Reaction Details |
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Target | Oxysterols receptor LXR-beta [154-461] |
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Ligand | BDBM20000 |
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Substrate/Competitor | BDBM19993 |
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Meas. Tech. | LXR Binding Assay and hLXR Reporter Assay |
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pH | 7.4±n/a |
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Temperature | 277.15±n/a K |
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IC50 | 2±n/a nM |
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EC50 | 90±n/a nM |
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Comments | 63% efficacy. |
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Citation | Wrobel, J; Steffan†, R; Bowen, SM; Magolda, R; Matelan†, E; Unwalla†, R; Basso, M; Clerin, V; Gardell, SJ; Nambi, P; Quinet, E; Reminick, JI; Vlasuk, GP; Wang, S; Feingold, I; Huselton, C; Bonn, 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 |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Oxysterols receptor LXR-beta [154-461] |
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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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BDBM20000 |
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BDBM19993 |
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Name | BDBM20000 |
Synonyms: | 2-(4-{3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}phenyl)acetic acid | CHEMBL214719 | JMC496151 Compound 15 | WAY-254011 |
Type | Small organic molecule |
Emp. Form. | C32H24F3NO3 |
Mol. Mass. | 527.5331 |
SMILES | OC(=O)Cc1ccc(COc2cccc(c2)-c2c(Cc3ccccc3)cnc3c(cccc23)C(F)(F)F)cc1 |
Structure |
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