Assay Detail
Functional
CHEMBL1035295
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.60 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL562864 | — | — | 1 | 8.70 |
| CHEMBL558083 | — | — | 2 | 6.97 |
| CHEMBL560830 | — | — | 1 | 6.73 |
| CHEMBL552240 | — | — | 1 | 6.64 |
| CHEMBL461571 | — | — | 1 | 6.50 |
| CHEMBL564902 | — | — | 1 | 6.43 |
| CHEMBL564036 | — | — | 1 | 6.42 |
| CHEMBL549746 | — | — | 1 | 6.30 |
| CHEMBL672 | FENOFIBRATE | 4.0 | 1 | 5.70 |
| CHEMBL452051 | — | — | 1 | 5.31 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
| CHEMBL560160 | — | — | 1 | - |
| CHEMBL559567 | — | — | 1 | - |
| CHEMBL556073 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL562864 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL558083 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL558083 | — | EC50 | = | 129.0 | nM | 6.89 |
| CHEMBL560830 | — | EC50 | = | 185.0 | nM | 6.73 |
| CHEMBL552240 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL461571 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL564902 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL564036 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL549746 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL672 | FENOFIBRATE | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL452051 | — | EC50 | = | 4890.0 | nM | 5.31 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | > | 3000.0 | nM | - |
| CHEMBL560160 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL559567 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL556073 | — | EC50 | > | 3000.0 | nM | - |