Target
Oxysterols receptor LXR-beta
Ligand
BDBM27271
Substrate
biotinylated SRC-1 peptide
Meas. Tech.
HTRF Cofactor Peptide Recruitment Assay
pH
7.5±n/a
Temperature
295.15±n/a K
EC50
1510±n/a nM
Citation
 Kher, SLake, KSircar, IPannala, MBakir, FZapf, JXu, KZhang, SHLiu, JMorera, LSakurai, NJack, RCheng, JF 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. Bioorg Med Chem Lett 17:4442-6 (2007) [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:
BDBM27271
Synonyms:
Boc-indole derivative, 29 | tert-butyl 2-(4-{2-[(2-methylpropyl)carbamoyl]ethyl}phenyl)-1H-indole-1-carboxylate
Type:
Small organic molecule
Emp. Form.:
C26H32N2O3
Mol. Mass.:
420.5439
SMILES:
CC(C)CNC(=O)CCc1ccc(cc1)-c1cc2ccccc2n1C(=O)OC(C)(C)C
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