Assay Detail
Functional
CHEMBL4683609
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay
14
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
The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.80 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744389 | — | — | 1 | 6.22 |
| CHEMBL4740282 | — | — | 1 | 6.19 |
| CHEMBL461384 | — | — | 1 | 6.19 |
| CHEMBL4750433 | — | — | 1 | 6.08 |
| CHEMBL4784857 | — | — | 1 | 5.85 |
| CHEMBL4749117 | — | — | 1 | 5.85 |
| CHEMBL4782382 | — | — | 1 | 5.84 |
| CHEMBL4776485 | — | — | 1 | 5.73 |
| CHEMBL4795875 | — | — | 1 | 5.71 |
| CHEMBL4764779 | — | — | 1 | 5.65 |
| CHEMBL4785060 | — | — | 1 | 5.59 |
| CHEMBL4743350 | — | — | 1 | 5.50 |
| CHEMBL4745258 | — | — | 1 | 5.40 |
| CHEMBL4751384 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744389 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4740282 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL461384 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4750433 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4784857 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4749117 | — | EC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4782382 | — | EC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL4776485 | — | EC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4795875 | — | EC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL4764779 | — | EC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL4785060 | — | EC50 | = | 2560.0 | nM | 5.59 |
| CHEMBL4743350 | — | EC50 | = | 3130.0 | nM | 5.50 |
| CHEMBL4745258 | — | EC50 | = | 3990.0 | nM | 5.40 |
| CHEMBL4751384 | — | EC50 | = | 4020.0 | nM | 5.40 |