Reaction Details |
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Target | Beta-secretase 1 [1-453] |
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Ligand | BDBM29744 |
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Substrate/Competitor | BACE Peptide Substrate |
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Meas. Tech. | Enzyme Inhibition Measurements |
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pH | 4.5±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 1400±n/a nM |
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Citation | Machauer, R; Veenstra, S; Rondeau, JM; Tintelnot-Blomley, M; Betschart, C; Neumann, U; Paganetti, P Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors. Bioorg Med Chem Lett19:1361-5 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Beta-secretase 1 [1-453] |
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Name: | Beta-secretase 1 [1-453] |
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.: | 50193.81 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant human BACE (SwissProt accession number P56817, amino acids 1-453 + a thrombin-cleavable C-kappa tag) was produced in-house using Sf9 insect cells. |
Residue: | 453 |
Sequence: | MAQALPWLLLWMGAGVLPAHGTQHGIRLPLRSGLGGAPLGLRLPRETDEEPEEPGRRGSF
VEMVDNLRGKSGQGYYVEMTVGSPPQTLNILVDTGSSNFAVGAAPHPFLHRYYQRQLSST
YRDLRKGVYVPYTQGKWEGELGTDLVSIPHGPNVTVRANIAAITESDKFFINGSNWEGIL
GLAYAEIARPDDSLEPFFDSLVKQTHVPNLFSLQLCGAGFPLNQSEVLASVGGSMIIGGI
DHSLYTGSLWYTPIRREWYYEVIIVRVEINGQDLKMDCKEYNYDKSIVDSGTTNLRLPKK
VFEAAVKSIKAASSTEKFPDGFWLGEQLVCWQAGTTPWNIFPVISLYLMGEVTNQSFRIT
ILPQQYLRPVEDVATSQDDCYKFAISQSSTGTVMGAVIMEGFYVVFDRARKRIGFAVSAC
HVHDEFRTAAVEGPFVTLDMEDCGYNIPQTDES
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BDBM29744 |
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BACE Peptide Substrate |
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Name: | BACE Peptide Substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 1917.56 |
Organism: | n/a |
Description: | Peptide substrates were obtained from Bachem (Bubendorf, Switzerland). |
Residue: | 17 |
Sequence: | |