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Literature summary for 3.4.23.46 extracted from

  • Ghosh, A.K.; Gemma, S.; Tang, J.
    beta-Secretase as a therapeutic target for Alzheimer's disease (2008), Neurotherapeutics, 5, 399-408.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine beta-secretase is a therapeutic target for Alzheimer's disease Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(7S,12Z)-N-[(2S,4R)-2-hydroxy-4-methyl-5-[[(1S)-2-methyl-1-(phenylcarbamoyl)propyl]amino]-1-(2-methylpropyl)-5-oxopentyl]-4-(1-methylethyl)-2,5,9-trioxo-1-oxa-3,6,10-triazacyclohexadec-12-ene-7-carboxamide
-
Homo sapiens
3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-(1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl)leucinamide
-
Homo sapiens
3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-[1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl]leucinamide
-
Homo sapiens
3-[2-amino-6-(phenylcarbonyl)quinazolin-3(4H)-yl]-N-cyclohexyl-N-methylpropanamide
-
Homo sapiens
3-[5-[(1R)-1-amino-1-methyl-2-phenylethyl]-1,3,4-oxadiazol-2-yl]-N-[1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]benzamide
-
Homo sapiens
3-[[(5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)carbonyl]amino]alanyl-L-valyl-N-[(1S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]phenylalaninamide
-
Homo sapiens
4-(2-amino-6-phenoxyquinazolin-3(4H)-yl)-N,4-dicyclohexyl-N-methylbutanamide
-
Homo sapiens
benzyl [2-([1-benzyl-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]amino)-2-oxo-1-[[(1-propylbutyl)sulfonyl]methyl]ethyl]carbamate
-
Homo sapiens
N-(2-methylpropyl)-N2-([17-[(methylsulfonyl)(propyl)amino]-2-oxo-3-azatricyclo[13.3.1.16,10]icosa-1(19),6(20),7,9,15,17-hexaen-4-yl]methyl)-L-norleucinamide
-
Homo sapiens
N-(tert-butoxycarbonyl)valyl-N-[(2S,4R)-2-hydroxy-4-methyl-5-([(1S)-2-methyl-1-[(1-methylethyl)carbamoyl]propyl]amino)-1-(2-methylpropyl)-5-oxopentyl]-L-methioninamide
-
Homo sapiens
N-[(1R,2S)-1-benzyl-2-hydroxy-3-[[3-(trifluoromethyl)benzyl]amino]propyl]-3-(1,1-dioxido-1,2-thiazinan-2-yl)-5-(ethylamino)-2-fluorobenzamide
-
Homo sapiens
N-[(1S)-1-[(butylsulfonyl)methyl]-2-([1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl]amino)-2-oxoethyl]benzamide
-
Homo sapiens
N-[(1Z)-amino(butylamino)methylidene]-2-[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]acetamide
-
Homo sapiens
N-[(2R)-2-amino-1-benzyl-3-fluoropropyl]-2-[[(2-methylcyclopropyl)methyl]amino]-6-[methyl[(1-methylethyl)sulfonyl]amino]pyridine-4-carboxamide
-
Homo sapiens
N-[(2S,4R)-2-hydroxy-4-methyl-5-([(1S)-2-methyl-1-[(2-methylpropyl)carbamoyl]propyl]amino)-1-(2-methylpropyl)-5-oxopentyl]-5-[methyl(methylsulfonyl)amino]-N'-(1-phenylethyl)benzene-1,3-dicarboxamide
-
Homo sapiens
N-[(5R)-5-amino-5-methyl-4,16-dioxo-14-phenyl-3-oxa-15-azatricyclo[15.3.1.17,11]docosa-1(21),7(22),8,10,17,19-hexaen-19-yl]-N-methylmethanesulfonamide
-
Homo sapiens
N-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-iodobenzyl)amino]propyl]-5-methyl-N'-propylbenzene-1,3-dicarboxamide
-
Homo sapiens
N-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]-5-methyl-N'-propylbenzene-1,3-dicarboxamide
-
Homo sapiens
N1-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]-N3-propylbenzene-1,3,5-tricarboxamide
-
Homo sapiens
N1-[1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl]-N3-propylbenzene-1,3,5-tricarboxamide
-
Homo sapiens
N2-[(2R,4S)-5-[[N-[[(2,5-dimethyl-1,3-oxazol-4-yl)methoxy]carbonyl]-3-(methylsulfonyl)-L-alanyl]amino]-4-hydroxy-2,7-dimethyloctanoyl]-N-(2-methylpropyl)-L-valinamide
-
Homo sapiens
N2-[(2R,4S)-5-[[N-[[(3,5-dimethyl-1H-pyrazol-1-yl)methoxy]carbonyl]-3-(methylsulfonyl)-L-alanyl]amino]-4-hydroxy-2,7-dimethyloctanoyl]-N-(2-methylpropyl)-L-valinamide
-
Homo sapiens
OM00-3
-
Homo sapiens
OM99-2
-
Homo sapiens
[3-([1-benzyl-2-hydroxy-3-[(1-methylethyl)amino]propyl]carbamoyl)-5-[(1-phenylethyl)carbamoyl]phenyl]methylsulfamic acid
-
Homo sapiens
[3-([1-benzyl-2-hydroxy-3-[(3-methylbenzyl)amino]propyl]carbamoyl)-5-[[(2,5-dimethyl-1,3-oxazol-4-yl)methyl]carbamoyl]phenyl]methylsulfamic acid
-
Homo sapiens
[3-[(1-[1-hydroxy-2-[(3-methoxybenzyl)amino]ethyl]-3-methylbutyl)carbamoyl]-5-[(1-phenylethyl)carbamoyl]phenyl]methylsulfamic acid
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cell surface beta-secretase is a type 1 transmembrane protein present at the cell surface Homo sapiens 9986
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
beta-amyloid precursor protein APP + H2O
-
Homo sapiens beta-amyloid protein + beta-amyloid precursor protein pre-peptide
-
?

