Assay Detail
Binding
CHEMBL2162354
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of human PPARalpha expressed in human HEK293 cells after 16 to 20 hrs by dual luciferase beta-galactosidase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and in vitro evaluation of a series of α-substituted phenylpropanoic acid PPARγ agonists to further investigate the stereochemistry-activity relationship.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.36 | 7.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL402840 | — | — | 1 | 7.27 |
| CHEMBL272137 | — | — | 1 | 6.30 |
| CHEMBL2158959 | — | — | 1 | 6.11 |
| CHEMBL2158012 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL402840 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL272137 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2158959 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL2158012 | — | EC50 | = | 1760.0 | nM | 5.75 |