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Assay Detail

CHEMBL765465

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

Binding
In vitro inhibition of bound [125I]L-T3 rat plasma membrane 3,5,3'' L-triiodothyronine receptor
27
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Plasma
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 27 6.08 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1544 LIOTHYRONINE 4.0 2 7.00
CHEMBL163067 1 6.70
CHEMBL159976 1 6.16
CHEMBL163221 1 6.10
CHEMBL163268 1 6.00
CHEMBL163228 1 6.00
CHEMBL559 DEXTROTHYROXINE 4.0 1 5.60
CHEMBL423977 1 5.52
CHEMBL163320 1 5.40
CHEMBL352126 1 -
CHEMBL163324 1 -
CHEMBL163380 1 -
CHEMBL347713 1 -
CHEMBL159595 1 -
CHEMBL162692 1 -
CHEMBL350199 1 -
CHEMBL441101 1 -
CHEMBL161828 1 -
CHEMBL348983 1 -
CHEMBL350265 1 -
CHEMBL41632 TIRATRICOL 3.0 1 -
CHEMBL289343 1 -
CHEMBL46882 1 -
CHEMBL350336 1 -
CHEMBL159682 AXITIROME 2.0 1 -
CHEMBL159334 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1544 LIOTHYRONINE IC50 = 100.0 nM 7.00
CHEMBL163067 IC50 = 200.0 nM 6.70
CHEMBL1544 LIOTHYRONINE IC50 = 500.0 nM 6.30
CHEMBL159976 IC50 = 700.0 nM 6.16
CHEMBL163221 IC50 = 800.0 nM 6.10
CHEMBL163268 IC50 = 1000.0 nM 6.00
CHEMBL163228 IC50 = 1000.0 nM 6.00
CHEMBL559 DEXTROTHYROXINE IC50 = 2500.0 nM 5.60
CHEMBL423977 IC50 = 3000.0 nM 5.52
CHEMBL163320 IC50 = 4000.0 nM 5.40
CHEMBL352126 IC50 > 5000.0 nM -
CHEMBL163324 IC50 > 5000.0 nM -
CHEMBL163380 IC50 > 5000.0 nM -
CHEMBL347713 IC50 > 5000.0 nM -
CHEMBL159595 IC50 > 5000.0 nM -
CHEMBL162692 IC50 > 5000.0 nM -
CHEMBL350199 IC50 > 5000.0 nM -
CHEMBL441101 IC50 > 5000.0 nM -
CHEMBL161828 IC50 > 5000.0 nM -
CHEMBL159334 IC50 > 5000.0 nM -
CHEMBL348983 IC50 > 5000.0 nM -
CHEMBL350265 IC50 > 5000.0 nM -
CHEMBL41632 TIRATRICOL IC50 > 5000.0 nM -
CHEMBL289343 IC50 > 5000.0 nM -
CHEMBL46882 IC50 > 5000.0 nM -
CHEMBL350336 IC50 > 5000.0 nM -
CHEMBL159682 AXITIROME IC50 > 5000.0 nM -