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Reaction Details
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TargetThyroid hormone receptor beta
LigandBDBM18913
Substrate/CompetitorBDBM18860
Meas. Tech.TRalpha-Binding Assay.
IC50 0.2±n/a nM
Citation Hangeland, JJDoweyko, AMDejneka, TFriends, TJDevasthale, PMellström, KSandberg, JGrynfarb, MSack, JSEinspahr, HFärnegård, MHusman, BLjunggren, JKoehler, KSheppard, CMalm, JRyono, DE Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta. Bioorg Med Chem Lett14:3549-53 (2004) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Thyroid hormone receptor beta
Name:Thyroid hormone receptor beta
Synonyms:ERBA2 | NR1A2 | Nuclear receptor subfamily 1 group A member 2 | THB_HUMAN | THR1 | THRB | c-erbA-2 | c-erbA-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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  Blast E-value cutoff:
BDBM18913
BDBM18860
NameBDBM18913
Synonyms:2-{3,5-dichloro-4-[3-(3-ethylphenyl)-4-hydroxyphenoxy]phenyl}acetic acid | 4-hydroxy bioisosteric thyromimetics, 3 | 4-hydroxy thyromimetic, 9e
TypeSmall organic molecule
Emp. Form.C22H18Cl2O4
Mol. Mass.417.282
SMILESCCc1cccc(c1)-c1cc(Oc2c(Cl)cc(CC(O)=O)cc2Cl)ccc1O
Structure
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