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Assay Detail

CHEMBL866541

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

Binding
Inhibition of human TR-alpha-1 by radioligand binding assay
8
Total Activities
8
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 alpha (CHEMBL1860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta.
Garcia Collazo AM, Koehler KF, Garg N, Färnegårdh M, Husman B, Ye L, Ljunggren J, Mellström K, Sandberg J, Grynfarb M, Ahola H, Malm J.
Bioorg Med Chem Lett (2006) 16 : 1240 -1244
PubMed 16338239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.43 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL557 DETROTHYRONINE 2.0 1 9.62
CHEMBL203777 1 8.85
CHEMBL425939 1 8.60
CHEMBL203828 1 7.42
CHEMBL203555 1 6.70
CHEMBL378593 1 6.60
CHEMBL251439 1 6.21
CHEMBL250880 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL557 DETROTHYRONINE IC50 = 0.24 nM 9.62
CHEMBL203777 IC50 = 1.4 nM 8.85
CHEMBL425939 IC50 = 2.5 nM 8.60
CHEMBL203828 IC50 = 38.0 nM 7.42
CHEMBL203555 IC50 = 200.0 nM 6.70
CHEMBL378593 IC50 = 250.0 nM 6.60
CHEMBL251439 IC50 = 620.0 nM 6.21
CHEMBL250880 IC50 = 3500.0 nM 5.46