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Assay Detail

CHEMBL814596

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

Binding
Concentration required to inhibit 50% of binding of [125I]-T3 to human Thyroid hormone receptor alpha-1 in CHO-K1 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone.
Carlsson B, Singh BN, Temciuc M, Nilsson S, Li YL, Mellin C, Malm J.
J Med Chem (2002) 45 : 623 -630
PubMed 11806713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.87 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL633 AMIODARONE 4.0 1 6.19
CHEMBL160883 1 6.09
CHEMBL160703 1 5.85
CHEMBL157885 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL633 AMIODARONE IC50 = 650.0 nM 6.19
CHEMBL160883 IC50 = 820.0 nM 6.09
CHEMBL160703 IC50 = 1400.0 nM 5.85
CHEMBL157885 IC50 = 4500.0 nM 5.35