Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetOxysterols receptor LXR-alpha
LigandBDBM20171
Substrate/Competitorbiotinylated SRC-1 peptide
Meas. Tech.Cell-Free Ligand Sensing Assay (LiSA)-LXRalpha-SRC1 Assay
pH7.5±n/a
Temperature295.15±n/a K
EC50 85±20 nM
CommentsThe relative efficacy (RE) compared to 24(S),25-epoxycholesterol is 0.7 in LXRalpha-SRC1 assay. The EC50=650 +/- 300 nM for LXRalpha-GAL4 gene expression with RE=0.3.
Citation Collins, JL; Fivush, AM; Watson, MA; Galardi, CM; Lewis, MC; Moore, LB; Parks, DJ; Wilson, JG; Tippin, TK; Binz, JG; Plunket, KD; Morgan, DG; Beaudet, EJ; Whitney, KD; Kliewer, SA; Willson, TM Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem45:1963-6 (2002) [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:
BDBM20171
biotinylated SRC-1 peptide
Name:biotinylated SRC-1 peptide
Synonyms:n/a
Type:Peptide
Mol. Mass.:3157.52
Organism:n/a
Description:A biotinylated peptide comprises amino acids 675-699 of steroid receptor coactivator 1 (SRC1).
Residue:28
Sequence:
CPSSHSSLTERHKILHRLLQEGSPS-CONH2