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Assay Detail

CHEMBL2212125

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

Binding
Binding affinity to TRbeta1
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Thyroid hormone receptor beta (CHEMBL1947)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia.
Joharapurkar AA, Dhote VV, Jain MR.
J Med Chem (2012) 55 : 5649 -5675
PubMed 22512468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.62 10.22
EC50 2 8.94 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203777 1 10.22
CHEMBL41036 1 9.43
CHEMBL2203702 1 9.33
CHEMBL235788 1 8.54
CHEMBL471897 MB07811 2.0 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203777 Ki = 0.06 nM 10.22
CHEMBL41036 Ki = 0.37 nM 9.43
CHEMBL2203702 EC50 = 0.47 nM 9.33
CHEMBL235788 EC50 = 2.9 nM 8.54
CHEMBL471897 MB07811 Ki = 600.0 nM 6.22