Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2341919

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

Binding
Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.
de Groot JC, Weidner C, Krausze J, Kawamoto K, Schroeder FC, Sauer S, Büssow K.
J Med Chem (2013) 56 : 1535 -1543
PubMed 23286787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.99 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 8.40
CHEMBL2337127 1 7.30
CHEMBL491820 AMORFRUTIN A 1 6.34
CHEMBL2337126 1 5.92
CHEMBL38508 1 -
CHEMBL21241 GW7647 1 -
CHEMBL1204498 1 -
CHEMBL2337128 1 -
CHEMBL370152 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE EC50 = 4.0 nM 8.40
CHEMBL2337127 EC50 = 50.0 nM 7.30
CHEMBL491820 AMORFRUTIN A EC50 = 458.0 nM 6.34
CHEMBL2337126 EC50 = 1200.0 nM 5.92
CHEMBL38508 EC50 - -
CHEMBL21241 GW7647 EC50 - -
CHEMBL1204498 EC50 - -
CHEMBL2337128 EC50 - -
CHEMBL370152 EC50 - -