Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetOxysterols receptor LXR-alpha
LigandBDBM28141
Substrate/CompetitorBDBM19993
Meas. Tech.Radioligand Binding Assay and Luciferase Transcriptional Reporter Gene Assay
pH7.4±n/a
Temperature295.15±n/a K
IC50 49±n/a nM
EC50 1350±n/a nM
Citation Ratni, HBlum-Kaelin, DDehmlow, HHartman, PJablonski, PMasciadri, RMaugeais, CPatiny-Adam, APanday, NWright, M Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator. Bioorg Med Chem Lett19:1654-7 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Oxysterols receptor LXR-alpha
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM28141
BDBM19993
NameBDBM28141
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
TypeSmall 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
Search PDB for entries with ligand similarity:Similarity to this molecule at least: