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Assay Detail

CHEMBL814598

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Binding
Binding affinity against human Thyroid hormone receptor alpha-1 (hTRalpha1) using radiolabeled T3
7
Total Activities
7
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

Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
Nguyen NH, Apriletti JW, Cunha Lima ST, Webb P, Baxter JD, Scanlan TS.
J Med Chem (2002) 45 : 3310 -3320
PubMed 12109914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 7.65 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 1 10.00
CHEMBL107400 SOBETIROME 2.0 1 8.74
CHEMBL109430 1 8.28
CHEMBL109279 1 7.03
CHEMBL112087 1 6.70
CHEMBL110158 1 6.48
CHEMBL111953 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE Kd = 0.1 nM 10.00
CHEMBL107400 SOBETIROME Kd = 1.8 nM 8.74
CHEMBL109430 Kd = 5.2 nM 8.28
CHEMBL109279 Kd = 93.0 nM 7.03
CHEMBL112087 Kd = 200.0 nM 6.70
CHEMBL110158 Kd = 330.0 nM 6.48
CHEMBL111953 Kd = 490.0 nM 6.31