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TargetOxysterols receptor LXR-beta [154-461]
LigandBDBM20001
Substrate/CompetitorBDBM19993
Meas. Tech.LXR Binding Assay and hLXR Reporter Assay
pH7.4±n/a
Temperature277.15±n/a K
IC50 2±n/a nM
EC50 90±n/a nM
Comments70% efficacy.
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-beta [154-461]
Name:Oxysterols receptor LXR-beta [154-461]
Synonyms:LXRB | Liver X Receptor beta (LXR-beta) | NER | NR1H2 | NR1H2_HUMAN | Nuclear orphan receptor LXR-beta | Nuclear receptor NER | Nuclear receptor subfamily 1 group H member 2 | Oxysterols receptor LXR-beta | UNR | Ubiquitously-expressed nuclear receptor
Type:Receptor
Mol. Mass.:34695.52
Organism:Homo sapiens (Human)
Description:LXR beta ligand binding domain (amino acid residues 154-461) with an N-terminal biotinylation tag expressed in E.coli, was used for the binding assays.
Residue:308
Sequence:
MREQCVLSEEQIRKKKIRKQQQQQESQSQSQSPVGPQGSSSSASGPGASPGGSEAGSQGS
GEGEGVQLTAAQELMIQQLVAAQLQCNKRSFSDQPKVTPWPLGADPQSRDARQQRFAHFT
ELAIISVQEIVDFAKQVPGFLQLGREDQIALLKASTIEIMLLETARRYNHETECITFLKD
FTYSKDDFHRAGLQVEFINPIFEFSRAMRRLGLDDAEYALLIAINIFSADRPNVQEPGRV
EALQQPYVEALLSYTRIKRPQDQLRFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPL
LSEIWDVH
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BDBM20001
BDBM19993
NameBDBM20001
Synonyms:2-{4-[({3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid | BMC153321 Compound 4 | JMC517161 Compound 4 | Quinoline 16
TypeSmall organic molecule
Emp. Form.C32H25F3N2O2
Mol. Mass.526.5483
SMILESOC(=O)Cc1ccc(CNc2cccc(c2)-c2c(Cc3ccccc3)cnc3c(cccc23)C(F)(F)F)cc1
Structure
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