Assay Detail
Functional
CHEMBL3869508
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 stimulation of cAMP level measured after 60 mins by HTRF assay
18
Total Activities
18
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
Novel 5-nitropyrimidine derivatives bearing endo-azabicyclic alcohols/amines as potent GPR119 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 8.16 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3893596 | — | — | 1 | 9.22 |
| CHEMBL3912040 | — | — | 1 | 8.89 |
| CHEMBL3982536 | — | — | 1 | 8.85 |
| CHEMBL3914281 | — | — | 1 | 8.82 |
| CHEMBL3951013 | — | — | 1 | 8.82 |
| CHEMBL3904015 | — | — | 1 | 8.80 |
| CHEMBL3946188 | — | — | 1 | 8.46 |
| CHEMBL3930728 | — | — | 1 | 8.21 |
| CHEMBL3894993 | — | — | 1 | 7.36 |
| CHEMBL3978259 | — | — | 1 | 6.69 |
| CHEMBL280065 | OLEOYLETHANOLAMIDE | — | 1 | 5.66 |
| CHEMBL3894674 | — | — | 1 | - |
| CHEMBL3923279 | — | — | 1 | - |
| CHEMBL3921610 | — | — | 1 | - |
| CHEMBL3966031 | — | — | 1 | - |
| CHEMBL3903618 | — | — | 1 | - |
| CHEMBL3986478 | — | — | 1 | - |
| CHEMBL3949135 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3893596 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3912040 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3982536 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3914281 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3951013 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3904015 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3946188 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3930728 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3894993 | — | EC50 | = | 44.2 | nM | 7.36 |
| CHEMBL3978259 | — | EC50 | = | 205.0 | nM | 6.69 |
| CHEMBL280065 | OLEOYLETHANOLAMIDE | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3894674 | — | EC50 | > | 2000.0 | nM | - |
| CHEMBL3923279 | — | EC50 | > | 2000.0 | nM | - |
| CHEMBL3921610 | — | EC50 | > | 2000.0 | nM | - |
| CHEMBL3966031 | — | EC50 | > | 2000.0 | nM | - |
| CHEMBL3903618 | — | EC50 | > | 2000.0 | nM | - |
| CHEMBL3986478 | — | EC50 | > | 2000.0 | nM | - |
| CHEMBL3949135 | — | EC50 | > | 2000.0 | nM | - |