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Assay Detail

CHEMBL3269595

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Binding
Agonist activity at human PPAR-alpha
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of the first potent, selective and bioavailable PPARα antagonist.
Bravo Y, Baccei CS, Broadhead A, Bundey R, Chen A, Clark R, Correa L, Jacintho JD, Lorrain DS, Messmer D, Stebbins K, Prasit P, Stock N.
Bioorg Med Chem Lett (2014) 24 : 2267 -2272
PubMed 24745969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.00 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424133 LY-518674 2.0 1 7.38
CHEMBL410478 1 6.62
CHEMBL3264932 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424133 LY-518674 EC50 = 42.0 nM 7.38
CHEMBL410478 EC50 = 240.0 nM 6.62
CHEMBL3264932 EC50 > 100000.0 nM -