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Assay Detail

CHEMBL4629620

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

Binding
Agonist activity at THRalpha (unknown origin) incubated for 14 to 16 hrs by dual glo luciferase reporter gene assay
4
Total Activities
4
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

Thyroid hormone receptor alpha (CHEMBL1860)
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 4 7.45 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1624 LEVOTHYROXINE 4.0 1 7.72
CHEMBL549748 TETRAC -1.0 1 7.70
CHEMBL4637025 1 7.52
CHEMBL4638870 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1624 LEVOTHYROXINE EC50 = 19.0 nM 7.72
CHEMBL549748 TETRAC EC50 = 20.0 nM 7.70
CHEMBL4637025 EC50 = 30.0 nM 7.52
CHEMBL4638870 EC50 = 140.0 nM 6.85