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Target
Beta-secretase 2
Ligand
BDBM26777
Substrate
Fluorescent Substrate
Meas. Tech.
Enzyme Inhibition Assay
IC50
600±n/a nM
Citation
Beswick, P; Charrier, N; Clarke, B; Demont, E; Dingwall, C; Dunsdon, R; Faller, A; Gleave, R; Hawkins, J; Hussain, I; Johnson, CN; MacPherson, D; Maile, G; Matico, R; Milner, P; Mosley, J; Naylor, A; O'Brien, A; Redshaw, S; Riddell, D; Rowland, P; Skidmore, J; Soleil, V; Smith, KJ; Stanway, S; Stemp, G; Stuart, A; Sweitzer, S; Theobald, P; Vesey, D; Walter, DS; Ward, J; Wayne, G BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells. Bioorg Med Chem Lett 18:1022-6 (2008) [PubMed] Article
More Info.:
Target
Name:
Beta-secretase 2
Synonyms:
AEPLC | ALP56 | ASP1 | ASP21 | Asp 1 | Aspartic-like protease 56 kDa | Aspartyl protease 1 | BACE2 | BACE2_HUMAN | Beta secretase 2 | Beta-secretase (BACE) | Beta-secretase 2 | Beta-secretase 2 (BACE-2) | Beta-secretase 2 precursor | Beta-site APP-cleaving enzyme 2 | Down region aspartic protease | Memapsin-1 | Membrane-associated aspartic protease 1 | beta-Secretase (BACE-2)
Type:
Protein
Mol. Mass.:
56171.20
Organism:
Homo sapiens (Human)
Description:
Q9Y5Z0
Residue:
518
Sequence:
MGALARALLLPLLAQWLLRAAPELAPAPFTLPLRVAAATNRVVAPTPGPGTPAERHADGLALALEPALASPAGAANFLAMVDNLQGDSGRGYYLEMLIGTPPQKLQILVDTGSSNFAVAGTPHSYIDTYFDTERSSTYRSKGFDVTVKYTQGSWTGFVGEDLVTIPKGFNTSFLVNIATIFESENFFLPGIKWNGILGLAYATLAKPSSSLETFFDSLVTQANIPNVFSMQMCGAGLPVAGSGTNGGSLVLGGIEPSLYKGDIWYTPIKEEWYYQIEILKLEIGGQSLNLDCREYNADKAIVDSGTTLLRLPQKVFDAVVEAVARASLIPEFSDGFWTGSQLACWTNSETPWSYFPKISIYLRDENSSRSFRITILPQLYIQPMMGAGLNYECYRFGISPSTNALVIGATVMEGFYVIFDRAQKRVGFAASPCAEIAGAAVSEISGPFSTEDVASNCVPAQSLSEPILWIVSYALMSVCGAILLVLIVLLLLPFRCQRRPRDPEVVNDESSLVRHRWK
Inhibitor
Name:
BDBM26777
Synonyms:
3-(1,1-dioxo-1,2-thiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-({[3-(trifluoromethoxy)phenyl]methyl}amino)butan-2-yl]benzamide | hydroxy ethylamine (HEA), 11
Type:
Small organic molecule
Emp. Form.:
C31H37F3N4O5S
Mol. Mass.:
634.709
SMILES:
CCNc1cc(cc(c1)C(=O)N[C@@H](Cc1ccccc1)[C@H](O)CNCc1cccc(OC(F)(F)F)c1)N1CCCCS1(=O)=O |r|
Substrate
Name:
Fluorescent Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2030.30
Organism:
n/a
Description:
n/a
Residue:
18
Sequence:
FAMSEVNLDAEFKTAMRA