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Assay Detail

CHEMBL880611

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

Binding
Inhibitory concentration against cloned human thyroid hormone receptor alpha 1
13
Total Activities
13
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

A new class of high affinity thyromimetics containing a phenyl-naphthylene core.
Hangeland JJ, Friends TJ, Doweyko AM, Mellström K, Sandberg J, Grynfarb M, Ryono DE.
Bioorg Med Chem Lett (2005) 15 : 4579 -4584
PubMed 16099653 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.55 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 1 9.62
CHEMBL194242 1 8.37
CHEMBL198367 1 8.27
CHEMBL198875 1 7.89
CHEMBL196642 1 7.85
CHEMBL193864 1 7.72
CHEMBL41036 1 7.60
CHEMBL193615 1 7.32
CHEMBL372428 1 7.21
CHEMBL195079 1 7.00
CHEMBL371245 1 6.96
CHEMBL196613 1 6.90
CHEMBL193851 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE IC50 = 0.24 nM 9.62
CHEMBL194242 IC50 = 4.3 nM 8.37
CHEMBL198367 IC50 = 5.4 nM 8.27
CHEMBL198875 IC50 = 13.0 nM 7.89
CHEMBL196642 IC50 = 14.0 nM 7.85
CHEMBL193864 IC50 = 19.0 nM 7.72
CHEMBL41036 IC50 = 25.0 nM 7.60
CHEMBL193615 IC50 = 48.0 nM 7.32
CHEMBL372428 IC50 = 62.0 nM 7.21
CHEMBL195079 IC50 = 101.0 nM 7.00
CHEMBL371245 IC50 = 109.0 nM 6.96
CHEMBL196613 IC50 = 125.0 nM 6.90
CHEMBL193851 IC50 = 3605.0 nM 5.44