Reaction Details |
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Target | Oxysterols receptor LXR-alpha |
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Ligand | BDBM19992 |
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Substrate/Competitor | biotinylated SRC-1 peptide |
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Meas. Tech. | Fluorescence Resonance Energy Transfer (FRET) Ligand Sensing Assay (LiSA) |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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EC50 | 175±n/a nM |
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Comments | 100% efficacy. |
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Citation | Washburn, DG; Hoang, TH; Campobasso, N; Smallwood, A; Parks, DJ; Webb, CL; Frank, KA; Nord, M; Duraiswami, C; Evans, C; Jaye, M; Thompson, SK Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. Bioorg Med Chem Lett19:1097-100 (2009) [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-alpha |
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Name: | Oxysterols receptor LXR-alpha |
Synonyms: | LXRA | Liver X Receptor alpha (LXR-alpha) | Liver X receptor alpha | Liver X receptor alpha (LXRA) | Liver X receptor alpha (NR1H3) | Liver X, LXR alpha | NR1H3 | NR1H3_HUMAN | Nuclear orphan receptor LXR-alpha | Nuclear receptor subfamily 1 group H member 3 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 50403.85 |
Organism: | Homo sapiens (Human) |
Description: | Q13133 |
Residue: | 447 |
Sequence: | MSLWLGAPVPDIPPDSAVELWKPGAQDASSQAQGGSSCILREEARMPHSAGGTAGVGLEA
AEPTALLTRAEPPSEPTEIRPQKRKKGPAPKMLGNELCSVCGDKASGFHYNVLSCEGCKG
FFRRSVIKGAHYICHSGGHCPMDTYMRRKCQECRLRKCRQAGMREECVLSEEQIRLKKLK
RQEEEQAHATSLPPRASSPPQILPQLSPEQLGMIEKLVAAQQQCNRRSFSDRLRVTPWPM
APDPHSREARQQRFAHFTELAIVSVQEIVDFAKQLPGFLQLSREDQIALLKTSAIEVMLL
ETSRRYNPGSESITFLKDFSYNREDFAKAGLQVEFINPIFEFSRAMNELQLNDAEFALLI
AISIFSADRPNVQDQLQVERLQHTYVEALHAYVSIHHPHDRLMFPRMLMKLVSLRTLSSV
HSEQVFALRLQDKKLPPLLSEIWDVHE
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BDBM19992 |
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biotinylated SRC-1 peptide |
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Name: | biotinylated SRC-1 peptide |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 3157.52 |
Organism: | n/a |
Description: | A biotinylated peptide comprises amino acids 675-699 of steroid receptor coactivator 1 (SRC1). |
Residue: | 28 |
Sequence: | CPSSHSSLTERHKILHRLLQEGSPS-CONH2
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