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Assay Detail

CHEMBL811714

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

Binding
Half-maximum activation of human Thyroid hormone receptor beta 1 (hTRbeta1)
4
Total Activities
4
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 beta (CHEMBL1947)
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
EC50 4 7.39 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 1 8.70
CHEMBL107400 SOBETIROME 2.0 1 8.15
CHEMBL109430 1 6.42
CHEMBL111953 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE EC50 = 2.0 nM 8.70
CHEMBL107400 SOBETIROME EC50 = 7.0 nM 8.15
CHEMBL109430 EC50 = 380.0 nM 6.42
CHEMBL111953 EC50 = 500.0 nM 6.30