Reaction Details |
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Target | Oxysterols receptor LXR-alpha |
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Ligand | BDBM19992 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_588776 (CHEMBL1054462) |
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EC50 | 200±n/a nM |
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Citation | Marino, JP; Kallander, LS; Ma, C; Oh, HJ; Lee, D; Gaitanopoulos, DE; Krawiec, JA; Parks, DJ; Webb, CL; Ziegler, K; Jaye, M; Thompson, SK The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. Bioorg Med Chem Lett19:5617-21 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, 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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n/a |
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Name | BDBM19992 |
Synonyms: | 2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-[2,2-di(phenyl)ethyl]amino]propoxy]phenyl]acetic acid | 2-{3-[3-({[2-chloro-3-(trifluoromethyl)phenyl]methyl}(2,2-diphenylethyl)amino)propoxy]phenyl}acetic acid | CHEMBL59030 | GSK-3965 | GW3965 | US10543183, Compound GW3965 | US10669296, Compound GW3965 | US10945978, Compound 2 |
Type | Small organic molecule |
Emp. Form. | C33H31ClF3NO3 |
Mol. Mass. | 582.052 |
SMILES | OC(=O)Cc1cccc(OCCCN(CC(c2ccccc2)c2ccccc2)Cc2cccc(c2Cl)C(F)(F)F)c1 |
Structure |
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