Target
Oxysterols receptor LXR-alpha
Ligand
BDBM50300578
Substrate
n/a
Meas. Tech.
ChEMBL_588776 (CHEMBL1054462)
EC50
365±n/a nM
Citation
 Marino, JPKallander, LSMa, COh, HJLee, DGaitanopoulos, DEKrawiec, JAParks, DJWebb, CLZiegler, KJaye, MThompson, SK The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. Bioorg Med Chem Lett 19:5617-21 (2009) [PubMed]  Article 
Target
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:
MSLWLGAPVPDIPPDSAVELWKPGAQDASSQAQGGSSCILREEARMPHSAGGTAGVGLEAAEPTALLTRAEPPSEPTEIRPQKRKKGPAPKMLGNELCSVCGDKASGFHYNVLSCEGCKGFFRRSVIKGAHYICHSGGHCPMDTYMRRKCQECRLRKCRQAGMREECVLSEEQIRLKKLKRQEEEQAHATSLPPRASSPPQILPQLSPEQLGMIEKLVAAQQQCNRRSFSDRLRVTPWPMAPDPHSREARQQRFAHFTELAIVSVQEIVDFAKQLPGFLQLSREDQIALLKTSAIEVMLLETSRRYNPGSESITFLKDFSYNREDFAKAGLQVEFINPIFEFSRAMNELQLNDAEFALLIAISIFSADRPNVQDQLQVERLQHTYVEALHAYVSIHHPHDRLMFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVHE
  
Inhibitor
Name:
BDBM50300578
Synonyms:
(S)-2-(3-(4-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)butan-2-yloxy)phenyl)acetic acid | CHEMBL573591
Type:
Small organic molecule
Emp. Form.:
C34H33ClF3NO3
Mol. Mass.:
596.079
SMILES:
C[C@@H](CCN(CC(c1ccccc1)c1ccccc1)Cc1cccc(c1Cl)C(F)(F)F)Oc1cccc(CC(O)=O)c1 |r|
Structure:
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