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3.4.23.46: memapsin 2

This is an abbreviated version!
For detailed information about memapsin 2, go to the full flat file.

Word Map on EC 3.4.23.46

Reaction

broad endopeptidase specificity. Cleaves Glu-Val-Asn-Leu-/-Asp-Ala-Glu-Phe in the Swedish variant of Alzheimer's amyloid precursor protein =

Synonyms

alpha-secretase, amyloid precursor protein secretase, APP secretase, Asec-1A, aspartic protease BACE, aspartic protease BACE1, Aspartic proteinase, aspartic proteinase BACE1, BACE, BACE 1, BACE I, BACE-1, BACE-2, BACE1, BACE1/beta-secretase, BACE2, beta protein amyloidogenase, beta secretase, beta-amyloid cleaving enzyme, beta-amyloid cleaving enzyme 1, beta-amyloid cleaving enzyme-1, beta-amyloid precursor protein cleavage enzyme 1, beta-amyloid precursor protein cleaving enzyme, beta-amyloid protein precursor secretase, beta-amyloid-cleaving enzyme, beta-amyloid-converting enzyme-1, beta-APP cleaving enzyme 1, beta-secretase, beta-secretase enzyme 1, beta-secretase-1, beta-site Alzheimer's amyloid precursor protein cleaving enzyme 1 (BACE1), beta-site amyloid cleaving enzyme, beta-site amyloid precursor protein cleavage enzyme, beta-site amyloid precursor protein cleaving enzyme, beta-site amyloid precursor protein cleaving enzyme 1, beta-site amyloid precursor protein cleaving enzyme-1, beta-site amyloid precursor protein enzyme 1, beta-site amyloid precursor protein-cleaving enzyme, beta-site amyloid precursor protein-cleaving enzyme 1, beta-site APP (amyloid precursor protein) cleaving enzyme, beta-site APP cleaving enzyme, beta-site APP cleaving enzyme 1, beta-site APP cleaving enzyme-1, beta-site APP-cleaving enzyme 1, D-aspartyl-beta-amyloid secretase, gamma-secretase, memapsin 1, memapsin 2, memapsin2, membrane-bound aspartic protease, NACE1, presenilin 1, presenilin-1, presenilin-2, protease Asp2, proteinase BACE1

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.23 Aspartic endopeptidases
                3.4.23.46 memapsin 2

Inhibitors

Inhibitors on EC 3.4.23.46 - memapsin 2

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(+)-byakangelicin
-
-
(+)-byakangelicol
-
-
(+)-canadaline
41.02% inhibition at 0.005 mM
(+)-corynoline
21.91% inhibition at 0.005 mM
(+)-N-((4S,4aS,6S,8aR)-10-amino-4,4a,5,6,7,8-hexahydro-1H,3H-4,8a-(epithiomethenoazeno)isochromen-6-yl)-3-chlorobenzamide
-
(+)-oxypeucedanin
-
-
(+/-)-corycavidine
26.87% inhibition at 0.005 mM
(-)-corycavamine
34.4% inhibition at 0.005 mM
(-)-gallocatechin gallate
-
less potent inhibitor
(-)-isocorypalmine
26.68% inhibition at 0.005 mM
(-)-scoulerine
24.34% inhibition at 0.005 mM
(13S)-15-amino-10,13-dicyclohexyl-19-fluoro-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(13S)-15-amino-10,13-dicyclohexyl-19-methoxy-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(13S)-15-amino-10,13-dicyclohexyl-2-oxa-10,14,16,19-tetraazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(14S)-16-amino-10,14-dicyclohexyl-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
potent inhibitor
(14S)-16-amino-10-cyclohexyl-14-(propan-2-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(14S)-16-amino-14-(propan-2-yl)-10-(tetrahydro-2H-pyran-4-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(14S)-16-amino-14-cyclohexyl-10-(tetrahydro-2H-pyran-4-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(15R)-17-amino-11,15-dicyclohexyl-2-oxa-11,16,18-triazatetracyclo[14.5.3.1(3,7).0(19,23)]pentacosa-1(21),3(25),4,6,17,19,22-heptaen-12-one
-
-
(15S)-17-amino-11,15-dicyclohexyl-2-oxa-11,16,18-triazatetracyclo[14.5.3.1(3,7).0(19,23)]pentacosa-1(21),3(25),4,6,17,19,22-heptaen-12-one
-
-
(1R,3S)-3-[(1S)-1-(acetylamino)-2-methylpropyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[(1S)-1-(acetylamino)-3-methylbutyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
11% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)butyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
15% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)ethyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
8% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)propyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
17% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)-3-methylbutyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
42% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)butyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
80% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)cyclopentyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[1-(acetylamino)ethyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
14% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)propyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
24% inhibition at 0.01 mM
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopiperidin-1-yl)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopyrrolidin-1-yl)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(propanoylamino)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-[methyl(propanoyl)amino]propan-2-yl]cyclohexanecarboxamide
-
-
(1R,4S,5R,7R)-3,4-dibenzyl-2-oxo-N-(prop-2-yn-1-yl)-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxamide
32% inhibition at 0.01 mM
