Assay Detail
Functional
CHEMBL906214
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARgamma 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 gamma (CHEMBL235) ↗| 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 | 8.45 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230814 | — | — | 1 | 10.00 |
| CHEMBL230705 | — | — | 1 | 9.72 |
| CHEMBL388645 | — | — | 1 | 9.52 |
| CHEMBL230707 | — | — | 1 | 9.51 |
| CHEMBL230706 | — | — | 1 | 9.44 |
| CHEMBL389297 | — | — | 1 | 9.27 |
| CHEMBL231523 | — | — | 1 | 9.26 |
| CHEMBL388422 | — | — | 1 | 9.00 |
| CHEMBL230517 | — | — | 1 | 8.68 |
| CHEMBL231425 | — | — | 1 | 8.68 |
| CHEMBL230518 | — | — | 1 | 8.54 |
| CHEMBL230411 | — | — | 1 | 8.52 |
| CHEMBL230305 | — | — | 1 | 8.40 |
| CHEMBL230519 | — | — | 1 | 8.30 |
| CHEMBL230304 | — | — | 1 | 8.30 |
| CHEMBL230623 | — | — | 1 | 8.28 |
| CHEMBL230409 | — | — | 1 | 8.17 |
| CHEMBL230410 | — | — | 1 | 8.11 |
| CHEMBL389298 | — | — | 1 | 7.89 |
| CHEMBL230622 | — | — | 1 | 7.70 |
| CHEMBL388008 | — | — | 1 | 7.55 |
| CHEMBL387588 | — | — | 1 | 7.32 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.09 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230814 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL230705 | — | EC50 | = | 0.19 | nM | 9.72 |
| CHEMBL388645 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL230707 | — | EC50 | = | 0.31 | nM | 9.51 |
| CHEMBL230706 | — | EC50 | = | 0.36 | nM | 9.44 |
| CHEMBL389297 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL231523 | — | EC50 | = | 0.55 | nM | 9.26 |
| CHEMBL388422 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL230517 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL231425 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL230518 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL230411 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL230305 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL230519 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL230304 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL230623 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL230409 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL230410 | — | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL389298 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL230622 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL388008 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL387588 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL282686 | TESAGLITAZAR | EC50 | = | 3528.0 | nM | 5.45 |