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Assay Detail

CHEMBL4236832

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

Binding
Synergistic agonist activity at human PPARgamma LBD assessed as biotin-labeled PGC1alpha (130 to 154 residues) co-activator recruitment after 1 hr in presence of 0.37 uM rosiglitazone by TR-FRET assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
Laghezza A, Piemontese L, Cerchia C, Montanari R, Capelli D, Giudici M, Crestani M, Tortorella P, Peiretti F, Pochetti G, Lavecchia A, Loiodice F.
J Med Chem (2018) 61 : 8282 -8298
PubMed 30199253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 5.43 5.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4237252 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4237252 EC50 = 3690.0 nM 5.43