Assay Detail
Binding
CHEMBL996816
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
5
Total Activities
5
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 alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 5.27 | 6.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 6.09 |
| CHEMBL485942 | — | — | 1 | 5.60 |
| CHEMBL270960 | — | — | 1 | 5.16 |
| CHEMBL520856 | — | — | 1 | 4.82 |
| CHEMBL487561 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL485942 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL270960 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL520856 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL487561 | — | EC50 | = | 20000.0 | nM | 4.70 |