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Assay Detail

CHEMBL4022342

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Agonist activity at GAL4 fused human PPARgamma LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
Shioi R, Okazaki S, Noguchi-Yachide T, Ishikawa M, Makishima M, Hashimoto Y, Yamaguchi T.
Bioorg Med Chem Lett (2017) 27 : 3131 -3134
PubMed 28539218 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.24 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24038 RAGAGLITAZAR 2.0 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24038 RAGAGLITAZAR EC50 = 570.0 nM 6.24