(1R,4S,5R,7R)-3,4-dibenzyl-7-(piperidin-1-ylcarbonyl)-6,8-dioxa-3-azabicyclo[3.2.1]octan-2-one
46% inhibition at 0.01 mM
(1R,5R,7R)-3-benzyl-7-(piperidin-1-ylcarbonyl)-6,8-dioxa-3-azabicyclo[3.2.1]octan-2-one
10% inhibition at 0.01 mM
(1R,5R,7R)-3-benzyl-N-[(2S)-1-hydroxy-4-methylpentan-2-yl]-2-oxo-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxamide
8% inhibition at 0.01 mM
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[(1-benzylpiperidin-4-yl)amino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
-
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl]-5-[methyl(methylsulfonyl)-amino]-N'-[(R)-1-(4-fluorophenyl)ethyl]isophthalamide
-
-
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
dual inhibitor of both beta-secretase and acetylcholinesterase, good inhibitory effects on amyloid beta production of amyloid precursor protein transfected HEK293 cells
(1S,2R)-N-{1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl}-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
dual inhibitor of both beta-secretase and acetylcholinesterase. Intracerebroventricular injection of into amyloid precursor protein transgenic mice causes a 29% reduction of amyloid beta1-40 production
(2R,4S)-N-butyl-4-hydroxy-2-methyl-4-[(2S,5S,7R)-1,2,7-trimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]butanamide
56fold selectivity for beta-secretase over cathepsin D
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,15-dioxo-1,4-diazacyclopentadecan-5-yl]-4-hydroxy-2-methylbutanamide
-
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]-4-hydroxy-2-methylbutanamide
-
(2R,4S,5S)-N-benzyl-4-hydroxy-2,7-dimethyl-5-[(N-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-seryl)amino]octanamide
-
16.45% inhibition at 0.01 mg/ml
(2R,4S,5S)-N-benzyl-4-hydroxy-5-([N-[(4-methoxyphenyl)acetyl]-L-seryl]amino)-2,7-dimethyloctanamide
-
25.09% inhibition at 0.01 mg/ml
(2S)-2-((3R)-3-acetamido-3-isobutyl-2-oxo-1-pyrrolidinyl)-N-((1S,2R)-1-(3,5-difluorobenzyl)-2-hydroxy-2-(1,2,3,4-tetrahydro-3-isoquinolinyl)ethyl)-4-phenylbutanamide
crystallization data, EC50 value for HEK293 cells 10 nM
(2S)-2-((S)-3-acetamido-3-((R)-sec-butyl)-2-oxopyrrolidin-1-yl)-N-((1S,2S)-3-(3,5-difluorophenyl)-1-hydroxy-1-((2R)-5-(propylsulfonyl)pyrrolidin-2-yl)propan-2-yl)-4-phenylbutanamide
(2S,5S,8S,11S,14S)-14-amino-5-benzyl-8-(cyclohexylmethyl)-16-(5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)-2-hydroxy-11-(1-methylethyl)-4,7,10,13,16-pentaoxo-N-[3-(2H-tetrazol-5-yl)phenyl]-3,6,9,12-tetraazahexadecan-1-amide
i.e. KMI-574, 100% and 97% inhibition at 2 microM and 0.2 microM, respectively, 84% inhibition of beta-secretase BACE1 in cultured cell-based assay at 100 microM
(3aR,6aS)-N-[(2R)-1-([(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]amino)-3-(methylsulfonyl)-1-oxopropan-2-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aR,6aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aR,6aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-5,11,14-trioxo-13-(propan-2-yl)-2-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aR,7aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,5,6,7a-tetrahydro-4H-pyrano[3,2-d][1,2]oxazole-3-carboxamide
-
(3aS,6aR)-N-[(2R)-1-([(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]amino)-3-(methylsulfonyl)-1-oxopropan-2-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aS,6aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aS,6aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-5,11,14-trioxo-13-(propan-2-yl)-2-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aS,7aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,5,6,7a-tetrahydro-4H-pyrano[3,2-d][1,2]oxazole-3-carboxamide
-
(3S,14R,16S)-16-[(1R)-1-hydroxy-2-([3-(1-methylethyl)benzyl]amino)ethyl]-3,4,14-trimethyl-1,4-diazacyclohexadecane-2,5-dione
(3S,14R,16S)-16-[(1S)-2-[[(1R)-3,3-dimethyl-7-(1-methylethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]amino]-1-hydroxyethyl]-3,4,14-trimethyl-1,4-diazacyclohexadecane-2,5-dione
(3S,5R)-3-(4-amino-3-fluoro-5-[[(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl]oxy]benzyl)-5-[(3-tert-butylbenzyl)amino]-4-hydroxytetrahydro-2H-thiopyranium-1-olate
highly potent, selective inhibitors with improved cellular activity. Sufficient central nervous system exposure can be achieved with a single oral dose of 60 micromol/kg to effect significant reduction in brain amyloid beta in APP51/16 transgenic mice
(4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(fluoromethyl)-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-amine
upon oral administration, inhibitor exhibits robust brain availability and is efficacious in lowering central amyloid beta levels in mouse and dog. Chronic treatment in aged PS1/APP mice effects a decrease in the number and size of amyloid-beta-derived plaques. Evaluation of the inhibitor in a 2-week exploratory toxicology study exhibits no accumulation of autofluorescent material in retinal pigment epithelium or histology findings in the eye
(4aS,4'S,10aR)-8-(2-fluoropyridin-3-yl)-4a-methyl-3,4,4a,10a-tetrahydro-2H,5'H-spiro[pyrano[3,2-b]chromene-10,4'-thiazol]-2'-amine
compound demonstrates a 69% reduction in rat cerebrospinal fluid amyloid beta1?40 at 60 mg/kg
