Reaction Details |
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Target | Beta-secretase 1 |
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Ligand | BDBM16034 |
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Substrate/Competitor | BACE Substrate Peptide |
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Meas. Tech. | In Vitro BACE1 Activity Assay |
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pH | 4.5±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 15±n/a nM |
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Citation | Stachel, SJ; Coburn, CA; Sankaranarayanan, S; Price, EA; Wu, G; Crouthamel, M; Pietrak, BL; Huang, Q; Lineberger, J; Espeseth, AS; Jin, L; Ellis, J; Holloway, MK; Munshi, S; Allison, T; Hazuda, D; Simon, AJ; Graham, SL; Vacca, JP Macrocyclic inhibitors of beta-secretase: functional activity in an animal model. J Med Chem49:6147-50 (2006) [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 |
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Name: | Beta-secretase 1 |
Synonyms: | ASP2 | Asp 2 | Aspartyl protease 2 | BACE | BACE1 | BACE1_HUMAN | Beta-secretase (BACE) | Beta-secretase 1 | Beta-secretase 1 (BACE 1) | Beta-secretase 1 (BACE-1) | Beta-secretase 1 (BACE1) | 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) | beta-Secretase (BACE1) |
Type: | Protein |
Mol. Mass.: | 55755.10 |
Organism: | Homo sapiens (Human) |
Description: | P56817 |
Residue: | 501 |
Sequence: | MAQALPWLLLWMGAGVLPAHGTQHGIRLPLRSGLGGAPLGLRLPRETDEEPEEPGRRGSF
VEMVDNLRGKSGQGYYVEMTVGSPPQTLNILVDTGSSNFAVGAAPHPFLHRYYQRQLSST
YRDLRKGVYVPYTQGKWEGELGTDLVSIPHGPNVTVRANIAAITESDKFFINGSNWEGIL
GLAYAEIARPDDSLEPFFDSLVKQTHVPNLFSLQLCGAGFPLNQSEVLASVGGSMIIGGI
DHSLYTGSLWYTPIRREWYYEVIIVRVEINGQDLKMDCKEYNYDKSIVDSGTTNLRLPKK
VFEAAVKSIKAASSTEKFPDGFWLGEQLVCWQAGTTPWNIFPVISLYLMGEVTNQSFRIT
ILPQQYLRPVEDVATSQDDCYKFAISQSSTGTVMGAVIMEGFYVVFDRARKRIGFAVSAC
HVHDEFRTAAVEGPFVTLDMEDCGYNIPQTDESTLMTIAYVMAAICALFMLPLCLMVCQW
RCLRCLRQQHDDFADDISLLK
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BDBM16034 |
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BACE Substrate Peptide |
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Name: | BACE Substrate Peptide |
Synonyms: | BACE-1 Substrate Peptide |
Type: | Peptide |
Mol. Mass.: | 1557.77 |
Organism: | n/a |
Description: | It is a coumarin (CM)-labeled peptide containing an optimized cleavage sequence NFEV. |
Residue: | 12 |
Sequence: | |