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Assay Detail

CHEMBL2072933

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Functional
Agonist activity at human PPARalpha
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators.
Pirat C, Farce A, Lebègue N, Renault N, Furman C, Millet R, Yous S, Speca S, Berthelot P, Desreumaux P, Chavatte P.
J Med Chem (2012) 55 : 4027 -4061
PubMed 22260081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.79 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219586 GW590735 2.0 1 8.40
CHEMBL278590 GSK-9578 1 8.22
CHEMBL21241 GW7647 1 7.30
CHEMBL107789 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219586 GW590735 EC50 = 4.0 nM 8.40
CHEMBL278590 GSK-9578 EC50 = 6.0 nM 8.22
CHEMBL21241 GW7647 EC50 = 50.0 nM 7.30
CHEMBL107789 EC50 = 60.0 nM 7.22