Reaction Details |
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Target | Oxysterols receptor LXR-beta [154-461] |
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Ligand | BDBM20001 |
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Substrate/Competitor | BDBM19993 |
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Meas. Tech. | LXR Binding Assay and hLXR beta 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 | 1.9±0.6 nM |
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EC50 | 33±2.4 nM |
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Comments | Efficacy=85 +/- 13% in transfected hLXRbeta reporter cell line assay. |
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Citation | Hu, B; Collini, M; Unwalla, R; Miller, C; Singhaus, R; Quinet, E; Savio, D; Halpern, A; Basso, M; Keith, J; Clerin, V; Chen, L; Resmini, C; Liu, QY; Feingold, I; Huselton, C; Azam, F; Farnegardh, M; Enroth, C; Bonn, T; Goos-Nilsson, A; Wilhelmsson, A; Nambi, P; Wrobel, J Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. J Med Chem49:6151-4 (2006) [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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BDBM20001 |
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BDBM19993 |
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Name | BDBM20001 |
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 |
Type | Small organic molecule |
Emp. Form. | C32H25F3N2O2 |
Mol. Mass. | 526.5483 |
SMILES | OC(=O)Cc1ccc(CNc2cccc(c2)-c2c(Cc3ccccc3)cnc3c(cccc23)C(F)(F)F)cc1 |
Structure |
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