Assay Detail
Binding
CHEMBL1815137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of human PPARgamma 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 gamma (CHEMBL235) ↗| 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 | 9.00 | 10.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1813011 | — | — | 1 | 10.74 |
| CHEMBL1813008 | — | — | 1 | 10.30 |
| CHEMBL1813009 | — | — | 1 | 9.22 |
| CHEMBL1813004 | — | — | 1 | 8.57 |
| CHEMBL1813007 | — | — | 1 | 8.52 |
| CHEMBL1813012 | — | — | 1 | 8.35 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.30 |
| CHEMBL1813003 | — | — | 1 | - |
| CHEMBL1813005 | — | — | 1 | - |
| CHEMBL1813006 | — | — | 1 | - |
| CHEMBL1813010 | — | — | 1 | - |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1813011 | — | EC50 | = | 0.018 | nM | 10.74 |
| CHEMBL1813008 | — | EC50 | = | 0.05 | nM | 10.30 |
| CHEMBL1813009 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1813004 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1813007 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1813012 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1813003 | — | EC50 | = | 0.0015 | nM | - |
| CHEMBL1813005 | — | EC50 | = | 0.0003 | nM | - |
| CHEMBL1813006 | — | EC50 | = | 0.0002 | nM | - |
| CHEMBL1813010 | — | EC50 | = | 0.0001 | nM | - |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | - | — | - |