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Assay Detail

CHEMBL831811

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

Binding
Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay
15
Total Activities
15
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

Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Henke BR.
J Med Chem (2004) 47 : 4118 -4127
PubMed 15293980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.55 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410478 1 8.70
CHEMBL173159 1 8.40
CHEMBL82602 1 8.05
CHEMBL189146 1 8.00
CHEMBL94306 1 7.52
CHEMBL25259 1 6.82
CHEMBL186179 MURAGLITAZAR 3.0 1 6.62
CHEMBL86658 1 6.44
CHEMBL24458 1 6.00
CHEMBL24038 RAGAGLITAZAR 2.0 1 5.50
CHEMBL672 FENOFIBRATE 4.0 1 4.52
CHEMBL264374 BEZAFIBRATE 3.0 1 4.30
CHEMBL565 CLOFIBRATE 4.0 1 4.26
CHEMBL121 ROSIGLITAZONE 4.0 1 -
CHEMBL189547 PLOGLITAZONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410478 EC50 = 2.0 nM 8.70
CHEMBL173159 EC50 = 4.0 nM 8.40
CHEMBL82602 EC50 = 9.0 nM 8.05
CHEMBL189146 EC50 = 10.0 nM 8.00
CHEMBL94306 EC50 = 30.0 nM 7.52
CHEMBL25259 EC50 = 150.0 nM 6.82
CHEMBL186179 MURAGLITAZAR EC50 = 240.0 nM 6.62
CHEMBL86658 EC50 = 360.0 nM 6.44
CHEMBL24458 EC50 = 1000.0 nM 6.00
CHEMBL24038 RAGAGLITAZAR EC50 = 3200.0 nM 5.50
CHEMBL672 FENOFIBRATE EC50 = 30000.0 nM 4.52
CHEMBL264374 BEZAFIBRATE EC50 = 50000.0 nM 4.30
CHEMBL565 CLOFIBRATE EC50 = 55000.0 nM 4.26
CHEMBL121 ROSIGLITAZONE EC50 - nM -
CHEMBL189547 PLOGLITAZONE EC50 - nM -