Reaction Details |
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Target | Beta-secretase 1 [22-454] |
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Ligand | BDBM16288 |
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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 | 11300±1500 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 Chem49:839-42 (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 1 [22-454] |
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Name: | Beta-secretase 1 [22-454] |
Synonyms: | ASP2 | Asp 2 | Aspartyl protease 2 | BACE | BACE1 | BACE1_HUMAN | Beta-site APP cleaving enzyme 1 | Beta-site amyloid precursor protein cleaving enzyme 1 | KIAA1149 | Memapsin-2 | Membrane-associated aspartic protease 2 | beta-Secretase (BACE-1) |
Type: | Enzyme |
Mol. Mass.: | 48079.72 |
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: | 433 |
Sequence: | TQHGIRLPLRSGLGGAPLGLRLPRETDEEPEEPGRRGSFVEMVDNLRGKSGQGYYVEMTV
GSPPQTLNILVDTGSSNFAVGAAPHPFLHRYYQRQLSSTYRDLRKGVYVPYTQGKWEGEL
GTDLVSIPHGPNVTVRANIAAITESDKFFINGSNWEGILGLAYAEIARPDDSLEPFFDSL
VKQTHVPNLFSLQLCGAGFPLNQSEVLASVGGSMIIGGIDHSLYTGSLWYTPIRREWYYE
VIIVRVEINGQDLKMDCKEYNYDKSIVDSGTTNLRLPKKVFEAAVKSIKAASSTEKFPDG
FWLGEQLVCWQAGTTPWNIFPVISLYLMGEVTNQSFRITILPQQYLRPVEDVATSQDDCY
KFAISQSSTGTVMGAVIMEGFYVVFDRARKRIGFAVSACHVHDEFRTAAVEGPFVTLDME
DCGYNIPQTDEST
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BDBM16288 |
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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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