Assay Detail
Binding
CHEMBL4265666
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay
8
Total Activities
8
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 |
|---|---|---|---|
| EC50 | 8 | 6.52 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 8.10 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 7.01 |
| CHEMBL4276678 | — | — | 1 | 6.76 |
| CHEMBL4293295 | — | — | 1 | 6.57 |
| CHEMBL146624 | MITOGLITAZONE | 2.0 | 1 | 6.18 |
| CHEMBL4291468 | — | — | 1 | 6.02 |
| CHEMBL4286980 | — | — | 1 | 5.76 |
| CHEMBL4284250 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL595 | PIOGLITAZONE | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4276678 | — | EC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4293295 | — | EC50 | = | 271.0 | nM | 6.57 |
| CHEMBL146624 | MITOGLITAZONE | EC50 | = | 657.0 | nM | 6.18 |
| CHEMBL4291468 | — | EC50 | = | 961.0 | nM | 6.02 |
| CHEMBL4286980 | — | EC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL4284250 | — | EC50 | = | 1740.0 | nM | 5.76 |