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Assay Detail

CHEMBL896601

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

Binding
Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.
Garg N, Li YL, Garcia Collazo AM, Litten C, Ryono DE, Zhang M, Caringal Y, Brigance RP, Meng W, Washburn WN, Agback P, Mellström K, Rehnmark S, Rahimi-Ghadim M, Norin T, Grynfarb M, Sandberg J, Grover G, Malm J.
Bioorg Med Chem Lett (2007) 17 : 4131 -4134
PubMed 17543524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.32 10.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39174 1 10.02
CHEMBL1544 LIOTHYRONINE 4.0 1 9.59
CHEMBL236289 1 9.57
CHEMBL236291 1 9.22
CHEMBL391512 1 9.15
CHEMBL236290 1 9.11
CHEMBL41036 1 8.96
CHEMBL391367 1 8.89
CHEMBL236080 1 8.57
CHEMBL440975 1 8.23
CHEMBL236499 1 7.92
CHEMBL236498 1 7.58
CHEMBL391513 1 6.54
CHEMBL393201 1 5.85
CHEMBL236500 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39174 IC50 = 0.095 nM 10.02
CHEMBL1544 LIOTHYRONINE IC50 = 0.26 nM 9.59
CHEMBL236289 IC50 = 0.27 nM 9.57
CHEMBL236291 IC50 = 0.6 nM 9.22
CHEMBL391512 IC50 = 0.71 nM 9.15
CHEMBL236290 IC50 = 0.78 nM 9.11
CHEMBL41036 IC50 = 1.1 nM 8.96
CHEMBL391367 IC50 = 1.3 nM 8.89
CHEMBL236080 IC50 = 2.7 nM 8.57
CHEMBL440975 IC50 = 5.9 nM 8.23
CHEMBL236499 IC50 = 12.0 nM 7.92
CHEMBL236498 IC50 = 26.0 nM 7.58
CHEMBL391513 IC50 = 290.0 nM 6.54
CHEMBL393201 IC50 = 1400.0 nM 5.85
CHEMBL236500 IC50 = 2600.0 nM 5.58