Assay Detail
Binding
CHEMBL759458
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Receptor binding affinity to human Peroxisome proliferator activated receptor gamma against [3H]ragalitazar radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.25 | 7.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24038 | RAGAGLITAZAR | 2.0 | 1 | 7.04 |
| CHEMBL282686 | TESAGLITAZAR | 3.0 | 1 | 6.46 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.36 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 5.13 |
| CHEMBL24683 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24038 | RAGAGLITAZAR | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL282686 | TESAGLITAZAR | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL595 | PIOGLITAZONE | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL24683 | — | IC50 | > | 10000.0 | nM | - |