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Assay Detail

CHEMBL752718

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

Binding
Ability to inhibit the bound [125I]L-T3 rat liver Nuclear L-triiodothyronine receptor is determined in vitro.
16
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Thyroid hormone receptor beta (CHEMBL3917)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of oxamic acid and acetic acid derivatives related to L-thyronine.
Yokoyama N, Walker GN, Main AJ, Stanton JL, Morrissey MM, Boehm C, Engle A, Neubert AD, Wasvary JM, Stephan ZF.
J Med Chem (1995) 38 : 695 -707
PubMed 7861417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.51 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350265 1 10.00
CHEMBL289343 1 9.96
CHEMBL159682 AXITIROME 2.0 3 9.85
CHEMBL159976 1 9.51
CHEMBL163380 1 8.96
CHEMBL162692 1 8.82
CHEMBL347713 1 8.46
CHEMBL352126 1 7.92
CHEMBL163611 1 7.47
CHEMBL349076 1 7.32
CHEMBL160203 1 7.24
CHEMBL350930 1 6.40
CHEMBL161776 1 6.26
CHEMBL163994 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350265 IC50 = 0.1 nM 10.00
CHEMBL289343 IC50 = 0.11 nM 9.96
CHEMBL159682 AXITIROME IC50 = 0.14 nM 9.85
CHEMBL159682 AXITIROME IC50 = 0.16 nM 9.80
CHEMBL159682 AXITIROME IC50 = 0.23 nM 9.64
CHEMBL159976 IC50 = 0.31 nM 9.51
CHEMBL163380 IC50 = 1.1 nM 8.96
CHEMBL162692 IC50 = 1.5 nM 8.82
CHEMBL347713 IC50 = 3.5 nM 8.46
CHEMBL352126 IC50 = 12.0 nM 7.92
CHEMBL163611 IC50 = 34.0 nM 7.47
CHEMBL349076 IC50 = 48.0 nM 7.32
CHEMBL160203 IC50 = 58.0 nM 7.24
CHEMBL350930 IC50 = 400.0 nM 6.40
CHEMBL161776 IC50 = 550.0 nM 6.26
CHEMBL163994 IC50 > 5000.0 nM -