(4S)-4-(2,4-difluorophenyl)-6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-(2-oxopyrrolidin-1-yl)-11,16-dioxa-3-azatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-(methoxymethyl)-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]ethyl]amino)ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([2-[3-(propan-2-yl)phenyl]propan-2-yl]amino)ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-methyl-11-oxa-3,16,18-triazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2,2,2-trifluoroethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2-fluoroethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2-methoxyethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)cyclobutyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)cyclopentyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[2,4-difluoro-5-(pyrimidin-5-yl)phenyl]-6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine
-
(4S,6R)-4-(2,4-difluorophenyl)-4-methyl-6-(pyrimidin-5-yl)-5,6-dihydro-4H-1,3-thiazin-2-amine
-
(5S)-2-amino-5-(2',4'-difluorobiphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
5fold selectivity for BACE2 over BACE1, 27fold selectivity for BACE2 over cathepsin D
(5S)-2-amino-5-[3-fluoro-5-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
(6R)-2,6-anhydro-5-O-[(E)-2-(4-hydroxyphenyl)ethenyl]-6-[2-[(2R)-2-hydroxypropyl]-7-methoxy-5-methyl-4-oxo-4H-chromen-8-yl]-L-glucitol
-
inhibitor isolated from Aloe vera and Aloe nobilis. Inhibition of amyloid beta1-42 production by 7.4% in B103 neuroblastoma cells at 30 ppm
(6R)-2,6-anhydro-6-[7-methoxy-5-methyl-4-oxo-2-[(1E)-prop-1-en-1-yl]-4H-chromen-8-yl]-L-glucitol
-
inhibitor isolated from Aloe vera and Aloe nobilis. Inhibition of amyloid beta1-42 production by 12.3% in B103 neuroblastoma cells at 30 ppm
(6R)-2-amino-3,6-dimethyl-6-(2-phenylethyl)-5,6-dihydropyrimidin-4(3H)-one
-
(6R)-2-amino-6-[2-(3'-methoxybiphenyl-4-yl)ethyl]-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
-
(6R)-2-amino-6-[2-(biphenyl-4-yl)ethyl]-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
-
(6S)-2-amino-6-(3'-methoxybiphenyl-3-yl)-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
-
(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
-
-
(R)-3-(2-amino-6-(3-chloropyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 80 nM
(R)-3-(2-amino-6-(3-methylpyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 35 nM
(R)-N-(3-(3-amino-1-methyl-9-oxa-4-thia-2-azaspiro[5.5]undec-2-en-1-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(R)-N-(3-(3-amino-5-methyl-9,9-dioxido-2,9-dithia-4-azaspiro[5.5]undec-3-en-5-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(R)-N-(3-(3-amino-9,9-difluoro-5-methyl-2-thia-4-azaspiro[5.5]undec-3-en-5-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(R)-N-(3-(7-amino-2,2-difluoro-9-methyl-6-thia-8-azaspiro[3.5]non-7-en-9-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(S)-3-(6,6-dimethyl-3,6-dihydro-2H-pyran-4-yl)-7-(2-fluoropyridin-3-yl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine
inhibitor shows good BACE1 functional potency, permeability, intrinsic stability, and P-glycoprotein efflux ratios
(S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5H-spiro[chromeno[2,3-b]pyridine-5,4-oxazol]-2-amine
i.e. AMG-8718.compound exhibits a balanced profile of BACE1 potency, hERG binding affinity, and P-glycoprotein recognition. Compound produces robust and sustained reductions of cerebrospinal fluid and brain amyloid beta levels in a rat pharmacodynamic model
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(2,2,2-trifluoroethoxy)pyrazine-2-carboxamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(difluoromethyl)pyrazine-2-carboxamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-chloropicolinamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-cyanopicolinamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-fluoropicolinamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide
-
1,1'-piperazine-1,4-diylbis[3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol]
-
inhibitor identified by in silico mulit-filter approaches. Calculated binding free energy of R,S-isomer -48 kcal/mol
1,1'-piperazine-1,4-diylbis[3-(9H-carbazol-9-yl)propan-2-ol]
-
inhibitor identified by in silico mulit-filter approaches. Calculated binding free energy of S,R-isomer -48.2 kcal/mol
1,3-bis(3,5-bis(trifluoromethyl)phenyl)urea
100% inhibition at 100 nM, 15% inhibition at 10 nM
1,5-anhydro-1-[7-hydroxy-2-[(2S)-2-hydroxypropyl]-5-methyl-4-oxo-4H-chromen-8-yl]hexitol
-
37.2% inhibition at 0.1 mM
1,5-anhydro-1-[7-hydroxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]-2-O-[(E)-2-(4-hydroxyphenyl)ethenyl]hexitol
-
39.5% inhibition at 0.1 mM
1,5-anhydro-1-[7-methoxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol
-
41.0% inhibition at 0.1 mM
1,5-anhydro-2-O-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-1-[7-hydroxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol
-
36.4% inhibition at 0.1 mM
1,5-anhydro-2-O-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-1-[7-methoxy-5-methyl-4-oxo-2-(2-oxopropyl)-4H-chromen-8-yl]hexitol
-
48.7% inhibition at 0.1 mM
1-(2-chlorobenzyl)-4-(4-(dibenzo[b,d]furan-1-yl)benzyl)-1H-imidazol-2-amine
-
0.005 mM, 37.8% inhibition. Inhibitor is predicted to be able to cross the blood-brain barrier
