Target
Oxysterols receptor LXR-alpha
Ligand
BDBM50258172
Substrate
n/a
Meas. Tech.
ChEMBL_566455 (CHEMBL958322)
EC50
3500±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:
BDBM50258172
Synonyms:
CHEMBL521811 | methyl 3-(4-(N-(3-chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenyl)-N-methylsulfamoyl)phenyl)propanoate
Type:
Small organic molecule
Emp. Form.:
C21H22ClF3N2O6S
Mol. Mass.:
522.922
SMILES:
COC(=O)CCc1ccc(cc1)S(=O)(=O)N(C)c1ccc(NC(=O)C(C)(O)C(F)(F)F)c(Cl)c1
Structure:
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