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TargetThyroid Hormone Receptor (TR-beta)
LigandBDBM18882
Substrate/CompetitorBDBM18860
Meas. Tech.TRbeta-Binding Assay and Thyroid Response Element (TRAFbeta1) Reporter Assay.
pH7±n/a
Temperature277.15±n/a K
IC50 2600±240 nM
EC50 1100±n/a nM
Citation Garg NLi YLGarcia Collazo AMLitten CRyono DEZhang MCaringal YBrigance RPMeng WWashburn WNAgback PMellström KRehnmark SRahimi-Ghadim MNorin TGrynfarb MSandberg JGrover GMalm J Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. Bioorg Med Chem Lett 17:4131-4 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Thyroid Hormone Receptor (TR-beta)
Name:Thyroid hormone receptor
Synonyms:Nuclear receptor subfamily 1 group A member 2 | Thyroid hormone receptor | Thyroid hormone receptor beta
Type:Receptor
Mol. Mass.:52793.62
Organism:Homo sapiens (Human)
Description:Recombinant hThR was obtained from nuclear extracts from SF9 cells infected with baculovirus vectors encoding for ThRbeta 1.
Residue:461
Sequence:
MTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQ
TTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYR
CITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVL
DDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWK
QKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCED
QIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSL
SSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPK
LLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED
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BDBM18882
BDBM18860
NameBDBM18882
Synonyms:(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-methyl-5-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid | N-acylated-alpha-amino acid derivative, 12
TypeSmall organic molecule
Emp. Form.C23H27Br2NO5
Mol. Mass.557.272
SMILESCC(C)[C@H](NC(=O)Cc1cc(Br)c(Oc2cc(C)c(O)c(c2)C(C)C)c(Br)c1)C(O)=O |r|
Structure
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