Assay Detail
Binding
CHEMBL3368588
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
9
Total Activities
9
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 gamma (CHEMBL235) ↗| 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 | 9 | 5.57 | 6.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3318041 | — | — | 1 | 6.31 |
| CHEMBL3318038 | — | — | 1 | 6.16 |
| CHEMBL3318037 | — | — | 1 | 5.97 |
| CHEMBL3318039 | — | — | 1 | 5.92 |
| CHEMBL3318040 | — | — | 1 | 5.63 |
| CHEMBL459972 | — | — | 1 | 5.52 |
| CHEMBL518038 | — | — | 1 | 5.44 |
| CHEMBL3318036 | — | — | 1 | 4.91 |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | 4.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3318041 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3318038 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL3318037 | — | EC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL3318039 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3318040 | — | EC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL459972 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL518038 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3318036 | — | EC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | = | 53700.0 | nM | 4.27 |