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Assay Detail

CHEMBL824651

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

Binding
Binding affinity at human PPAR alpha
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
Brooks DA, Etgen GJ, Rito CJ, Shuker AJ, Dominianni SJ, Warshawsky AM, Ardecky R, Paterniti JR, Tyhonas J, Karanewsky DS, Kauffman RF, Broderick CL, Oldham BA, Montrose-Rafizadeh C, Winneroski LL, Faul MM, McCarthy JR.
J Med Chem (2001) 44 : 2061 -2064
PubMed 11405642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.30 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65458 1 7.21
CHEMBL25259 1 6.83
CHEMBL64972 1 6.20
CHEMBL66206 1 6.14
CHEMBL59132 1 6.11
CHEMBL24458 1 6.04
CHEMBL294807 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65458 EC50 = 61.9 nM 7.21
CHEMBL25259 EC50 = 149.5 nM 6.83
CHEMBL64972 EC50 = 625.0 nM 6.20
CHEMBL66206 EC50 = 717.0 nM 6.14
CHEMBL59132 EC50 = 771.0 nM 6.11
CHEMBL24458 EC50 = 922.0 nM 6.04
CHEMBL294807 EC50 = 2751.0 nM 5.56