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Assay Detail

CHEMBL3399152

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

Binding
Displacement of [125I]-L-3,5,3'-triiodothyronine from human TRalpha expressed in human Hela cell lysate measured after overnight incubation by competition binding assays
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thyroid hormone receptor alpha (CHEMBL1860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists.
Burkholder TP, Cunningham BE, Clayton JR, Lander PA, Brown ML, Doti RA, Durst GL, Montrose-Rafizadeh C, King C, Osborne HE, Amos RM, Zink RW, Stramm LE, Burris TP, Cardona G, Konkol DL, Reidy C, Christe ME, Genin MJ.
Bioorg Med Chem Lett (2015) 25 : 1377 -1380
PubMed 25752984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.14 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3397337 1 9.46
CHEMBL3397339 1 9.42
CHEMBL3397341 1 9.29
CHEMBL3397336 1 8.96
CHEMBL3397338 1 8.69
CHEMBL3397340 1 8.56
CHEMBL3397335 1 8.11
CHEMBL3397342 1 8.00
CHEMBL3397333 1 7.87
CHEMBL3397334 1 7.79
CHEMBL3397344 1 7.49
CHEMBL3397343 1 7.44
CHEMBL3397345 1 7.33
CHEMBL3397346 1 7.05
CHEMBL3397347 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3397337 Ki = 0.35 nM 9.46
CHEMBL3397339 Ki = 0.38 nM 9.42
CHEMBL3397341 Ki = 0.51 nM 9.29
CHEMBL3397336 Ki = 1.09 nM 8.96
CHEMBL3397338 Ki = 2.05 nM 8.69
CHEMBL3397340 Ki = 2.77 nM 8.56
CHEMBL3397335 Ki = 7.74 nM 8.11
CHEMBL3397342 Ki = 9.98 nM 8.00
CHEMBL3397333 Ki = 13.45 nM 7.87
CHEMBL3397334 Ki = 16.33 nM 7.79
CHEMBL3397344 Ki = 32.33 nM 7.49
CHEMBL3397343 Ki = 36.53 nM 7.44
CHEMBL3397345 Ki = 46.55 nM 7.33
CHEMBL3397346 Ki = 89.89 nM 7.05
CHEMBL3397347 Ki = 199.97 nM 6.70