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Assay Detail

CHEMBL839772

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
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

Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
Liu K, Xu L, Berger JP, Macnaul KL, Zhou G, Doebber TW, Forrest MJ, Moller DE, Jones AB.
J Med Chem (2005) 48 : 2262 -2265
PubMed 15801817 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.48 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190665 1 8.00
CHEMBL190739 1 7.22
CHEMBL192152 1 6.52
CHEMBL190645 1 6.21
CHEMBL364774 1 6.12
CHEMBL981 FENOFIBRIC ACID 4.0 1 4.82
CHEMBL121 ROSIGLITAZONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190665 EC50 = 10.0 nM 8.00
CHEMBL190739 EC50 = 60.0 nM 7.22
CHEMBL192152 EC50 = 300.0 nM 6.52
CHEMBL190645 EC50 = 620.0 nM 6.21
CHEMBL364774 EC50 = 750.0 nM 6.12
CHEMBL981 FENOFIBRIC ACID EC50 = 15000.0 nM 4.82
CHEMBL121 ROSIGLITAZONE EC50 > 10000.0 nM -