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Assay Detail

CHEMBL814601

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Binding
Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor beta) was determined
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.
Ye L, Li YL, Mellström K, Mellin C, Bladh LG, Koehler K, Garg N, Garcia Collazo AM, Litten C, Husman B, Persson K, Ljunggren J, Grover G, Sleph PG, George R, Malm J.
J Med Chem (2003) 46 : 1580 -1588
PubMed 12699376 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 9.64 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291053 THYROPROPIC ACID 2.0 1 10.72
CHEMBL289343 1 10.60
CHEMBL41632 TIRATRICOL 3.0 1 10.32
CHEMBL39174 1 10.02
CHEMBL41314 1 9.96
CHEMBL418432 1 9.82
CHEMBL557 DETROTHYRONINE 2.0 1 9.59
CHEMBL41036 1 8.96
CHEMBL289965 1 8.68
CHEMBL40738 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291053 THYROPROPIC ACID IC50 = 0.019 nM 10.72
CHEMBL289343 IC50 = 0.025 nM 10.60
CHEMBL41632 TIRATRICOL IC50 = 0.048 nM 10.32
CHEMBL39174 IC50 = 0.095 nM 10.02
CHEMBL41314 IC50 = 0.11 nM 9.96
CHEMBL418432 IC50 = 0.15 nM 9.82
CHEMBL557 DETROTHYRONINE IC50 = 0.26 nM 9.59
CHEMBL41036 IC50 = 1.1 nM 8.96
CHEMBL289965 IC50 = 2.1 nM 8.68
CHEMBL40738 IC50 = 21.0 nM 7.68