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Assay Detail

CHEMBL3587209

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

Binding
Activity at human PPARgamma transfected in HEK293 cells assessed as transactivation activity by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Peroxisome Proliferator-Activated Receptor γ (PPARγ) and Ligand Choreography: Newcomers Take the Stage.
Garcia-Vallvé S, Guasch L, Tomas-Hernández S, del Bas JM, Ollendorff V, Arola L, Pujadas G, Mulero M.
J Med Chem (2015) 58 : 5381 -5394
PubMed 25734377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.24 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370152 1 7.24
CHEMBL3585572 1 6.81
CHEMBL491820 AMORFRUTIN A 1 6.34
CHEMBL1204498 1 5.89
CHEMBL2103824 ARHALOFENATE 2.0 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370152 EC50 = 57.0 nM 7.24
CHEMBL3585572 EC50 = 155.0 nM 6.81
CHEMBL491820 AMORFRUTIN A EC50 = 458.0 nM 6.34
CHEMBL1204498 EC50 = 1300.0 nM 5.89
CHEMBL2103824 ARHALOFENATE EC50 = 12000.0 nM 4.92