Assay Detail
Binding
CHEMBL1035759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
32
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CV-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 5.18 | 6.17 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL526740 | — | — | 1 | 6.17 |
| CHEMBL501335 | — | — | 1 | 5.64 |
| CHEMBL490425 | — | — | 1 | 5.57 |
| CHEMBL482827 | — | — | 1 | 5.56 |
| CHEMBL489765 | — | — | 1 | 5.54 |
| CHEMBL490426 | — | — | 1 | 5.53 |
| CHEMBL484263 | — | — | 1 | 5.51 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 5.50 |
| CHEMBL491627 | — | — | 1 | 5.49 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 5.46 |
| CHEMBL521925 | — | — | 1 | 5.40 |
| CHEMBL485291 | — | — | 1 | 5.40 |
| CHEMBL521289 | — | — | 1 | 5.39 |
| CHEMBL484462 | — | — | 1 | 5.36 |
| CHEMBL489766 | — | — | 1 | 5.25 |
| CHEMBL490832 | — | — | 1 | 5.23 |
| CHEMBL523650 | — | — | 1 | 5.17 |
| CHEMBL490220 | — | — | 1 | 5.14 |
| CHEMBL519857 | — | — | 1 | 4.95 |
| CHEMBL482824 | — | — | 1 | 4.92 |
| CHEMBL482823 | — | — | 1 | 4.88 |
| CHEMBL484063 | — | — | 1 | 4.67 |
| CHEMBL483032 | — | — | 1 | 4.61 |
| CHEMBL492047 | — | — | 1 | 4.52 |
| CHEMBL483035 | — | — | 1 | 4.43 |
| CHEMBL489559 | — | — | 1 | 4.35 |
| CHEMBL488991 | — | — | 1 | 4.23 |
| CHEMBL520305 | — | — | 1 | - |
| CHEMBL457 | GEMFIBROZIL | 4.0 | 1 | - |
| CHEMBL484264 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL526740 | — | EC50 | = | 674.0 | nM | 6.17 |
| CHEMBL501335 | — | EC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL490425 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL482827 | — | EC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL489765 | — | EC50 | = | 2910.0 | nM | 5.54 |
| CHEMBL490426 | — | EC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL484263 | — | EC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 3124.0 | nM | 5.50 |
| CHEMBL491627 | — | EC50 | = | 3260.0 | nM | 5.49 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL521925 | — | EC50 | = | 3990.0 | nM | 5.40 |
| CHEMBL485291 | — | EC50 | = | 3950.0 | nM | 5.40 |
| CHEMBL521289 | — | EC50 | = | 4060.0 | nM | 5.39 |
| CHEMBL484462 | — | EC50 | = | 4390.0 | nM | 5.36 |
| CHEMBL489766 | — | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL490832 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL523650 | — | EC50 | = | 6780.0 | nM | 5.17 |
| CHEMBL490220 | — | EC50 | = | 7220.0 | nM | 5.14 |
| CHEMBL519857 | — | EC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL482824 | — | EC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL482823 | — | EC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL484063 | — | EC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL483032 | — | EC50 | = | 24400.0 | nM | 4.61 |
| CHEMBL492047 | — | EC50 | = | 30400.0 | nM | 4.52 |
| CHEMBL483035 | — | EC50 | = | 37400.0 | nM | 4.43 |
| CHEMBL489559 | — | EC50 | = | 44500.0 | nM | 4.35 |
| CHEMBL488991 | — | EC50 | = | 58800.0 | nM | 4.23 |
| CHEMBL520305 | — | EC50 | - | — | - | |
| CHEMBL457 | GEMFIBROZIL | EC50 | = | 193300.0 | nM | - |
| CHEMBL484264 | — | Activity | - | — | - | |
| CHEMBL492046 | — | Activity | - | — | - | |
| CHEMBL521796 | — | Activity | - | — | - |