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Assay Detail

CHEMBL872845

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

Binding
In vitro inhibition of the bound [125I]L-T3 rat liver nuclear L-triiodothyronine receptor
31
Total Activities
30
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 31 8.59 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL163221 1 10.00
CHEMBL41632 TIRATRICOL 3.0 1 9.82
CHEMBL46882 1 9.72
CHEMBL350049 1 9.64
CHEMBL164421 1 9.59
CHEMBL163324 1 9.57
CHEMBL159334 1 9.43
CHEMBL161828 1 9.37
CHEMBL423977 1 9.17
CHEMBL159595 1 9.10
CHEMBL350199 1 9.02
CHEMBL161535 1 9.00
CHEMBL348983 1 8.96
CHEMBL434476 1 8.82
CHEMBL1544 LIOTHYRONINE 4.0 2 8.74
CHEMBL159610 1 8.60
CHEMBL163268 1 8.52
CHEMBL346112 1 8.48
CHEMBL163020 1 8.44
CHEMBL163067 1 8.35
CHEMBL163320 1 8.22
CHEMBL264041 1 8.10
CHEMBL161245 1 7.85
CHEMBL441101 1 7.66
CHEMBL559 DEXTROTHYROXINE 4.0 1 7.46
CHEMBL163283 1 7.33
CHEMBL350336 1 7.32
CHEMBL163228 1 7.32
CHEMBL163518 1 7.28
CHEMBL163805 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL163221 IC50 = 0.1 nM 10.00
CHEMBL41632 TIRATRICOL IC50 = 0.15 nM 9.82
CHEMBL46882 IC50 = 0.19 nM 9.72
CHEMBL350049 IC50 = 0.23 nM 9.64
CHEMBL164421 IC50 = 0.26 nM 9.59
CHEMBL163324 IC50 = 0.27 nM 9.57
CHEMBL159334 IC50 = 0.37 nM 9.43
CHEMBL161828 IC50 = 0.43 nM 9.37
CHEMBL423977 IC50 = 0.68 nM 9.17
CHEMBL159595 IC50 = 0.8 nM 9.10
CHEMBL350199 IC50 = 0.95 nM 9.02
CHEMBL161535 IC50 = 1.0 nM 9.00
CHEMBL348983 IC50 = 1.1 nM 8.96
CHEMBL434476 IC50 = 1.5 nM 8.82
CHEMBL1544 LIOTHYRONINE IC50 = 1.8 nM 8.74
CHEMBL159610 IC50 = 2.5 nM 8.60
CHEMBL163268 IC50 = 3.0 nM 8.52
CHEMBL346112 IC50 = 3.3 nM 8.48
CHEMBL163020 IC50 = 3.6 nM 8.44
CHEMBL1544 LIOTHYRONINE IC50 = 4.4 nM 8.36
CHEMBL163067 IC50 = 4.5 nM 8.35
CHEMBL163320 IC50 = 6.0 nM 8.22
CHEMBL264041 IC50 = 8.0 nM 8.10
CHEMBL161245 IC50 = 14.0 nM 7.85
CHEMBL441101 IC50 = 22.0 nM 7.66
CHEMBL559 DEXTROTHYROXINE IC50 = 35.0 nM 7.46
CHEMBL163283 IC50 = 47.0 nM 7.33
CHEMBL350336 IC50 = 48.0 nM 7.32
CHEMBL163228 IC50 = 48.0 nM 7.32
CHEMBL163518 IC50 = 52.0 nM 7.28
CHEMBL163805 IC50 = 120.0 nM 6.92