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Assay Detail

CHEMBL1655217

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

Binding
Transactivation of Gal4-fused human PPARalpha expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay
6
Total Activities
6
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 alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structural analysis of phenylpropanoic acid-type PPARγ-selective agonists: discovery of reversed stereochemistry-activity relationship.
Ohashi M, Oyama T, Nakagome I, Satoh M, Nishio Y, Nobusada H, Hirono S, Morikawa K, Hashimoto Y, Miyachi H.
J Med Chem (2011) 54 : 331 -341
PubMed 21128600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.85 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL202118 1 7.92
CHEMBL402840 1 7.27
CHEMBL382655 1 6.82
CHEMBL375471 1 6.60
CHEMBL272137 1 6.30
CHEMBL427071 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL202118 EC50 = 12.0 nM 7.92
CHEMBL402840 EC50 = 54.0 nM 7.27
CHEMBL382655 EC50 = 150.0 nM 6.82
CHEMBL375471 EC50 = 250.0 nM 6.60
CHEMBL272137 EC50 = 500.0 nM 6.30
CHEMBL427071 EC50 = 620.0 nM 6.21