Synonyms

Synonyms Comment Organism
BACE1
-
Homo sapiens
beta-secretase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000012
-
N2-[(2R,4S)-5-[[N-[[(2,5-dimethyl-1,3-oxazol-4-yl)methoxy]carbonyl]-3-(methylsulfonyl)-L-alanyl]amino]-4-hydroxy-2,7-dimethyloctanoyl]-N-(2-methylpropyl)-L-valinamide
-
Homo sapiens
0.0000003
-
OM00-3
-
Homo sapiens
0.0000003
-
N2-[(2R,4S)-5-[[N-[[(3,5-dimethyl-1H-pyrazol-1-yl)methoxy]carbonyl]-3-(methylsulfonyl)-L-alanyl]amino]-4-hydroxy-2,7-dimethyloctanoyl]-N-(2-methylpropyl)-L-valinamide
-
Homo sapiens
0.0000011
-
N-[(2S,4R)-2-hydroxy-4-methyl-5-([(1S)-2-methyl-1-[(2-methylpropyl)carbamoyl]propyl]amino)-1-(2-methylpropyl)-5-oxopentyl]-5-[methyl(methylsulfonyl)amino]-N'-(1-phenylethyl)benzene-1,3-dicarboxamide
-
Homo sapiens
0.0000018
-
OM99-2
-
Homo sapiens
0.000011
-
4-(2-amino-6-phenoxyquinazolin-3(4H)-yl)-N,4-dicyclohexyl-N-methylbutanamide
-
Homo sapiens
0.000014
-
(7S,12Z)-N-[(2S,4R)-2-hydroxy-4-methyl-5-[[(1S)-2-methyl-1-(phenylcarbamoyl)propyl]amino]-1-(2-methylpropyl)-5-oxopentyl]-4-(1-methylethyl)-2,5,9-trioxo-1-oxa-3,6,10-triazacyclohexadec-12-ene-7-carboxamide
-
Homo sapiens
0.000425
-
[3-([1-benzyl-2-hydroxy-3-[(1-methylethyl)amino]propyl]carbamoyl)-5-[(1-phenylethyl)carbamoyl]phenyl]methylsulfamic acid
-
Homo sapiens
0.000552
-
[3-([1-benzyl-2-hydroxy-3-[(3-methylbenzyl)amino]propyl]carbamoyl)-5-[[(2,5-dimethyl-1,3-oxazol-4-yl)methyl]carbamoyl]phenyl]methylsulfamic acid
-
Homo sapiens
0.0009
-
3-[2-amino-6-(phenylcarbonyl)quinazolin-3(4H)-yl]-N-cyclohexyl-N-methylpropanamide
-
Homo sapiens
0.000916
-
[3-[(1-[1-hydroxy-2-[(3-methoxybenzyl)amino]ethyl]-3-methylbutyl)carbamoyl]-5-[(1-phenylethyl)carbamoyl]phenyl]methylsulfamic acid
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000012
-
-
Homo sapiens 3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-[1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl]leucinamide
0.000002
-
-
Homo sapiens N-[(5R)-5-amino-5-methyl-4,16-dioxo-14-phenyl-3-oxa-15-azatricyclo[15.3.1.17,11]docosa-1(21),7(22),8,10,17,19-hexaen-19-yl]-N-methylmethanesulfonamide
0.000002
-
-
Homo sapiens N-[(1S)-1-[(butylsulfonyl)methyl]-2-([1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl]amino)-2-oxoethyl]benzamide
0.0000048
-
-
Homo sapiens 3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-(1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl)leucinamide
0.000005
-
-
Homo sapiens N-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-iodobenzyl)amino]propyl]-5-methyl-N'-propylbenzene-1,3-dicarboxamide
0.000005
-
-
Homo sapiens N-[(1R,2S)-1-benzyl-2-hydroxy-3-[[3-(trifluoromethyl)benzyl]amino]propyl]-3-(1,1-dioxido-1,2-thiazinan-2-yl)-5-(ethylamino)-2-fluorobenzamide
0.0000056
-
-
Homo sapiens 3-[[(5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)carbonyl]amino]alanyl-L-valyl-N-[(1S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]phenylalaninamide
0.000049
-
-
Homo sapiens N-[(2R)-2-amino-1-benzyl-3-fluoropropyl]-2-[[(2-methylcyclopropyl)methyl]amino]-6-[methyl[(1-methylethyl)sulfonyl]amino]pyridine-4-carboxamide
0.000076
-
-
Homo sapiens N-(2-methylpropyl)-N2-([17-[(methylsulfonyl)(propyl)amino]-2-oxo-3-azatricyclo[13.3.1.16,10]icosa-1(19),6(20),7,9,15,17-hexaen-4-yl]methyl)-L-norleucinamide
0.00011
-
-
Homo sapiens N-[(1Z)-amino(butylamino)methylidene]-2-[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]acetamide
0.00012
-
-
Homo sapiens 3-[5-[(1R)-1-amino-1-methyl-2-phenylethyl]-1,3,4-oxadiazol-2-yl]-N-[1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]benzamide