Assay Detail
Functional
CHEMBL1831689
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Agonist activity at Gal4-fused PPARalpha expressed in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 5.00 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL21241 | GW7647 | — | 1 | 6.70 |
| CHEMBL1828826 | — | — | 1 | 6.00 |
| CHEMBL1828822 | — | — | 1 | 5.18 |
| CHEMBL1828831 | — | — | 1 | 5.04 |
| CHEMBL1828832 | — | — | 1 | 5.03 |
| CHEMBL19641 | — | — | 1 | 5.03 |
| CHEMBL1828821 | — | — | 1 | 4.95 |
| CHEMBL1828825 | — | — | 1 | 4.73 |
| CHEMBL1828829 | — | — | 1 | 4.57 |
| CHEMBL1828834 | — | — | 1 | 4.36 |
| CHEMBL457 | GEMFIBROZIL | 4.0 | 1 | 4.23 |
| CHEMBL1828828 | — | — | 1 | 4.21 |
| CHEMBL1828827 | — | — | 1 | - |
| CHEMBL1828823 | — | — | 1 | - |
| CHEMBL1828833 | — | — | 1 | - |
| CHEMBL1828830 | — | — | 1 | - |
| CHEMBL1828824 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL21241 | GW7647 | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1828826 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1828822 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL1828831 | — | EC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1828832 | — | EC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL19641 | — | EC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL1828821 | — | EC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL1828825 | — | EC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL1828829 | — | EC50 | = | 27100.0 | nM | 4.57 |
| CHEMBL1828834 | — | EC50 | = | 43700.0 | nM | 4.36 |
| CHEMBL457 | GEMFIBROZIL | EC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL1828828 | — | EC50 | = | 61500.0 | nM | 4.21 |
| CHEMBL1828827 | — | EC50 | = | 109300.0 | nM | - |
| CHEMBL1828823 | — | EC50 | - | — | - | |
| CHEMBL1828833 | — | EC50 | - | — | - | |
| CHEMBL1828830 | — | EC50 | - | — | - | |
| CHEMBL1828824 | — | EC50 | - | — | - |