Target
Oxysterols receptor LXR-alpha
Ligand
BDBM19992
Substrate
n/a
Meas. Tech.
ChEMBL_566734 (CHEMBL961726)
EC50
310±n/a nM
Citation
 Swahn, BMMacsari, IViklund, JOhberg, LSjödin, JNeelissen, JLindquist, J Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides. Bioorg Med Chem Lett 19:2009-12 (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:
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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