Assay Detail
Binding
CHEMBL4236816
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay
8
Total Activities
8
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
Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 5.73 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.41 |
| CHEMBL4237252 | — | — | 1 | 6.92 |
| CHEMBL191275 | — | — | 1 | 6.26 |
| CHEMBL4248276 | — | — | 1 | 6.05 |
| CHEMBL4251393 | — | — | 1 | 5.01 |
| CHEMBL4243327 | — | — | 1 | 4.82 |
| CHEMBL4247103 | — | — | 1 | 4.75 |
| CHEMBL4242324 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4237252 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL191275 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4248276 | — | EC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4251393 | — | EC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL4243327 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4247103 | — | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4242324 | — | EC50 | = | 25000.0 | nM | 4.60 |