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TargetThyroid hormone receptor
LigandBDBM18885
Substrate/CompetitorBDBM18860
Meas. Tech.TRalpha-Binding Assay.
pH7±n/a
Temperature277.15±n/a K
IC50 93±29 nM
Citation Koehler KGordon SBrandt PCarlsson BBäcksbro-Saeidi AApelqvist TAgback PGrover GJNelson WGrynfarb MFärnegård MRehnmark SMalm J Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. J Med Chem 49:6635-7 (2006) [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:
BDBM18885
BDBM18860
NameBDBM18885
Synonyms:2-[4-({4-hydroxy-3-[2-(4-nitrophenyl)ethynyl]-5-(propan-2-yl)phenyl}methyl)-3,5-dimethylphenoxy]acetic acid | CHEMBL109279 | JMC496635 Compound 5 | thyromimetic, 5b
TypeSmall organic molecule
Emp. Form.C28H27NO6
Mol. Mass.473.5171
SMILESCC(C)c1cc(Cc2c(C)cc(OCC(O)=O)cc2C)cc(C#Cc2ccc(cc2)[N+]([O-])=O)c1O
Structure
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