Assay Detail
Functional
CHEMBL4738432
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 6.66 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL461384 | — | — | 1 | 8.22 |
| CHEMBL4784457 | — | — | 1 | 7.37 |
| CHEMBL4748865 | — | — | 1 | 7.12 |
| CHEMBL4741006 | — | — | 1 | 7.06 |
| CHEMBL4743968 | — | — | 1 | 6.98 |
| CHEMBL4751616 | — | — | 1 | 6.97 |
| CHEMBL4790521 | — | — | 1 | 6.90 |
| CHEMBL4779985 | — | — | 1 | 6.89 |
| CHEMBL4789532 | — | — | 1 | 6.81 |
| CHEMBL4744049 | — | — | 1 | 6.80 |
| CHEMBL4790469 | — | — | 1 | 6.14 |
| CHEMBL4777445 | — | — | 1 | 6.13 |
| CHEMBL4755177 | — | — | 1 | 6.10 |
| CHEMBL4760659 | — | — | 1 | 6.09 |
| CHEMBL4796294 | — | — | 1 | 6.09 |
| CHEMBL4782568 | — | — | 1 | 5.85 |
| CHEMBL4778466 | — | — | 1 | 5.73 |
| CHEMBL4782353 | — | — | 1 | - |
| CHEMBL4754701 | — | — | 1 | - |
| CHEMBL4789657 | — | — | 1 | - |
| CHEMBL4790432 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL461384 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4784457 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4748865 | — | EC50 | = | 75.1 | nM | 7.12 |
| CHEMBL4741006 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4743968 | — | EC50 | = | 105.7 | nM | 6.98 |
| CHEMBL4751616 | — | EC50 | = | 107.4 | nM | 6.97 |
| CHEMBL4790521 | — | EC50 | = | 125.3 | nM | 6.90 |
| CHEMBL4779985 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4789532 | — | EC50 | = | 153.4 | nM | 6.81 |
| CHEMBL4744049 | — | EC50 | = | 157.4 | nM | 6.80 |
| CHEMBL4790469 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4777445 | — | EC50 | = | 745.0 | nM | 6.13 |
| CHEMBL4755177 | — | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4760659 | — | EC50 | = | 805.0 | nM | 6.09 |
| CHEMBL4796294 | — | EC50 | = | 819.0 | nM | 6.09 |
| CHEMBL4782568 | — | EC50 | = | 1414.0 | nM | 5.85 |
| CHEMBL4778466 | — | EC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL4782353 | — | EC50 | - | — | - | |
| CHEMBL4754701 | — | EC50 | - | — | - | |
| CHEMBL4789657 | — | EC50 | - | — | - | |
| CHEMBL4790432 | — | EC50 | - | — | - |