Assay Detail
Binding
CHEMBL3367520
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
10
Total Activities
10
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 | 10 | 6.07 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3318038 | — | — | 1 | 7.16 |
| CHEMBL21241 | GW7647 | — | 1 | 6.64 |
| CHEMBL3318039 | — | — | 1 | 6.55 |
| CHEMBL3318040 | — | — | 1 | 6.55 |
| CHEMBL3318037 | — | — | 1 | 6.46 |
| CHEMBL3318041 | — | — | 1 | 6.14 |
| CHEMBL518038 | — | — | 1 | 6.00 |
| CHEMBL459972 | — | — | 1 | 5.92 |
| CHEMBL3318036 | — | — | 1 | 4.92 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3318038 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL21241 | GW7647 | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3318039 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3318040 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3318037 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3318041 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL518038 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL459972 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3318036 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 39800.0 | nM | 4.40 |