Reaction Details |
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Target | Oxysterols receptor LXR-alpha |
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Ligand | BDBM20136 |
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Substrate/Competitor | biotinylated SRC-1 peptide |
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Meas. Tech. | Fluorescence-Resonance Energy Transfer Assay |
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pH | 7.2±n/a |
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Temperature | 310.15±n/a K |
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EC50 | 70±n/a nM |
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Comments | Efficacy = 92 % in FRET LXRalpha assay. There was 99% induction of ABCA1 gene activity in human THP-1 cells @ 1uM. |
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Citation | Molteni, V; Li, X; Nabakka, J; Liang, F; Wityak, J; Koder, A; Vargas, L; Romeo, R; Mitro, N; Mak, PA; Seidel, HM; Haslam, JA; Chow, D; Tuntland, T; Spalding, TA; Brock, A; Bradley, M; Castrillo, A; Tontonoz, P; Saez, E N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. J Med Chem50:4255-9 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, 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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BDBM20136 |
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biotinylated SRC-1 peptide |
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Name: | biotinylated SRC-1 peptide |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 2905.78 |
Organism: | n/a |
Description: | n/a |
Residue: | 26 |
Sequence: | CPSSHSSLTE RHKILHRLLQ EGSPSC
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