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TargetThyroid hormone receptor
LigandBDBM18875
Substrate/CompetitorBDBM18860
Meas. Tech.TRalpha-Binding Assay and Thyroid Response Element (TRAFalpha1) Reporter Assay.
pH7±n/a
Temperature277.15±n/a K
IC50 9.8±1.0 nM
EC50 2.3±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
Name:Thyroid hormone receptor
Synonyms:C-erbA-alpha | EAR-7 | EAR7 | Nuclear receptor subfamily 1 group A member 1 | Thyroid Hormone Receptor (TR-alpha) | Thyroid hormone receptor | Thyroid hormone receptor alpha | c-erbA-1
Type:Receptor
Mol. Mass.:54818.00
Organism:Homo sapiens (Human)
Description:Recombinant hThR was obtained from nuclear extracts from SF9 cells infected with baculovirus vectors encoding for ThRalpha 1.
Residue:490
Sequence:
MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA
TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM
AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA
QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS
ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF
ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI
PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL
GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC
EDLAGNAASP
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  Blast E-value cutoff:
BDBM18875
BDBM18860
NameBDBM18875
Synonyms:(2R)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid | N-acylated-alpha-amino acid derivative, 3e
TypeSmall organic molecule
Emp. Form.C22H25Br2NO5
Mol. Mass.543.246
SMILESCC(C)[C@@H](NC(=O)Cc1cc(Br)c(Oc2ccc(O)c(c2)C(C)C)c(Br)c1)C(O)=O |r|
Structure
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