Ki Summary new BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
Targetbeta-Secretase (BACE-1)
LigandBDBM16292
Substrate/Competitorfluorescent substrate FS-2
Meas. Tech.Enzyme Inhibition Assay
pH4.5±n/a
Temperature295.15±n/a K
Ki 26±5 nM
Citation Yang WLu WLu YZhong MSun JThomas AEWilkinson JMFucini RVLam MRandal MShi XPJacobs JWMcDowell RSGordon EMBallinger MD Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1. J Med Chem 49:839-42 (2006) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
beta-Secretase (BACE-1)
Name:beta-Secretase (BACE-1)
Synonyms:ASP2 | Asp 2 | Aspartyl protease 2 | Beta-site APP cleaving enzyme 1 | Beta-site amyloid precursor protein cleaving enzyme 1 | Memapsin-2 | Membrane-associated aspartic protease 2
Type:Enzyme
Mol. Mass.:43208.90
Organism:Homo sapiens (Human)
Description:C-terminally 6XHis-tagged human proBACE-1 (residues 22-454, numbering starting from the N-terminal methionine) was expressed in Hi5 cells using the baculovirus expression vector pFastbac1 (Invitrogen) and purified on Ni-NTA fast flow resin (Qiagen).
Residue:388
Sequence:
SFVEMVDNLRGKSGQGYYVEMTVGSPPQTLNILVDTGSSNFAVGAAPHPFLHRYYQRQLS
STYRDLRKGVYVPYTQGKWEGELGTDLVSIPHGPNVTVRANIAAITESDKFFINGSNWEG
ILGLAYAEIARPDDSLEPFFDSLVKQTHVPNLFSLQLCGAGFPLNQSEVLASVGGSMIIG
GIDHSLYTGSLWYTPIRREWYYEVIIVRVEINGQDLKMDCKEYNYDKSIVDSGTTNLRLP
KKVFEAAVKSIKAASSTEKFPDGFWLGEQLVCWQAGTTPWNIFPVISLYLMGEVTNQSFR
ITILPQQYLRPVEDVATSQDDCYKFAISQSSTGTVMGAVIMEGFYVVFDRARKRIGFAVS
ACHVHDEFRTAAVEGPFVTLDMEDCGYN
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM16292
fluorescent substrate FS-2
Name:fluorescent substrate FS-2
Synonyms:n/a
Type:Peptide
Mol. Mass.:4309.84
Organism:n/a
Description:n/a
Residue:42
Sequence:
MOCAc-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(DNP)-Arg-Arg-C
OOH