 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3354795 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3354779 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3354804 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3354777 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3354780 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3354784 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3354791 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3354798 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3354805 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3354786 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3354781 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3354788 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3354799 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3354803 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3354787 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3354797 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3354776 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3354789 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3354790 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3354802 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3352841 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3354793 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3354782 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3354783 | — | EC50 | = | 101.0 | nM | 7.00 |
| CHEMBL3354785 | — | EC50 | = | 125.0 | nM | 6.90 |
| CHEMBL3354792 | — | EC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3354794 | — | EC50 | = | 298.0 | nM | 6.53 |
| CHEMBL3354796 | — | EC50 | = | 436.0 | nM | 6.36 |
| CHEMBL3354800 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3354775 | — | EC50 | > | 10.0 | nM | - |