Assay Detail
Binding
CHEMBL942384
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2/C3A |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 7.18 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 8.42 |
| CHEMBL479207 | — | — | 1 | 7.13 |
| CHEMBL477312 | — | — | 1 | 6.95 |
| CHEMBL477119 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL479207 | — | EC50 | = | 73.3 | nM | 7.13 |
| CHEMBL477312 | — | EC50 | = | 111.3 | nM | 6.95 |
| CHEMBL477119 | — | EC50 | = | 593.0 | nM | 6.23 |