1-(3,5-bis(trifluoromethyl)-phenyl)-3-(3,5-dimethylphenyl)urea
80% inhibition at 100 nM
1-(4-fluorobenzyl)-4-((30,50-dimethoxybiphenyl-4-yl)methyl)-1H-imidazol-2-amine
-
0.005 mM, 40% inhibition. Inhibitor is predicted to be able to cross the blood-brain barrier
1-[ (3-benzoylamino-phenylcarbamoyl)-methyl]-pyridinium chloride
-
51% inhibition at 0.05 mM
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-carbamoyl-pyridiniumchloride
-
54% inhibition at 0.05 mM
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
55% inhibition at 0.05 mM
1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
61% inhibition at 0.05 mM
1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
42% inhibition at 0.05 mM
1-[(E)-[(4-methylquinazolin-2-yl)amino][(phenylcarbamoyl)amino]methylidene]-3-phenylurea
-
complete inhibition at 0.1 mM
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
78% inhibition at 0.05 mM
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
44% inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylsulfamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
50% inhibition at 0.05 mM
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
-
11-oxo-N-(pyridin-4-yl)-10,11-dihydro-5H-dibenzo[b,e][1,4]-diazepine-3-carboxamide
-
-
15,16-dihydrotanshinone
-
16-amino-11-cyclohexyl-2-oxa-11,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-12-one
-
-
1[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
68% inhibition at 0.05 mM
2'-O-coumaroyl-(S)-aloesinol
-
51.9% inhibition at 0.1 mM
2'-O-[p-methoxy-(E)-cinnamoyl]-(S)-aloesinol
-
34.1% inhibition at 0.1 mM
2,3-dihydro-6-methylginkgetin
isolated from from Cephalotaxus harringtonia var. fastigiata
2,3-dihydroamentoflavone
a 2,3-dihydroamentoflavone from Cycas revoluta
2-((4-amino-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
17.8% inhibition at 0.05 mM
2-((5-amino-1,3,4-thiadiazol-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
21.8% inhibition at 0.05 mM
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
62.4% inhibition at 0.05 mM
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
77.5% inhibition at 0.05 mM
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
25.9% inhibition at 0.05 mM
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide
9.4% inhibition at 0.05 mM
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
85.6% inhibition at 0.05 mM
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(p-tolyl)thiazol-2-yl)acetamide
11.5% inhibition at 0.05 mM
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide
84.5% inhibition at 0.01 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(2-nitrophenyl)thiazol-2-yl)acetamide
6.5% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-(2-fluoropyridin-3-yl)phenyl)thiazol-2-yl)acetamide
88.7% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
78.5% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide
16.5% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
83.9% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(p-tolyl)thiazol-2-yl)acetamide
8.1% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide
78.6% inhibition at 0.01 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
50.7% inhibition at 0.05 mM
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
12.3% inhibition at 0.01 mM
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
5.9% inhibition at 0.01 mM
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
10.7% inhibition at 0.05 mM
2-((5-cyano-6-oxo-4-(3-(trifluoromethoxy)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
85.8% inhibition at 0.05 mM
2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
82.5% inhibition at 0.05 mM
2-((6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
22.5% inhibition at 0.05 mM
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
-
i.e. norartocarpetin, prenylated flavone from the stem bark of Morus lhou, noncompetitive
2-(2-(4-(6-bromo-3-(tert-butylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
34.28% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)-5-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
87.94% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)-6-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
63.7% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)-7-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
complete inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)-8-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
69.43% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl)isoindoline-1,3-dione
69.49% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
less than 10% inhibition at 0.05 mM
2-(3-(4-(3-(tert-butylamino)-6-chloroimidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl)isoindoline-1,3-dione
37.9% inhibition at 0.05 mM
2-(3-(4-(3-(tert-butylamino)-6-chloroimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
32.95% inhibition at 0.05 mM
2-(3-(4-(3-(tert-butylamino)-7-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
24.24% inhibition at 0.01 mM
2-(3-(4-(6-bromo-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione
43.17% inhibition at 0.05 mM
2-(3-(4-(6-bromo-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
45.3% inhibition at 0.05 mM
2-(3-(4-(6-bromo-3-(tert-butylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione
