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Assay Detail

CHEMBL4629574

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

Binding
Binding affinity to recombinant PPARgamma LBD (unknown origin) by isothermal titration calorimetry
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

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
Kd 5 6.48 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL549748 TETRAC -1.0 1 6.96
CHEMBL41632 TIRATRICOL 3.0 1 6.70
CHEMBL1624 LEVOTHYROXINE 4.0 1 6.40
CHEMBL1743304 REVERSE TRIIODOTHYRONINE 1 6.20
CHEMBL1544 LIOTHYRONINE 4.0 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL549748 TETRAC Kd = 110.0 nM 6.96
CHEMBL41632 TIRATRICOL Kd = 200.0 nM 6.70
CHEMBL1624 LEVOTHYROXINE Kd = 400.0 nM 6.40
CHEMBL1743304 REVERSE TRIIODOTHYRONINE Kd = 630.0 nM 6.20
CHEMBL1544 LIOTHYRONINE Kd = 710.0 nM 6.15