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Assay Detail

CHEMBL885330

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

Binding
Effective concentration binding towards TRalpha in E25B2 cells (agonistic activity)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type E25B2
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.
Dow RL, Schneider SR, Paight ES, Hank RF, Chiang P, Cornelius P, Lee E, Newsome WP, Swick AG, Spitzer J, Hargrove DM, Patterson TA, Pandit J, Chrunyk BA, LeMotte PK, Danley DE, Rosner MH, Ammirati MJ, Simons SP, Schulte GK, Tate BF, DaSilva-Jardine P.
Bioorg Med Chem Lett (2003) 13 : 379 -382
PubMed 12565933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.48 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 1 8.70
CHEMBL124205 1 7.92
CHEMBL125946 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE EC50 = 2.0 nM 8.70
CHEMBL124205 EC50 = 12.0 nM 7.92
CHEMBL125946 EC50 = 1500.0 nM 5.82