Reaction Details |
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Target | Oxysterols receptor LXR-alpha |
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Ligand | BDBM28141 |
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Substrate/Competitor | BDBM19993 |
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Meas. Tech. | Radioligand Binding Assay and Luciferase Transcriptional Reporter Gene Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 49±n/a nM |
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EC50 | 1350±n/a nM |
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Citation | Ratni, H; Blum-Kaelin, D; Dehmlow, H; Hartman, P; Jablonski, P; Masciadri, R; Maugeais, C; Patiny-Adam, A; Panday, N; Wright, M Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator. Bioorg Med Chem Lett19:1654-7 (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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BDBM28141 |
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BDBM19993 |
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Name | BDBM28141 |
Synonyms: | methyl (2S)-2-[(2R)-7-chloro-1H,2H,3H,4H-cyclopenta[b]indol-2-yl]-2-fluoro-2-[(3-fluorobenzene)sulfonyl]acetate | tetrahydro-cyclopenta[b]indole, (+/-)21 |
Type | Small organic molecule |
Emp. Form. | C20H16ClF2NO4S |
Mol. Mass. | 439.86 |
SMILES | [H][C@@]1(Cc2[nH]c3ccc(Cl)cc3c2C1)[C@@](F)(C(=O)OC)S(=O)(=O)c1cccc(F)c1 |r| |
Structure |
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