Assay Detail
Binding
CHEMBL3368591
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at wild-type human PPARalpha Thr279Ala mutant expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| 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 improved activity at PPARα: structure-activity relationship of pirinixic acid derivatives, docking study and site-directed mutagenesis of PPARα.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.84 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3318039 | — | — | 1 | 7.16 |
| CHEMBL3318038 | — | — | 1 | 7.00 |
| CHEMBL3318040 | — | — | 1 | 6.82 |
| CHEMBL3318041 | — | — | 1 | 6.62 |
| CHEMBL21241 | GW7647 | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3318039 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3318038 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3318040 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3318041 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL21241 | GW7647 | EC50 | = | 250.0 | nM | 6.60 |