Assay Detail
Binding
CHEMBL1815135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of human PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay
12
Total Activities
12
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
Revisiting glitazars: thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 8.36 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1813003 | — | — | 1 | 10.59 |
| CHEMBL1813008 | — | — | 1 | 10.00 |
| CHEMBL1813009 | — | — | 1 | 8.72 |
| CHEMBL1813004 | — | — | 1 | 8.52 |
| CHEMBL1813007 | — | — | 1 | 7.70 |
| CHEMBL1813012 | — | — | 1 | 7.66 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 5.32 |
| CHEMBL1813005 | — | — | 1 | - |
| CHEMBL1813006 | — | — | 1 | - |
| CHEMBL1813010 | — | — | 1 | - |
| CHEMBL1813011 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1813003 | — | EC50 | = | 0.026 | nM | 10.59 |
| CHEMBL1813008 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1813009 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1813004 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1813007 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1813012 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL1813005 | — | EC50 | = | 6e-05 | nM | - |
| CHEMBL1813006 | — | EC50 | = | 5e-05 | nM | - |
| CHEMBL1813010 | — | EC50 | = | 7e-05 | nM | - |
| CHEMBL1813011 | — | EC50 | = | 0.00031 | nM | - |
| CHEMBL121 | ROSIGLITAZONE | EC50 | - | — | - |