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Assay Detail

CHEMBL5166797

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Binding
Agonist activity at human TRbeta H435 mutant expressed in Escherichia coli BL21 (DE3) cells by alphascreen assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
Li Q, Yao B, Zhao S, Lu Z, Zhang Y, Xiang Q, Wu X, Yu H, Zhang C, Li J, Zhuang X, Wu D, Li Y, Xu Y.
J Med Chem (2022) 65 : 7193 -7211
PubMed 35507418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.58 5.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5200322 1 5.87
CHEMBL5178993 1 5.62
CHEMBL5181604 1 5.53
CHEMBL5173831 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5200322 EC50 = 1344.0 nM 5.87
CHEMBL5178993 EC50 = 2386.0 nM 5.62
CHEMBL5181604 EC50 = 2925.0 nM 5.53
CHEMBL5173831 EC50 = 5277.0 nM 5.28