Reaction Details |
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Target | beta-Secretase (BACE-1) |
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Ligand | BDBM16292 |
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Substrate/Competitor | fluorescent substrate FS-2 |
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Meas. Tech. | Enzyme Inhibition Assay |
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pH | 4.5±n/a |
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Temperature | 295.15±n/a K |
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Ki | 26±5 nM |
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Citation | Yang W; Lu W; Lu Y; Zhong M; Sun J; Thomas AE; Wilkinson JM; Fucini RV; Lam M; Randal M; Shi XP; Jacobs JW; McDowell RS; Gordon EM; Ballinger MD Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1. J Med Chem 49:839-42 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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beta-Secretase (BACE-1) |
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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
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BDBM16292 |
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fluorescent substrate FS-2 |
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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
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