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Assay Detail

CHEMBL827048

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Binding
Inhibitory activity against human TRAFalpha
8
Total Activities
8
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 alpha (CHEMBL1860)
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 8 6.11 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192142 1 6.38
CHEMBL192427 1 6.28
CHEMBL195556 1 6.22
CHEMBL192639 1 6.16
CHEMBL425366 1 6.09
CHEMBL193198 1 5.96
CHEMBL157885 1 5.66
CHEMBL425557 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192142 IC50 = 420.0 nM 6.38
CHEMBL192427 IC50 = 530.0 nM 6.28
CHEMBL195556 IC50 = 600.0 nM 6.22
CHEMBL192639 IC50 = 700.0 nM 6.16
CHEMBL425366 IC50 = 820.0 nM 6.09
CHEMBL193198 IC50 = 1100.0 nM 5.96
CHEMBL157885 IC50 = 2200.0 nM 5.66
CHEMBL425557 IC50 > 10000.0 nM -