Assay Detail
Functional
CHEMBL906215
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay
24
Total Activities
24
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 | Intermediate |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 7.59 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230705 | — | — | 1 | 8.89 |
| CHEMBL388645 | — | — | 1 | 8.66 |
| CHEMBL230706 | — | — | 1 | 8.51 |
| CHEMBL230518 | — | — | 1 | 8.46 |
| CHEMBL230517 | — | — | 1 | 8.40 |
| CHEMBL231523 | — | — | 1 | 8.31 |
| CHEMBL230623 | — | — | 1 | 8.00 |
| CHEMBL389297 | — | — | 1 | 7.97 |
| CHEMBL230411 | — | — | 1 | 7.94 |
| CHEMBL388008 | — | — | 1 | 7.93 |
| CHEMBL230409 | — | — | 1 | 7.92 |
| CHEMBL388422 | — | — | 1 | 7.92 |
| CHEMBL231425 | — | — | 1 | 7.72 |
| CHEMBL389298 | — | — | 1 | 7.72 |
| CHEMBL230410 | — | — | 1 | 7.64 |
| CHEMBL230814 | — | — | 1 | 7.58 |
| CHEMBL230707 | — | — | 1 | 7.50 |
| CHEMBL278590 | GSK-9578 | — | 1 | 7.11 |
| CHEMBL230305 | — | — | 1 | 7.04 |
| CHEMBL230519 | — | — | 1 | 6.98 |
| CHEMBL230622 | — | — | 1 | 6.86 |
| CHEMBL230304 | — | — | 1 | 6.22 |
| CHEMBL387588 | — | — | 1 | 5.91 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230705 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL388645 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL230706 | — | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL230518 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL230517 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL231523 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL230623 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL389297 | — | EC50 | = | 10.6 | nM | 7.97 |
| CHEMBL230411 | — | EC50 | = | 11.5 | nM | 7.94 |
| CHEMBL388008 | — | EC50 | = | 11.7 | nM | 7.93 |
| CHEMBL230409 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL388422 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL231425 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL389298 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL230410 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL230814 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL230707 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL278590 | GSK-9578 | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL230305 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL230519 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL230622 | — | EC50 | = | 139.0 | nM | 6.86 |
| CHEMBL230304 | — | EC50 | = | 596.0 | nM | 6.22 |
| CHEMBL387588 | — | EC50 | = | 1237.0 | nM | 5.91 |
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 9798.0 | nM | 5.01 |