48.72% inhibition at 0.05 mM
2-(3-(4-(6-chloro-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione
88.097% inhibition at 0.05 mM
2-(3-(4-(6-chloro-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
19.6% inhibition at 0.05 mM
2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole
inhibitor of BACE1, EC 3.4.23.46. 150fold more effective on BACE1 than BACE2
2-amino-3,4-dihydroquinazoline
-
-
2-amino-3-ethyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-3-methyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(pyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
exhibits modest selectivity (about 8fold) against BACE2
2-amino-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-5-[3-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-3-methyl-5-phenyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-3-methyl-5-[2-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-[2-methyl-6-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
24% inhibition at 0.0125 mM
2-amino-3-methyl-6-(naphthalen-2-ylmethyl)pyrimidin-4(3H)-one
-
2-amino-3-[(1R)-1-cyclohexyl-2-[(cyclohexylcarbonyl)amino]ethyl]-6-phenoxyquinazolin-3-ium
-
2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl 3-chlorobenzoate
-
2-amino-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(1,3-benzodioxol-5-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(2,3-dihydro-1-benzofuran-5-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(2,6-diethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2,6-dimethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2-ethyl-6-methylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
28% inhibition at 0.0125 mM
2-amino-5-(2-ethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3,4-dimethoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-butoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-chlorophenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-ethoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-methoxy-4-methylphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-methoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-methoxyphenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-chlorophenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-ethyl-3-methoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-(6-methylbiphenyl-3-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-methoxyphenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3,4-dimethoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-butoxy-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-chloro-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-cyclopentyl-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-ethoxy-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-ethoxy-4-propoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-fluoro-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-[3-(cyclopentyloxy)-4-methoxyphenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-[4-methoxy-3-(propan-2-yloxy)phenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-[4-methoxy-3-(trifluoromethyl)phenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[2-fluoro-3-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
2-amino-5-[3-(2-methoxypyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[3-(6-fluoropyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[3-(6-methoxypyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[3-fluoro-5-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[4-fluoro-3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
aminohydantoin inhibitor, shows comparable activity in a cell-based assay, and demonstrates more than 100fold selectivity for the other structurally related aspartyl proteases BACE2, cathepsinD, renin, and pepsin
2-amino-6-(3a,7a-dihydro-1H-indol-6-ylmethyl)-3-methylpyrimidin-4(3H)-one
-
2-amino-6-(3a,7a-dihydro-1H-indol-6-ylmethyl)pyrimidin-4(3H)-one
-
2-amino-6-benzyl-3-methylpyrimidin-4(3H)-one
-
2-amino-8-(2-nitrophenyl)-9-phenyl-1,9-dihydro-6H-purin-6-one
-
2-amino-8-(4-bromophenyl)-9-phenyl-1,9-dihydro-6H-purin-6-one
-
2-deoxy-4-O-beta-D-glucopyranuronosyl-6-O-sulfo-2-(sulfoamino)-beta-D-glucopyranose
-
IC50: 0.000053 mg/ml
2-[(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)amino]-2-oxoethyl [(4,6-diphenylpyrimidin-2-yl)sulfanyl]acetate
-
75% inhibition at 0.1 mM
2-[(3-cyano-4,6-diphenylpyridin-2-yl)sulfanyl]-N-(3-nitrophenyl)acetamide
-
complete inhibition at 0.1 mM
2-[(4-methyl-5-[2-[(4-methylphenyl)amino]-2-oxoethyl]-4H-1,2,4-triazol-3-yl)sulfanyl]-N-(4-phenyl-1,3-thiazol-2-yl)acetamide
-
83% inhibition at 0.1 mM
2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]-N-(2-fluorophenyl)acetamide
-
90% inhibition at 0.1 mM
2-[[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]carbamoyl]-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]pyridin-4-yl methanesulfonate
i.e. KMI-1036, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
-
-
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]ethanol
-
1.7% inhibition at 0.0125 mM
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-5-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
-
8.46% inhibition at 0.0125 mM
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-5-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]ethanol
