Assay Detail
Binding
CHEMBL2379022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at GAL4-fused PPARalpha A454M mutant (unknown origin) expressed in human HepG2 cells by transactivation assay
3
Total Activities
3
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 | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 5.87 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489074 | — | — | 1 | 6.40 |
| CHEMBL472245 | — | — | 1 | 6.05 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489074 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL472245 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 7100.0 | nM | 5.15 |