Assay Detail
Functional
CHEMBL1648428
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor delta (CHEMBL3979) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 6.65 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38943 | GW501516 | 2.0 | 1 | 8.92 |
| CHEMBL1644299 | — | — | 1 | 8.00 |
| CHEMBL1644310 | — | — | 1 | 6.52 |
| CHEMBL1644304 | — | — | 1 | 6.16 |
| CHEMBL1644301 | — | — | 1 | 6.10 |
| CHEMBL1644305 | — | — | 1 | 6.10 |
| CHEMBL264374 | BEZAFIBRATE | 3.0 | 1 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38943 | GW501516 | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1644299 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1644310 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1644304 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1644301 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1644305 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL264374 | BEZAFIBRATE | EC50 | = | 18900.0 | nM | 4.72 |