-
5.43% inhibition at 0.0125 mM
2-[[3-cyano-4-(4-fluorophenyl)-6-phenylpyridin-2-yl]sulfanyl]-N-(tricyclo[3.3.1.1(3,7)]dec-1-yl)acetamide
-
45% inhibition at 0.1 mM
2-[[3-cyano-6-(4-fluorophenyl)-4-phenylpyridin-2-yl]sulfanyl]-N-(5-ethyl-1,3,4-thiadiazol-2-yl)acetamide
-
80% inhibition at 0.1 mM
2-[[4-(4-chlorophenyl)-3-cyano-6-(4-methoxyphenyl)pyridin-2-yl]sulfanyl]-N-(naphthalen-2-yl)-N-phenylacetamide
-
68% inhibition at 0.1 mM
2-[[4-benzyl-5-(1H-indol-3-ylmethyl)-4H-1,2,4-triazol-3-yl]sulfanyl]-1-(1H-indol-3-yl)ethanone
-
75% inhibition at 0.1 mM
3-(3H-imidazo[4,5-c]pyridin-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(5-((7aR)-6-(5-fluoropyrimidin-2-yl)-2-imino-3-methyl-4-oxooctahydro-1H-pyrrolo[3,4-d]pyrimidin-7a-yl)thiophen-3-yl)benzonitrile
orally active, brain penetrant inhibitor that reduces amyloid beta40 in the plasma, cerebrospinal fluid, and cortex of rats in a dose-dependent manner
3-(5-(4-fluorophenyl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(5-(pyridin-4-yl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]-diazepin-11(10H)-one
-
-
3-(6-(2-acetylphenyl)-2-aminoquinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 11 nM
3-(6-fluoro-1H-benzo[d]imidazol-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(benzylsulfanyl)-6-(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
-
48% inhibition at 0.1 mM
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(3,3,3-trifluoropropanoyl)-D-alaninamide
-
-
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(methoxyacetyl)-D-alaninamide
-
-
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(pyridin-3-ylacetyl)-D-alaninamide
-
-
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(pyridin-4-ylacetyl)-D-alaninamide
-
-
3-(butylsulfonyl)-N2-(3-cyanopropanoyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
-
-
3-(butylsulfonyl)-N2-(cyclopropylcarbonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
-
-
3-(cyclohexylsulfonyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
-
-
3-(dibutylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
-
-
3-(dipropylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
-
-
3-(heptan-4-ylsulfonyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
-
-
3-carbamoyl-1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
44% inhibition at 0.05 mM
3-carbamoyl-1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
69% inhibition at 0.05 mM
3-carbamoyl-1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
64% inhibition at 0.05 mM
3-carbamoyl-1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
complete inhibition at 0.05 mM
3-carbamoyl-1-[[3-(4-methoxy-phenylsulfamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
34% inhibition at 0.05 mM
3-carbamoyl-1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
24% inhibition at 0.05 mM
3-carbamoyl-1-[[3-(toluene-4-sulfonylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
4% inhibition at 0.05 mM
3-chloro-N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]benzamide
-
-
3-phenethylcarbamoyl-1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
58% inhibition at 0.05 mM
3-phenethylcarbamoyl-1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
72% inhibition at 0.05 mM
3-phenethylcarbamoyl-1-[[3-(toluene-4-sulfonylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
36% inhibition at 0.05 mM
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carbamoylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.0002 mM, 78.1% inhibition
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
0.0002 mM, 94.2% inhibition, IC50: 6.6 nM
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
0.0002 mM, 97.2% inhibition, IC50: 6.4 nM
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
-
-
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
-
-
3-[2-amino-6-(phenylcarbonyl)quinazolin-3(4H)-yl]-N-cyclohexyl-N-methylpropanamide
-
-
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
-
-
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
-
-
3-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]propan-1-ol
-
-
3-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]propan-1-ol
-
47% inhibition at 0.0125 mM
4',5,7-trimethoxyflavone
-
4-(2-amino-6-phenoxyquinazolin-3(4H)-yl)-N,4-dicyclohexyl-N-methylbutanamide
-
-
4-(4-[1-[(6-aminopyridin-2-yl)methyl]-5-(2-chlorophenyl)-1H-pyrrol-2-yl]phenoxy)butanenitrile
-
-
4-(cyclohexylamino)-1-(4-fluorobenzyl)-8-[(2'-methylbiphenyl-4-yl)methyl]-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
-
4-(dipropylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]butanamide
-
-
4-bromo-N-[(4-bromophenyl)sulfonyl]-N-[1-(3,4-dichlorobenzyl)-1H-pyrazol-4-yl]benzenesulfonamide
-
50% inhibition at 0.1 mM
4-fluoro-1-(pyridin-4-yl)-1-[3-(pyrimidin-5-yl)phenyl]-1H-isoindol-3-amine
i.e. AZ2000. Inhibitor with improved brain disposition, reduces amyloid beta levels in both brain and periphery already after acute dosing. Mice heterozygous for BACE1, display a 62% reduction in plasma amyloid beta40 levels, whereas brain amyloid beta40 is only lowered by 11%
4-[1-(4-methoxyphenyl)-2-[4-(trifluoromethyl)phenyl]ethyl]-1-methyl-1H-imidazol-2-amine
-
-
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-(prop-2-en-1-yl)benzamide
-
