Assay Detail
Binding
CHEMBL1655219
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and structural analysis of phenylpropanoic acid-type PPARγ-selective agonists: discovery of reversed stereochemistry-activity relationship.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.59 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1651239 | — | — | 1 | 8.44 |
| CHEMBL1651238 | — | — | 1 | 7.66 |
| CHEMBL402840 | — | — | 1 | 7.39 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.37 |
| CHEMBL272137 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1651239 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1651238 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL402840 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL272137 | — | EC50 | = | 83.0 | nM | 7.08 |