Assay Detail
Binding
CHEMBL4265665
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive displacement of fluorescently labelled PPAR tracer ligand from GST-tagged human PPARgamma ligand binding domain after 1 hr in dark by TR-FRET competitive binding assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.42 | 6.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 6.95 |
| CHEMBL186179 | MURAGLITAZAR | 3.0 | 1 | 6.92 |
| CHEMBL408 | TROGLITAZONE | 4.0 | 1 | 6.43 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 5.75 |
| CHEMBL4276678 | — | — | 1 | 5.63 |
| CHEMBL4293295 | — | — | 1 | 5.51 |
| CHEMBL4288064 | — | — | 1 | 5.07 |
| CHEMBL4280830 | — | — | 1 | 4.93 |
| CHEMBL4291468 | — | — | 1 | 4.74 |
| CHEMBL146624 | MITOGLITAZONE | 2.0 | 1 | 4.65 |
| CHEMBL4284250 | — | — | 1 | 4.30 |
| CHEMBL4286980 | — | — | 1 | 4.11 |
| CHEMBL7002 | CIGLITAZONE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL186179 | MURAGLITAZAR | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL408 | TROGLITAZONE | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL595 | PIOGLITAZONE | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL4276678 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL4293295 | — | IC50 | = | 3120.0 | nM | 5.51 |
| CHEMBL4288064 | — | IC50 | = | 8460.0 | nM | 5.07 |
| CHEMBL4280830 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4291468 | — | IC50 | = | 18140.0 | nM | 4.74 |
| CHEMBL146624 | MITOGLITAZONE | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL4284250 | — | IC50 | = | 50140.0 | nM | 4.30 |
| CHEMBL4286980 | — | IC50 | = | 78450.0 | nM | 4.11 |
| CHEMBL7002 | CIGLITAZONE | IC50 | > | 5000.0 | nM | - |