Assay Detail
Functional
CHEMBL4812956
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR119 expressed in CHO cells co-expressing cyclic AMP response element-luciferase reporter gene incubated for 2 hrs by steady-glo luciferase assay
21
Total Activities
21
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
Discovery of a novel series of GPR119 agonists: Design, synthesis, and biological evaluation of N-(Piperidin-4-yl)-N-(trifluoromethyl)pyrimidin-4-amine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 7.57 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4875358 | — | — | 1 | 8.60 |
| CHEMBL4851479 | — | — | 1 | 8.57 |
| CHEMBL4869157 | — | — | 1 | 8.54 |
| CHEMBL4855738 | — | — | 1 | 8.44 |
| CHEMBL4870635 | — | — | 1 | 8.34 |
| CHEMBL4846307 | — | — | 1 | 8.27 |
| CHEMBL3113629 | — | — | 1 | 8.08 |
| CHEMBL4861760 | — | — | 1 | 7.85 |
| CHEMBL4779950 | — | — | 1 | 7.80 |
| CHEMBL3113840 | — | — | 1 | 7.77 |
| CHEMBL4877468 | — | — | 1 | 7.75 |
| CHEMBL4871114 | — | — | 1 | 7.68 |
| CHEMBL4873459 | — | — | 1 | 7.54 |
| CHEMBL4876465 | — | — | 1 | 7.37 |
| CHEMBL4858330 | — | — | 1 | 7.29 |
| CHEMBL3113626 | — | — | 1 | 7.17 |
| CHEMBL4846489 | — | — | 1 | 6.57 |
| CHEMBL4856239 | — | — | 1 | 6.52 |
| CHEMBL4857801 | — | — | 1 | 6.02 |
| CHEMBL4851910 | — | — | 1 | 5.15 |
| CHEMBL4853684 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4875358 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4851479 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4869157 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4855738 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4870635 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4846307 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3113629 | — | EC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4861760 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4779950 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3113840 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4877468 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4871114 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4873459 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4876465 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4858330 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3113626 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4846489 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4856239 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4857801 | — | EC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4851910 | — | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4853684 | — | EC50 | > | 10000.0 | nM | - |