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Assay Detail

CHEMBL4629572

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

Binding
Agonist activity at recombinant human pFA-CMV fused PPARgamma expressed in HEK293T cells transfected with pFR-luciferase plasmid and pRL-SV40 plasmid incubated for 14 to 16 hrs by dual glo luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
Gellrich L, Heitel P, Heering J, Kilu W, Pollinger J, Goebel T, Kahnt A, Arifi S, Pogoda W, Paulke A, Steinhilber D, Proschak E, Wurglics M, Schubert-Zsilavecz M, Chaikuad A, Knapp S, Bischoff I, Fürst R, Merk D.
J Med Chem (2020) 63 : 6727 -6740
PubMed 32356658 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 5.77 7.00
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL549748 TETRAC -1.0 1 7.00
CHEMBL4637025 1 6.52
CHEMBL41632 TIRATRICOL 3.0 1 6.43
CHEMBL1743304 REVERSE TRIIODOTHYRONINE 1 5.42
CHEMBL1544 LIOTHYRONINE 4.0 1 5.24
CHEMBL1624 LEVOTHYROXINE 4.0 1 4.92
CHEMBL4638870 1 4.89
CHEMBL595 PIOGLITAZONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL549748 TETRAC EC50 = 100.0 nM 7.00
CHEMBL4637025 EC50 = 300.0 nM 6.52
CHEMBL41632 TIRATRICOL EC50 = 370.0 nM 6.43
CHEMBL1743304 REVERSE TRIIODOTHYRONINE EC50 = 3800.0 nM 5.42
CHEMBL1544 LIOTHYRONINE EC50 = 5800.0 nM 5.24
CHEMBL1624 LEVOTHYROXINE EC50 = 12000.0 nM 4.92
CHEMBL4638870 EC50 = 12900.0 nM 4.89
CHEMBL595 PIOGLITAZONE Activity - -