Assay Detail
Binding
CHEMBL2320327
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.06 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.41 |
| CHEMBL2312713 | — | — | 1 | 6.34 |
| CHEMBL191275 | — | — | 1 | 6.26 |
| CHEMBL2312712 | — | — | 1 | 6.23 |
| CHEMBL2312715 | — | — | 1 | 6.19 |
| CHEMBL2312707 | — | — | 1 | 6.16 |
| CHEMBL2312708 | — | — | 1 | 6.16 |
| CHEMBL2312716 | — | — | 1 | 6.16 |
| CHEMBL2312702 | — | — | 1 | 6.00 |
| CHEMBL2312717 | — | — | 1 | 6.00 |
| CHEMBL2312701 | — | — | 1 | 5.92 |
| CHEMBL2312714 | — | — | 1 | 5.87 |
| CHEMBL2312718 | — | — | 1 | 5.85 |
| CHEMBL2312710 | — | — | 1 | 5.69 |
| CHEMBL2312700 | — | — | 1 | 5.64 |
| CHEMBL2312711 | — | — | 1 | 5.59 |
| CHEMBL2312709 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2312713 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL191275 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2312712 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL2312715 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2312707 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2312708 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2312716 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL2312702 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2312717 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2312701 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2312714 | — | EC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL2312718 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2312710 | — | EC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL2312700 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2312711 | — | EC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL2312709 | — | EC50 | = | 3100.0 | nM | 5.51 |