6.2% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-(propan-2-yl)benzamide
-
6.58% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-butylbenzamide
-
45% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-cyclobutylbenzamide
-
38.4% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-cyclopropylbenzamide
-
10.6% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-ethylbenzamide
-
36% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-propylbenzamide
-
28% inhibition at 0.0125 mM
4-[2-(2,6-diethylpyridin-4-yl)-5-(pyrimidin-5-yl)phenyl]-1-methyl-4,5-dihydro-1H-imidazol-2-amine
-
4-[2-(2-methoxy-5-nitrophenyl)-1-(4-methoxyphenyl)ethyl]-1-methyl-1H-imidazol-2-amine
-
-
4-[4-fluoro-5-methoxy-2-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
-
highly active BACE-1 inhibitor
4-[5-methoxy-2-(2-methoxy-5-nitrophenyl)-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
-
-
4-[5-methoxy-2-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
-
-
4-[8-benzyl-4-(cyclohexylamino)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-1-yl]benzamide
-
-
4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-2-amine
-
5-[(E)-benzylideneamino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
-
5-[(E)-[(2,4,-diclorophenyl)methylidene]amino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
-
5-[(E)-[(2-chlorophenyl)methylidene]amino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
-
5-[2-amino-4-(4-methoxy-3-methylphenyl)-1-methyl-5-oxo-4,5-dihydro-1H-imidazol-4-yl]biphenyl-2-carbonitrile
-
5-[2-amino-4-(biphenyl-3-yl)-1-methyl-5-oxo-4,5-dihydro-1H-imidazol-4-yl]-2-methoxybenzonitrile
-
6,7-furano-5,8a-dimethoxy hydrocoumaric acid methyl ester
-
inhibits 57.2% of the BACE1 activity at a concentration of 1 mM
6,7-furano-5-methoxy hydrocoumaric acid
-
-
6,7-furano-5-methoxy hydrocoumaric acid methyl ester
-
-
6,7-furano-5-prenyloxy hydrocoumaric acid
-
-
6,7-furano-5-prenyloxy hydrocoumaric acid methyl ester
-
-
6,7-furano-8,8a-dimethoxy hydrocoumaric acid methyl ester
-
inhibits 48.3% of the BACE1 activity at a concentration of 1 mM
6,7-furano-8-methoxy hydrocoumaric acid
-
-
6,7-furano-8-methoxy hydrocoumaric acid methyl ester
-
inhibits 36.4% of the BACE1 activity at a concentration of 1 mM
6,7-furano-8a-methoxy-5-prenyloxy hydrocoumaric acid
-
-
6,7-furano-8a-methoxy-5-prenyloxy hydrocoumaric acid methyl ester
-
competitive-type inhibitor
6-([2-(2-chlorophenyl)-5-[4-(1,3-thiazol-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
3.4% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(hexyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
13% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
31% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyrazin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
46.6% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyridazin-3-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
10.4% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyridin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
6.61% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyridin-3-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
7.1% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyridin-4-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
7.22% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
9.7% inhibition at 0.0125 mM
6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole
inhibitor of BACE1, EC 3.4.23.46. 200fold more effective on BACE1 than BACE2
6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole
inhibitor of BACE1, EC 3.4.23.46. 100fold more effective on BACE1 than BACE2
6-methoxy-5-[(E)-(4-methylbenzylidene)amino]-N4-phenylpyrimidine-2,4-diamine
-
6-methoxy-5-[(E)-[(2-nitrophenyl)methylidene]amino]-N4-phenylpyrimidine-2,4-diamine
-
6-methoxy-N4-phenyl-5-[(E)-[4-(trifluoromethyl)benzylidene]amino]pyrimidine-2,4-diamine
-
6-[(2,5-diphenyl-1H-pyrrol-1-yl)methyl]pyridin-2-amine
-
15% inhibition at 0.0125 mM
6-[(3R,4S)-3-benzyl-4-hydroxy-5-oxo-5-[[3-(2H-tetrazol-5-yl)phenyl]amino]pentanoyl]-N-[(1R)-1-(4-fluorophenyl)ethyl]-4-oxo-4H-pyran-2-carboxamide
76% inhibition at 2 microM
6-[[2-(2-chlorophenyl)-5-(4-methoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine
-
30% inhibition at 0.0125 mM
6-[[2-(2-chlorophenyl)-5-(4-phenoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine
-
16% inhibition at 0.0125 mM
6-[[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine
-
48% inhibition at 0.0125 mM
6-[[2-(4-butoxyphenyl)-5-(2-chlorophenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine
-
31% inhibition at 0.0125 mM
7-phloroethol
-
significant BACE1 inhibition in a dose-dependent manner
8,8-diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine
-
-
8-(biphenyl-4-ylmethyl)-4-(cyclohexylamino)-1-(4-fluorobenzyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
-
8-benzyl-4-(cyclohexylamino)-1-(3-fluorophenyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
-
8-C-glucosyl-(R)-aloesol
-
39.2% inhibition at 0.1 mM
8-C-glucosyl-7-methoxy-(R)-aloesol
-
26.8% inhibition at 0.1 mM
8-C-glucosyl-7-O-methylaloediol
-
-
AD115
-
a fragment of Gleevec
AD28
-
a fragment of Gleevec
AD94
-
a fragment of Gleevec
AD95
-
a fragment of Gleevec, strong inhibition
allo-aloeresin D
-
-
Allocryptopine
