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Assay Detail

CHEMBL986574

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Functional
Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells by TRE-luciferase assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands.
Raval S, Raval P, Bandyopadhyay D, Soni K, Yevale D, Jogiya D, Modi H, Joharapurkar A, Gandhi N, Jain MR, Patel PR.
Bioorg Med Chem Lett (2008) 18 : 3919 -3924
PubMed 18585912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.54 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41036 1 8.95
CHEMBL480312 1 7.16
CHEMBL480313 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41036 EC50 = 1.12 nM 8.95
CHEMBL480312 EC50 = 70.0 nM 7.16
CHEMBL480313 EC50 = 317.0 nM 6.50