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Assay Detail

CHEMBL1805526

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Functional
Agonist activity at PPARgamma expressed in HepG2 cells co-expressing PPRE assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HepG2
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Novel thiazolidinedione derivatives with anti-obesity effects: dual action as PTP1B inhibitors and PPAR-γ activators.
Bhattarai BR, Kafle B, Hwang JS, Ham SW, Lee KH, Park H, Han IO, Cho H.
Bioorg Med Chem Lett (2010) 20 : 6758 -6763
PubMed 20850970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.27 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1801440 1 6.47
CHEMBL574813 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1801440 EC50 = 340.0 nM 6.47
CHEMBL574813 EC50 = 870.0 nM 6.06