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Assay Detail

CHEMBL814593

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Binding
Binding affinity towards thyroid hormone receptor (hTR alpha 1)
6
Total Activities
6
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 designed antagonist of the thyroid hormone receptor.
Yoshihara HA, Apriletti JW, Baxter JD, Scanlan TS.
Bioorg Med Chem Lett (2001) 11 : 2821 -2825
PubMed 11597408 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 6.90 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 1 9.77
CHEMBL318132 1 6.95
CHEMBL264527 1 6.62
CHEMBL97613 1 6.37
CHEMBL97187 1 5.85
CHEMBL98135 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE Kd = 0.17 nM 9.77
CHEMBL318132 Kd = 112.0 nM 6.95
CHEMBL264527 Kd = 240.0 nM 6.62
CHEMBL97613 Kd = 430.0 nM 6.37
CHEMBL97187 Kd = 1400.0 nM 5.85
CHEMBL98135 Kd = 1400.0 nM 5.85