Assay Detail
Functional
CHEMBL1074807
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human full length PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by firefly luciferase assay
15
Total Activities
15
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 | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of novel bis-oximinoalkanoic acids as potent PPAR alpha agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.33 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL592054 | IMIGLITAZAR | 3.0 | 1 | 8.40 |
| CHEMBL591348 | — | — | 1 | 7.00 |
| CHEMBL591347 | — | — | 1 | 6.70 |
| CHEMBL589256 | — | — | 1 | 6.70 |
| CHEMBL592234 | — | — | 1 | 6.70 |
| CHEMBL589747 | — | — | 1 | 6.16 |
| CHEMBL592235 | — | — | 1 | 6.10 |
| CHEMBL592236 | — | — | 1 | 6.00 |
| CHEMBL591533 | — | — | 1 | 5.96 |
| CHEMBL591055 | — | — | 1 | 5.85 |
| CHEMBL591534 | — | — | 1 | 5.85 |
| CHEMBL603612 | — | — | 1 | 5.80 |
| CHEMBL591539 | — | — | 1 | 5.72 |
| CHEMBL606462 | — | — | 1 | 5.68 |
| CHEMBL590341 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL592054 | IMIGLITAZAR | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL591348 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL591347 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL589256 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL592234 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL589747 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL592235 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL592236 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL591533 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL591055 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL591534 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL603612 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL591539 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL606462 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL590341 | — | EC50 | - | — | - |