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Assay Detail

CHEMBL828585

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

Binding
Inhibition of human Peroxisome proliferator activated receptor gamma binding
9
Total Activities
9
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 gamma (CHEMBL235)
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
IC50 9 6.03 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 6.60
CHEMBL190665 1 5.91
CHEMBL192152 1 5.80
CHEMBL190739 1 5.79
CHEMBL363369 1 -
CHEMBL190645 1 -
CHEMBL364774 1 -
CHEMBL190352 1 -
CHEMBL981 FENOFIBRIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE IC50 = 250.0 nM 6.60
CHEMBL190665 IC50 = 1220.0 nM 5.91
CHEMBL192152 IC50 = 1580.0 nM 5.80
CHEMBL190739 IC50 = 1620.0 nM 5.79
CHEMBL363369 IC50 > 10000.0 nM -
CHEMBL190645 IC50 > 10000.0 nM -
CHEMBL364774 IC50 > 15000.0 nM -
CHEMBL190352 IC50 > 15000.0 nM -
CHEMBL981 FENOFIBRIC ACID IC50 > 50000.0 nM -