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TargetThyroid Hormone Receptor (TR-beta)
LigandBDBM50012911
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1351953
EC50 220±n/a nM
Citation Kelly, MJPietranico-Cole, SLarigan, JDHaynes, NEReynolds, CHScott, NVermeulen, JDvorozniak, MConde-Knape, KHuang, KSSo, SSThakkar, KQian, YBanner, BMennona, FDanzi, SKlein, ITaub, RTilley, J Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor▀ agonist in clinical trials for the treatment of dyslipidemia. J Med Chem57:3912-23 (2014) [PubMed]  Article
More Info.:Get all data from this article,  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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50012911
NameBDBM50012911
Synonyms:CHEMBL3261332 | USRE46024, 12
TypeSmall organic molecule
Emp. Form.C18H14Cl2N6O3
Mol. Mass.433.248
SMILESCC(C)c1cc(Cc2c(Cl)cc(cc2Cl)-n2nc(C#N)c(=O)[nH]c2=O)n[nH]c1=O
Structure
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