Assay Detail
Binding
CHEMBL1042379
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Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
22
Total Activities
22
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 | Intermediate |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 6.33 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489074 | — | — | 1 | 7.94 |
| CHEMBL572794 | — | — | 1 | 7.80 |
| CHEMBL578860 | — | — | 1 | 7.22 |
| CHEMBL572565 | — | — | 1 | 6.97 |
| CHEMBL489075 | — | — | 1 | 6.82 |
| CHEMBL572795 | — | — | 1 | 6.80 |
| CHEMBL191275 | — | — | 1 | 6.72 |
| CHEMBL573015 | — | — | 1 | 6.51 |
| CHEMBL574386 | — | — | 1 | 6.48 |
| CHEMBL573252 | — | — | 1 | 6.31 |
| CHEMBL572566 | — | — | 1 | 6.22 |
| CHEMBL574607 | — | — | 1 | 6.14 |
| CHEMBL574606 | — | — | 1 | 5.87 |
| CHEMBL574824 | — | — | 1 | 5.85 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 5.80 |
| CHEMBL573018 | — | — | 1 | 5.76 |
| CHEMBL573492 | — | — | 1 | 5.75 |
| CHEMBL583300 | — | — | 1 | 5.62 |
| CHEMBL583759 | — | — | 1 | 5.44 |
| CHEMBL981 | FENOFIBRIC ACID | 4.0 | 1 | 4.52 |
| CHEMBL575687 | — | — | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489074 | — | EC50 | = | 11.5 | nM | 7.94 |
| CHEMBL572794 | — | EC50 | = | 15.9 | nM | 7.80 |
| CHEMBL578860 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL572565 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL489075 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL572795 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL191275 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL573015 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL574386 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL573252 | — | EC50 | = | 488.0 | nM | 6.31 |
| CHEMBL572566 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL574607 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL574606 | — | EC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL574824 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL573018 | — | EC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL573492 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL583300 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL583759 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL981 | FENOFIBRIC ACID | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL575687 | — | EC50 | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | EC50 | - | — | - |