Assay Detail
Functional
CHEMBL979054
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HepG2 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.63 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL481551 | — | — | 1 | 7.82 |
| CHEMBL468159 | — | — | 1 | 7.70 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.30 |
| CHEMBL512084 | — | — | 1 | 7.02 |
| CHEMBL468160 | — | — | 1 | 6.62 |
| CHEMBL513145 | — | — | 1 | 5.86 |
| CHEMBL467349 | — | — | 1 | 5.39 |
| CHEMBL512789 | — | — | 1 | 5.30 |
| CHEMBL513916 | — | — | 1 | - |
| CHEMBL466952 | — | — | 1 | - |
| CHEMBL467369 | — | — | 1 | - |
| CHEMBL515003 | — | — | 1 | - |
| CHEMBL476719 | — | — | 1 | - |
| CHEMBL514054 | — | — | 1 | - |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL481551 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL468159 | — | EC50 | = | 19.8 | nM | 7.70 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL512084 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL468160 | — | EC50 | = | 239.0 | nM | 6.62 |
| CHEMBL513145 | — | EC50 | = | 1385.0 | nM | 5.86 |
| CHEMBL467349 | — | EC50 | = | 4096.0 | nM | 5.39 |
| CHEMBL512789 | — | EC50 | = | 5010.0 | nM | 5.30 |
| CHEMBL513916 | — | EC50 | - | — | - | |
| CHEMBL466952 | — | EC50 | - | — | - | |
| CHEMBL467369 | — | EC50 | - | — | - | |
| CHEMBL515003 | — | EC50 | - | — | - | |
| CHEMBL476719 | — | EC50 | - | — | - | |
| CHEMBL514054 | — | EC50 | - | — | - | |
| CHEMBL295416 | PIRINIXIC ACID | EC50 | - | — | - |