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Assay Detail

CHEMBL4233587

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

Binding
Agonist activity at PPARgamma in human HepG2 cells assessed as activation of PPRE incubated for 24 hrs by dual luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
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 novel l-phenylglycine derivatives as potential PPARγ lead compounds.
Liu J, Su X, Li H, Fan L, Li Y, Tang X, Yan J, Chen X, Chen F, Liu J, Yang D.
Bioorg Med Chem (2018) 26 : 4153 -4167
PubMed 30001846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.44 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595 PIOGLITAZONE 4.0 1 6.62
CHEMBL4250971 1 5.05
CHEMBL4247845 1 4.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595 PIOGLITAZONE EC50 = 240.0 nM 6.62
CHEMBL4250971 EC50 = 8970.0 nM 5.05
CHEMBL4247845 EC50 = 22390.0 nM 4.65