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Assay Detail

CHEMBL969512

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

Binding
Displacement of [125I]T3 from recombinant thyroid hormone receptor alpha expressed in sf9 cells by scintillation proximity assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index.
Erion MD, Cable EE, Ito BR, Jiang H, Fujitaki JM, Finn PD, Zhang BH, Hou J, Boyer SH, van Poelje PD, Linemeyer DL.
Proc Natl Acad Sci U S A (2007) 104 : 15490 -15495
PubMed 17878314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.54 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 1 9.66
CHEMBL41036 1 8.14
CHEMBL471488 MB07344 -1.0 1 7.45
CHEMBL471897 MB07811 2.0 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE Ki = 0.22 nM 9.66
CHEMBL41036 Ki = 7.18 nM 8.14
CHEMBL471488 MB07344 Ki = 35.2 nM 7.45
CHEMBL471897 MB07811 Ki = 12500.0 nM 4.90