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Assay Detail

CHEMBL5250901

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

Binding
Agonist activity at human THRbeta transfected in Huh7 cells co-transfected with luciferase reporter plasmid assessed as reduction in luciferase activity incubated for 16 hrs by Steady-Glo luciferase assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Huh-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thyroid hormone receptor beta (CHEMBL1947)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Highly Potent and Selective Thyroid Hormone Receptor β Agonists for the Treatment of Nonalcoholic Steatohepatitis.
Hu L, Gu Y, Liang J, Ning M, Yang J, Zhang Y, Qu H, Yang Y, Leng Y, Zhou B.
J Med Chem (2023) 66 : 3284 -3300
PubMed 36799411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.28 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 1 8.96
CHEMBL5267199 1 8.05
CHEMBL5274251 1 7.70
CHEMBL5281631 1 7.70
CHEMBL5286305 1 7.52
CHEMBL5279191 1 7.52
CHEMBL5281151 1 7.52
CHEMBL5284123 1 7.40
CHEMBL5266872 1 7.40
CHEMBL5271234 1 7.16
CHEMBL5268293 1 6.70
CHEMBL5284849 1 6.70
CHEMBL5269031 1 6.68
CHEMBL5283585 1 6.19
CHEMBL3261331 RESMETIROM 4.0 1 6.00
CHEMBL5290997 1 -
CHEMBL5281233 1 -
CHEMBL5269734 1 -
CHEMBL5277807 1 -
CHEMBL5290804 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE EC50 = 1.1 nM 8.96
CHEMBL5267199 EC50 = 9.0 nM 8.05
CHEMBL5274251 EC50 = 20.0 nM 7.70
CHEMBL5281631 EC50 = 20.0 nM 7.70
CHEMBL5286305 EC50 = 30.0 nM 7.52
CHEMBL5279191 EC50 = 30.0 nM 7.52
CHEMBL5281151 EC50 = 30.0 nM 7.52
CHEMBL5284123 EC50 = 40.0 nM 7.40
CHEMBL5266872 EC50 = 40.0 nM 7.40
CHEMBL5271234 EC50 = 70.0 nM 7.16
CHEMBL5268293 EC50 = 200.0 nM 6.70
CHEMBL5284849 EC50 = 200.0 nM 6.70
CHEMBL5269031 EC50 = 210.0 nM 6.68
CHEMBL5283585 EC50 = 650.0 nM 6.19
CHEMBL3261331 RESMETIROM EC50 = 990.0 nM 6.00
CHEMBL5290997 EC50 > 100000.0 nM -
CHEMBL5281233 EC50 > 100000.0 nM -
CHEMBL5269734 EC50 > 3700.0 nM -
CHEMBL5277807 EC50 > 1200.0 nM -
CHEMBL5290804 EC50 > 33000.0 nM -