Assay Detail
Binding
CHEMBL5162400
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at yeast Gal4-fused human PPARdelta transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase activity incubated for 20 hrs by luminometry
26
Total Activities
26
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 delta (CHEMBL3979) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 23 | - | - |
| EC50 | 3 | 5.55 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL153057 | — | — | 1 | 7.68 |
| CHEMBL5195064 | — | — | 1 | 4.55 |
| CHEMBL1967191 | — | — | 1 | 4.43 |
| CHEMBL5184438 | — | — | 1 | - |
| CHEMBL5207420 | — | — | 1 | - |
| CHEMBL5196830 | — | — | 1 | - |
| CHEMBL5171340 | — | — | 1 | - |
| CHEMBL5204992 | — | — | 1 | - |
| CHEMBL5173134 | — | — | 1 | - |
| CHEMBL5191690 | — | — | 1 | - |
| CHEMBL5194126 | — | — | 1 | - |
| CHEMBL5191536 | — | — | 1 | - |
| CHEMBL5207071 | — | — | 1 | - |
| CHEMBL5203327 | — | — | 1 | - |
| CHEMBL5172173 | — | — | 1 | - |
| CHEMBL5199782 | — | — | 1 | - |
| CHEMBL5186824 | — | — | 1 | - |
| CHEMBL5194570 | — | — | 1 | - |
| CHEMBL5173310 | — | — | 1 | - |
| CHEMBL5190696 | — | — | 1 | - |
| CHEMBL5171949 | — | — | 1 | - |
| CHEMBL5196394 | — | — | 1 | - |
| CHEMBL5173673 | — | — | 1 | - |
| CHEMBL5193822 | — | — | 1 | - |
| CHEMBL295416 | PIRINIXIC ACID | 2.0 | 1 | - |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL153057 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5195064 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL1967191 | — | EC50 | = | 37100.0 | nM | 4.43 |
| CHEMBL5184438 | — | Activity | - | — | - | |
| CHEMBL5207420 | — | Activity | - | — | - | |
| CHEMBL5196830 | — | Activity | - | — | - | |
| CHEMBL5171340 | — | Activity | - | — | - | |
| CHEMBL5204992 | — | Activity | - | — | - | |
| CHEMBL5173134 | — | Activity | - | — | - | |
| CHEMBL5191690 | — | Activity | - | — | - | |
| CHEMBL5194126 | — | Activity | - | — | - | |
| CHEMBL5191536 | — | Activity | - | — | - | |
| CHEMBL5207071 | — | Activity | - | — | - | |
| CHEMBL5203327 | — | Activity | - | — | - | |
| CHEMBL5172173 | — | Activity | - | — | - | |
| CHEMBL5199782 | — | Activity | - | — | - | |
| CHEMBL5186824 | — | Activity | - | — | - | |
| CHEMBL5194570 | — | Activity | - | — | - | |
| CHEMBL5173310 | — | Activity | - | — | - | |
| CHEMBL5190696 | — | Activity | - | — | - | |
| CHEMBL5171949 | — | Activity | - | — | - | |
| CHEMBL5196394 | — | Activity | - | — | - | |
| CHEMBL5173673 | — | Activity | - | — | - | |
| CHEMBL5193822 | — | Activity | - | — | - | |
| CHEMBL295416 | PIRINIXIC ACID | Activity | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | Activity | - | — | - |