Assay Detail
Functional
CHEMBL1052140
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha expressed in HEK293 cells assessed as receptor transactivation at by luciferase reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor alpha agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 4.72 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL21241 | GW7647 | — | 1 | 6.70 |
| CHEMBL573895 | — | — | 1 | 5.75 |
| CHEMBL567390 | — | — | 1 | 5.72 |
| CHEMBL583973 | — | — | 1 | 5.60 |
| CHEMBL566082 | — | — | 1 | 5.03 |
| CHEMBL573896 | — | — | 1 | 5.03 |
| CHEMBL575755 | — | — | 1 | 5.01 |
| CHEMBL583932 | — | — | 1 | 4.84 |
| CHEMBL575347 | — | — | 1 | 4.83 |
| CHEMBL583774 | — | — | 1 | 4.48 |
| CHEMBL574122 | — | — | 1 | 4.45 |
| CHEMBL572676 | — | — | 1 | 4.44 |
| CHEMBL575126 | — | — | 1 | 4.41 |
| CHEMBL575553 | — | — | 1 | 4.34 |
| CHEMBL572674 | — | — | 1 | 4.34 |
| CHEMBL575111 | — | — | 1 | 4.33 |
| CHEMBL683 | CLOFIBRIC ACID | 2.0 | 1 | 4.26 |
| CHEMBL583796 | — | — | 1 | 4.25 |
| CHEMBL572662 | — | — | 1 | 4.24 |
| CHEMBL566081 | — | — | 1 | 4.20 |
| CHEMBL583065 | — | — | 1 | 4.16 |
| CHEMBL567389 | — | — | 1 | 4.13 |
| CHEMBL575316 | — | — | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL21241 | GW7647 | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL573895 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL567390 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL583973 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL566082 | — | EC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL573896 | — | EC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL575755 | — | EC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL583932 | — | EC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL575347 | — | EC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL583774 | — | EC50 | = | 33300.0 | nM | 4.48 |
| CHEMBL574122 | — | EC50 | = | 35900.0 | nM | 4.45 |
| CHEMBL572676 | — | EC50 | = | 36100.0 | nM | 4.44 |
| CHEMBL575126 | — | EC50 | = | 38900.0 | nM | 4.41 |
| CHEMBL575553 | — | EC50 | = | 45800.0 | nM | 4.34 |
| CHEMBL572674 | — | EC50 | = | 45800.0 | nM | 4.34 |
| CHEMBL575111 | — | EC50 | = | 46300.0 | nM | 4.33 |
| CHEMBL683 | CLOFIBRIC ACID | EC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL583796 | — | EC50 | = | 55900.0 | nM | 4.25 |
| CHEMBL572662 | — | EC50 | = | 57300.0 | nM | 4.24 |
| CHEMBL566081 | — | EC50 | = | 62500.0 | nM | 4.20 |
| CHEMBL583065 | — | EC50 | = | 69300.0 | nM | 4.16 |
| CHEMBL567389 | — | EC50 | = | 73500.0 | nM | 4.13 |
| CHEMBL575316 | — | EC50 | = | 84300.0 | nM | 4.07 |