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Assay Detail

CHEMBL4368718

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

Binding
Antagonist actvity in sGFP-tagged PPARgamma LBD (unknown origin) assessed as inhibition of rosiglitazone-induced PPARgamma activation incubated for 1 hr in presence of CBP-1 cofactor peptide by HTRF based cofactor recruitment 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

Structure optimization of a new class of PPARγ antagonists.
Hernandez-Olmos V, Knape T, Heering J, von Knethen A, Kilu W, Kaiser A, Wurglics M, Helmstädter M, Merk D, Schubert-Zsilavecz M, Parnham MJ, Steinhilber D, Proschak E.
Bioorg Med Chem (2019) 27 : 115082 -115082
PubMed 31548084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.19 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4467078 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4467078 IC50 = 6400.0 nM 5.19