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Assay Detail

CHEMBL939179

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

Binding
Displacement of [125I]T3 from human TRalpha receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thyroid hormone receptor alpha (CHEMBL1860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Characterization of thyroid hormone receptor alpha (TRalpha)-specific analogs with varying inner- and outer-ring substituents.
Ocasio CA, Scanlan TS.
Bioorg Med Chem (2008) 16 : 762 -770
PubMed 17988877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 7.76 10.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 1 10.24
CHEMBL263630 1 8.92
CHEMBL264153 1 7.82
CHEMBL263631 1 7.77
CHEMBL259096 1 7.62
CHEMBL260482 1 7.60
CHEMBL264152 1 7.38
CHEMBL258886 1 7.37
CHEMBL264410 1 7.09
CHEMBL407819 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE Kd = 0.058 nM 10.24
CHEMBL263630 Kd = 1.2 nM 8.92
CHEMBL264153 Kd = 15.0 nM 7.82
CHEMBL263631 Kd = 17.0 nM 7.77
CHEMBL259096 Kd = 24.0 nM 7.62
CHEMBL260482 Kd = 25.0 nM 7.60
CHEMBL264152 Kd = 42.0 nM 7.38
CHEMBL258886 Kd = 43.0 nM 7.37
CHEMBL264410 Kd = 82.0 nM 7.09
CHEMBL407819 Kd = 1700.0 nM 5.77