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Assay Detail

CHEMBL832459

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Binding
Inhibitory activity against human Thyroid hormone receptor beta
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor.
Hedfors A, Appelqvist T, Carlsson B, Bladh LG, Litten C, Agback P, Grynfarb M, Koehler KF, Malm J.
J Med Chem (2005) 48 : 3114 -3117
PubMed 15857115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.77 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192427 1 6.72
CHEMBL195556 1 6.44
CHEMBL425557 1 6.22
CHEMBL192142 1 6.11
CHEMBL425366 1 6.10
CHEMBL192426 1 6.09
CHEMBL193198 1 6.04
CHEMBL192639 1 5.82
CHEMBL195855 1 5.75
CHEMBL192490 1 5.72
CHEMBL157885 1 5.29
CHEMBL193152 1 5.24
CHEMBL192508 1 4.75
CHEMBL192346 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192427 IC50 = 190.0 nM 6.72
CHEMBL195556 IC50 = 360.0 nM 6.44
CHEMBL425557 IC50 = 600.0 nM 6.22
CHEMBL192142 IC50 = 770.0 nM 6.11
CHEMBL425366 IC50 = 800.0 nM 6.10
CHEMBL192426 IC50 = 810.0 nM 6.09
CHEMBL193198 IC50 = 910.0 nM 6.04
CHEMBL192639 IC50 = 1500.0 nM 5.82
CHEMBL195855 IC50 = 1800.0 nM 5.75
CHEMBL192490 IC50 = 1900.0 nM 5.72
CHEMBL157885 IC50 = 5100.0 nM 5.29
CHEMBL193152 IC50 = 5700.0 nM 5.24
CHEMBL192508 IC50 = 18000.0 nM 4.75
CHEMBL192346 IC50 = 32000.0 nM 4.50