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TargetOxysterols receptor LXR-alpha [197-447]
LigandBDBM26065
Substrate/CompetitorBDBM19993
Meas. Tech.LXR Binding Assay and hLXR Reporter Assay
IC50 78±n/a nM
EC50 1810±n/a nM
Citation Wrobel, JSteffan†, RBowen, SMMagolda, RMatelan†, EUnwalla†, RBasso, MClerin, VGardell, SJNambi, PQuinet, EReminick, JIVlasuk, GPWang, SFeingold, IHuselton, CBonn, T Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis J Med Chem51:7161-8 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Oxysterols receptor LXR-alpha [197-447]
Name:Oxysterols receptor LXR-alpha [197-447]
Synonyms:LXRA | Liver X Receptor alpha (LXR-alpha) | NR1H3 | NR1H3_HUMAN | Nuclear orphan receptor LXR-alpha | Nuclear receptor subfamily 1 group H member 3 | Oxysterols receptor LXR-alpha
Type:Receptor
Mol. Mass.:28986.41
Organism:Homo sapiens (Human)
Description:LXR alpha ligand binding domain (amino acid residues 197-447) with an N-terminal biotinylation tag expressed in E.coli, was used for the binding assays.
Residue:251
Sequence:
SSPPQILPQLSPEQLGMIEKLVAAQQQCNRRSFSDRLRVTPWPMAPDPHSREARQQRFAH
FTELAIVSVQEIVDFAKQLPGFLQLSREDQIALLKTSAIEVMLLETSRRYNPGSESITFL
KDFSYNREDFAKAGLQVEFINPIFEFSRAMNELQLNDAEFALLIAISIFSADRPNVQDQL
QVERLQHTYVEALHAYVSIHHPHDRLMFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLP
PLLSEIWDVHE
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BDBM26065
BDBM19993
NameBDBM26065
Synonyms:2-[(2,4-dimethylphenyl)methyl]-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole | 2-benzyl-3-aryl-7-trifluoromethylindazole, 11
TypeSmall organic molecule
Emp. Form.C23H18F4N2
Mol. Mass.398.396
SMILESCc1ccc(Cn2nc3c(cccc3c2-c2ccc(F)cc2)C(F)(F)F)c(C)c1
Structure
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