Assay Detail
Functional
CHEMBL4018045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
21
Total Activities
14
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 |
Target
Glucose-dependent insulinotropic receptor (CHEMBL5652) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of pyrimidine derivatives with diverse azabicyclic ether/amine as novel GPR119 agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 7.66 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098760 | — | — | 1 | 8.92 |
| CHEMBL4078300 | — | — | 2 | 8.74 |
| CHEMBL4063625 | — | — | 2 | 8.51 |
| CHEMBL4065265 | — | — | 2 | 8.31 |
| CHEMBL4067982 | — | — | 1 | 8.25 |
| CHEMBL4062726 | — | — | 2 | 8.25 |
| CHEMBL4067384 | — | — | 2 | 7.32 |
| CHEMBL4078851 | — | — | 2 | 7.28 |
| CHEMBL4095373 | — | — | 1 | 7.11 |
| CHEMBL4080761 | — | — | 1 | 6.96 |
| CHEMBL4086187 | — | — | 1 | 6.50 |
| CHEMBL280065 | OLEOYLETHANOLAMIDE | — | 1 | 5.66 |
| CHEMBL4071750 | — | — | 1 | - |
| CHEMBL4088637 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098760 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4078300 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4063625 | — | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4065265 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4078300 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4067982 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4062726 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4062726 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4067384 | — | EC50 | = | 48.2 | nM | 7.32 |
| CHEMBL4078851 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4095373 | — | EC50 | = | 77.7 | nM | 7.11 |
| CHEMBL4080761 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4078851 | — | EC50 | = | 236.0 | nM | 6.63 |
| CHEMBL4086187 | — | EC50 | = | 315.0 | nM | 6.50 |
| CHEMBL280065 | OLEOYLETHANOLAMIDE | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4071750 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4065265 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4088637 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4088637 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4067384 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4063625 | — | EC50 | > | 10000.0 | nM | - |