Reaction Details  Report a problem with these data
Target
Oxysterols receptor LXR-beta
Ligand
BDBM20163
Substrate
biotinylated SRC-1 peptide
Meas. Tech.
Cell-Free Ligand Sensing Assay (LiSA)-LXRbeta-SRC1 Assay
pH
7.5±n/a
Temperature
295.15±n/a K
EC50
575±150 nM
Citation
 Jaye, MC; Krawiec, JA; Campobasso, N; Smallwood, A; Qiu, C; Lu, Q; Kerrigan, JJ; De Los Frailes Alvaro, M; Laffitte, B; Liu, WS; Marino, JP; Meyer, CR; Nichols, JA; Parks, DJ; Perez, P; Sarov-Blat, L; Seepersaud, SD; Steplewski, KM; Thompson, SK; Wang, P; Watson, MA; Webb, CL; Haigh, D; Caravella, JA; Macphee, CH; Willson, TM; Collins, JL Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. J Med Chem 48:5419-22 (2005) [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:
BDBM20163
Synonyms:
3-[(4-chlorophenyl)amino]-1-ethyl-4-phenyl-2,5-dihydro-1H-pyrrole-2,5-dione | GSK3987 Analogue | Substituted Maleimide, 11
Type:
Small organic molecule
Emp. Form.:
C18H15ClN2O2
Mol. Mass.:
326.777
SMILES:
CCN1C(=O)C(Nc2ccc(Cl)cc2)=C(C1=O)c1ccccc1 |c:14|
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