Assay Detail
Binding
CHEMBL5240488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at PPARgamma in mouse 3T3-L1 adipocytes assessed as inhibition of adipogenesis by measuring lipid droplet staining by BODIPY 495 incubated for 6 days by fluorescence based assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | 3T3-L1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL2459) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.41 | 8.06 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5267263 | — | — | 1 | 8.06 |
| CHEMBL5271038 | — | — | 1 | 7.62 |
| CHEMBL5286386 | — | — | 1 | 7.14 |
| CHEMBL5207130 | — | — | 1 | 6.83 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5267263 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5271038 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5286386 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5207130 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL121 | ROSIGLITAZONE | Activity | - | — | - |