Reaction Details |
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Target | Beta-secretase 1 |
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Ligand | BDBM17783 |
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Substrate/Competitor | FS1 FRET Substrate |
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Meas. Tech. | BACE-1 Enzymatic Assay |
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pH | 5±n/a |
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Temperature | 295.15±n/a K |
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Ki | 900±n/a nM |
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Citation | Baxter, EW; Conway, KA; Kennis, L; Bischoff, F; Mercken, MH; Winter, HL; Reynolds, CH; Tounge, BA; Luo, C; Scott, MK; Huang, Y; Braeken, M; Pieters, SM; Berthelot, DJ; Masure, S; Bruinzeel, WD; Jordan, AD; Parker, MH; Boyd, RE; Qu, J; Alexander, RS; Brenneman, DE; Reitz, AB 2-Amino-3,4-dihydroquinazolines as Inhibitors of BACE-1 (beta-Site APP Cleaving Enzyme): Use of Structure Based Design to Convert a Micromolar Hit into a Nanomolar Lead. J Med Chem50:4261-4 (2007) [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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BDBM17783 |
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FS1 FRET Substrate |
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Name: | FS1 FRET Substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 2858.98 |
Organism: | n/a |
Description: | n/a |
Residue: | 24 |
Sequence: | H-RE(EDANS)EVNLDAEFK(DABCYL)R-OH
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