Reaction Details Report a problem with these data
Target
Oxysterols receptor LXR-beta
Ligand
BDBM27174
Substrate
biotinylated SRC-1 peptide
Meas. Tech.
Fluorescence Resonance Energy Transfer (FRET) Ligand Sensing Assay (LiSA)
pH
7.5±n/a
Temperature
295.15±n/a K
EC50
4±n/a nM
Comments
105% efficacy.
Citation
 Washburn, DG; Hoang, TH; Campobasso, N; Smallwood, A; Parks, DJ; Webb, CL; Frank, KA; Nord, M; Duraiswami, C; Evans, C; Jaye, M; Thompson, SK Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. Bioorg Med Chem Lett 19:1097-100 (2009) [PubMed]  Article 
Target
Name:
Oxysterols receptor LXR-beta
Synonyms:
LXRB | Liver X receptor beta (NR1H2) | Liver X, LXR beta | NER | NR1H2 | NR1H2_HUMAN | Nuclear receptor NER | UNR | Ubiquitously-expressed nuclear receptor
Type:
Enzyme Catalytic Domain
Mol. Mass.:
50978.79
Organism:
Homo sapiens (Human)
Description:
P55055
Residue:
460
Sequence:
MSSPTTSSLDTPLPGNGPPQPGAPSSSPTVKEEGPEPWPGGPDPDVPGTDEASSACSTDWVIPDPEEEPERKRKKGPAPKMLGHELCRVCGDKASGFHYNVLSCEGCKGFFRRSVVRGGARRYACRGGGTCQMDAFMRRKCQQCRLRKCKEAGMREQCVLSEEQIRKKKIRKQQQESQSQSQSPVGPQGSSSSASGPGASPGGSEAGSQGSGEGEGVQLTAAQELMIQQLVAAQLQCNKRSFSDQPKVTPWPLGADPQSRDARQQRFAHFTELAIISVQEIVDFAKQVPGFLQLGREDQIALLKASTIEIMLLETARRYNHETECITFLKDFTYSKDDFHRAGLQVEFINPIFEFSRAMRRLGLDDAEYALLIAINIFSADRPNVQEPGRVEALQQPYVEALLSYTRIKRPQDQLRFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVHE
  
Inhibitor
Name:
BDBM27174
Synonyms:
1H-indol-1-yl tertiary amine, 18 | 2-{4-[3-({[2-chloro-3-(trifluoromethyl)phenyl]methyl}(2,2-diphenylethyl)amino)propoxy]-1H-indol-1-yl}acetic acid
Type:
Small organic molecule
Emp. Form.:
C35H32ClF3N2O3
Mol. Mass.:
621.088
SMILES:
OC(=O)Cn1ccc2c(OCCCN(CC(c3ccccc3)c3ccccc3)Cc3cccc(c3Cl)C(F)(F)F)cccc12
Structure:
Search PDB for entries with ligand similarity:
Substrate
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:
CPSSHSSLTERHKILHRLLQEGSPSCNH