Assay Detail
Binding
CHEMBL942181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay
34
Total Activities
34
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor alpha (CHEMBL239) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 6.14 | 7.57 |
| Activity | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL472245 | — | — | 1 | 7.57 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.41 |
| CHEMBL472246 | — | — | 1 | 7.31 |
| CHEMBL472451 | — | — | 1 | 7.19 |
| CHEMBL472244 | — | — | 1 | 7.19 |
| CHEMBL470145 | — | — | 1 | 6.62 |
| CHEMBL469937 | — | — | 1 | 6.46 |
| CHEMBL471011 | — | — | 1 | 6.38 |
| CHEMBL470144 | — | — | 1 | 6.35 |
| CHEMBL513244 | — | — | 1 | 6.16 |
| CHEMBL508225 | — | — | 1 | 5.96 |
| CHEMBL471814 | — | — | 1 | 5.94 |
| CHEMBL486365 | — | — | 1 | 5.84 |
| CHEMBL486205 | — | — | 1 | 5.78 |
| CHEMBL525772 | — | — | 1 | 5.67 |
| CHEMBL486357 | — | — | 1 | 5.66 |
| CHEMBL486364 | — | — | 1 | 5.65 |
| CHEMBL471191 | — | — | 1 | 5.65 |
| CHEMBL471851 | — | — | 1 | 5.60 |
| CHEMBL449099 | — | — | 1 | 5.55 |
| CHEMBL486363 | — | — | 1 | 5.35 |
| CHEMBL442909 | — | — | 1 | 5.03 |
| CHEMBL364748 | — | — | 1 | 4.84 |
| CHEMBL471815 | — | — | 1 | - |
| CHEMBL443335 | — | — | 1 | - |
| CHEMBL471850 | — | — | 1 | - |
| CHEMBL486362 | — | — | 1 | - |
| CHEMBL485762 | — | — | 1 | - |
| CHEMBL486766 | — | — | 1 | - |
| CHEMBL486765 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL472245 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL472246 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL472451 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL472244 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL470145 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL469937 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL471011 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL470144 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL513244 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL508225 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL471814 | — | EC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL486365 | — | EC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL486205 | — | EC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL525772 | — | EC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL486357 | — | EC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL471191 | — | EC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL486364 | — | EC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL471851 | — | EC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL449099 | — | EC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL486363 | — | EC50 | = | 4490.0 | nM | 5.35 |
| CHEMBL442909 | — | EC50 | = | 9250.0 | nM | 5.03 |
| CHEMBL364748 | — | EC50 | = | 14460.0 | nM | 4.84 |
| CHEMBL295416 | PIRINIXIC ACID | Activity | - | — | - | |
| CHEMBL471643 | — | Activity | - | — | - | |
| CHEMBL486350 | — | EC50 | - | — | - | |
| CHEMBL486764 | — | EC50 | - | — | - | |
| CHEMBL486765 | — | Activity | - | — | - | |
| CHEMBL486766 | — | Activity | - | — | - | |
| CHEMBL485762 | — | Activity | - | — | - | |
| CHEMBL486362 | — | Activity | - | — | - | |
| CHEMBL471850 | — | Activity | - | — | - | |
| CHEMBL443335 | — | Activity | - | — | - | |
| CHEMBL471815 | — | Activity | - | — | - |