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Assay Detail

CHEMBL2067031

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

Binding
Binding affinity to PPARgamma LBD by fluorescence polarization based competitive binding assay
5
Total Activities
5
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

Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
Nevin DK, Peters MB, Carta G, Fayne D, Lloyd DG.
J Med Chem (2012) 55 : 4978 -4989
PubMed 22582973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.33 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434063 1 7.58
CHEMBL121 ROSIGLITAZONE 4.0 1 6.72
CHEMBL2064741 1 6.49
CHEMBL2064743 1 5.62
CHEMBL2064742 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434063 EC50 = 26.0 nM 7.58
CHEMBL121 ROSIGLITAZONE EC50 = 190.0 nM 6.72
CHEMBL2064741 EC50 = 325.0 nM 6.49
CHEMBL2064743 EC50 = 2400.0 nM 5.62
CHEMBL2064742 EC50 = 5450.0 nM 5.26