Assay Detail
Functional
CHEMBL3387656
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glucose-dependent insulinotropic receptor (CHEMBL5263) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 7.75 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354777 | — | — | 1 | 8.10 |
| CHEMBL3354778 | — | — | 1 | 8.10 |
| CHEMBL3354780 | — | — | 1 | 8.05 |
| CHEMBL3354774 | — | — | 1 | 7.96 |
| CHEMBL3354784 | — | — | 1 | 7.96 |
| CHEMBL3354791 | — | — | 1 | 7.85 |
| CHEMBL3354788 | — | — | 1 | 7.82 |
| CHEMBL3354779 | — | — | 1 | 7.77 |
| CHEMBL3354776 | — | — | 1 | 7.62 |
| CHEMBL3354789 | — | — | 1 | 7.60 |
| CHEMBL3354781 | — | — | 1 | 7.57 |
| CHEMBL3354790 | — | — | 1 | 7.46 |
| CHEMBL3354793 | — | — | 1 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354777 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3354778 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3354780 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3354774 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3354784 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3354791 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3354788 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3354779 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3354776 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3354789 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3354781 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3354790 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3354793 | — | EC50 | = | 135.0 | nM | 6.87 |