Assay Detail
Binding
CHEMBL4023665
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled LCOR (39 to 63 residues) co-activator recruitment by TR-FRET assay
2
Total Activities
2
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
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 6.71 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 7.28 |
| CHEMBL4091374 | LANIFIBRANOR | 3.0 | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121 | ROSIGLITAZONE | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4091374 | LANIFIBRANOR | EC50 | = | 727.0 | nM | 6.14 |