| Reaction Details |
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 | Report a problem with these data |
| Target | Oxysterols receptor LXR-beta [154-461] |
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| Ligand | BDBM26065 |
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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 | 10±n/a nM |
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| EC50 | 990±n/a nM |
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| Comments | 75% 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] |
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| 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 |
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| Type: | Receptor |
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| Mol. Mass.: | 34695.52 |
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| Organism: | Homo sapiens (Human) |
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| 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. |
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| Residue: | 308 |
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| Sequence: | MREQCVLSEEQIRKKKIRKQQQQQESQSQSQSPVGPQGSSSSASGPGASPGGSEAGSQGS
GEGEGVQLTAAQELMIQQLVAAQLQCNKRSFSDQPKVTPWPLGADPQSRDARQQRFAHFT
ELAIISVQEIVDFAKQVPGFLQLGREDQIALLKASTIEIMLLETARRYNHETECITFLKD
FTYSKDDFHRAGLQVEFINPIFEFSRAMRRLGLDDAEYALLIAINIFSADRPNVQEPGRV
EALQQPYVEALLSYTRIKRPQDQLRFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPL
LSEIWDVH
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| BDBM26065 |
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| BDBM19993 |
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| Name | BDBM26065 |
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| Synonyms: | 2-[(2,4-dimethylphenyl)methyl]-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole | 2-benzyl-3-aryl-7-trifluoromethylindazole, 11 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H18F4N2 |
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| Mol. Mass. | 398.396 |
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| SMILES | Cc1ccc(Cn2nc3c(cccc3c2-c2ccc(F)cc2)C(F)(F)F)c(C)c1 |
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| Structure | 
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