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Assay Detail

CHEMBL764652

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Functional
Agonistic activity for Peroxisome proliferator activated receptor alpha
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 Expert

Target

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

Publication

Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
Ebdrup S, Pettersson I, Rasmussen HB, Deussen HJ, Frost Jensen A, Mortensen SB, Fleckner J, Pridal L, Nygaard L, Sauerberg P.
J Med Chem (2003) 46 : 1306 -1317
PubMed 12672231 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.06 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25259 1 6.82
CHEMBL24458 1 6.00
CHEMBL282686 TESAGLITAZAR 3.0 1 5.92
CHEMBL24038 RAGAGLITAZAR 2.0 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25259 EC50 = 150.0 nM 6.82
CHEMBL24458 EC50 = 1000.0 nM 6.00
CHEMBL282686 TESAGLITAZAR EC50 = 1200.0 nM 5.92
CHEMBL24038 RAGAGLITAZAR EC50 = 3200.0 nM 5.50