26.18% inhibition at 0.005 mM
aloeresin D
-
71.5% inhibition at 0.1 mM
aloesin
-
37.5% inhibition at 0.1 mM
BACEi-II
-
inhibition may protect neurons from death induced by okadaic acid
benzyl 1-(3-acetoxypropyl)-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-(dimethylamino)-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-(isopropyl(methyl)amino)-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-ethoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-2,4-dimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-methoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1-(2-morpholino-2-oxoethyl)-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-1-(methylsulfonyl)-4-phenyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-1-(methylsulfonyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-ethyl-2,6-dimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-isopropyl-2,6-dimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
-
-
benzyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
-
-
benzyl [2-([1-benzyl-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]amino)-2-oxo-1-[[(1-propylbutyl)sulfonyl]methyl]ethyl]carbamate
-
-
beta-secretase inhibitor IV
-
complete inhibition at 0.001 mM
beta-secretase inhibitor-II
-
-
C-2'-decoumaroyl-aloeresin G
-
72.0% inhibition at 0.1 mM
CA074Me
-
treatment of London APP transgenic mouse model of Alzheimer's disease that expresses human amyloid precursor protein containing the wild-type beta-secretase site results in substantial improvement in memory deficit assessed by the Morris water maze test. Improved memory function is accompanied by reduced amyloid plaque load, decreased amyloid beta40 and amyloid beta42, and reduced C-terminal beta-secretase fragment derived from amyloid precursor protein by beta-secretase. Inhibitor has no effects on any of these parameters in mice expressing the Swedish mutant beta-secretase site of amyloid precursor protein
caffeic acid
-
chitosan oligosaccharide
IC50 of 0.098 mg/ml
cis-4-[(13S)-15-amino-13-cyclohexyl-11-oxo-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-10-yl]cyclohexanecarboxylic acid
-
-
cryptotanshinone
-
dehydrodanshenol A
-
deoxyneocryptotanshinone
mixed-type inhibition
dieckol
-
significant BACE1 inhibition in a dose-dependent manner
dioxinodehydroeckol
-
significant BACE1 inhibition in a dose-dependent manner
E64d
-
treatment of London APP transgenic mouse model of Alzheimer's disease that expresses human amyloid precursor protein containing the wild-type beta-secretase site results in substantial improvement in memory deficit assessed by the Morris water maze test. Improved memory function is accompanied by reduced amyloid plaque load, decreased amyloid beta40 and amyloid beta42, and reduced C-terminal beta-secretase fragment derived from amyloid precursor protein by beta-secretase. Inhibitor has no effects on any of these parameters in mice expressing the Swedish mutant beta-secretase site of amyloid precursor protein
eckol
-
significant BACE1 inhibition in a dose-dependent manner
EMD 565788
-
specific BACE1 inhibitor
ethyl 4-[[(1R,4S,5R,7R)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl]carbonyl]piperazine-1-carboxylate
9% inhibition at 0.01 mM
ethyl 4-[[(1R,5R,7R)-3-benzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl]carbonyl]piperazine-1-carboxylate
29% inhibition at 0.01 mM
EVD(statine)VAEF
EVE(statine)VAEF
EVG(statine)VAEF
EVL(statine)VAEF
EVNLAAEF
EVW(statine)VAEF
EVY(statine)VAEF
ferruginol
-
Gleevec
-
-
grandifolia F
-
-
GRL-8234
heparin
-
leads to increased autocatalytic cleavage of beta-secretase and a subsequent loss of enzyme activity in vitro
heparin sulfate
-
heparin sulfate analogue derived from porcine mucosal intestinal heparin are effective beta-secretase inhibitors, but have negligible activity as anticoagulants or as inhibitors of other aspartyl proteases structurally related to beta-secretase. The structure of the polysaccharide is important for the interaction with beta-secretase, not simply the level of sulfation or charge
imperatorin
isoimperatorin
-
-
isopropyl 2-(3-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-5-((R)-1-phenylethylcarbamoyl)-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-methyl-5-((R)-1-phenylethylcarbamoyl)pyridin-1(4H)-yl) acetate
-
-
isopropyl 2-(3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-5-((R)-1-phenylethylcarbamoyl)-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxybenzylamino)-1-phenyl butan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxybenzylamino)-1-phenylbutan-2-ylcarbamoyl)-2,4-dimethylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4-dimethylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
-
-
KTEEISEVN(statine)VAEF
KTEETSEVN(statine)VAEF
i.e. P10-P40 StatVal, activity completely abolished using saturating dose of 2.1 microM of the inhibitor, cleavage products of beta-secretase measured by fluoresence assay
kuwanon
-
prenylated flavone from the stem bark of Morus lhou, noncompetitive
kuwanon A
-
prenylated flavone from the stem bark of Morus lhou, noncompetitive
L-alpha-glutamyl-L-leucyl-N-[(2S,5S,8S,14R)-2-carboxy-5-(carboxymethoxy)-13-hydroxy-11,16-dimethyl-13-oxido-4,7,10-trioxo-1-phenyl-8-(propan-2-yl)-3,6,9-triaza-13-lambda5-phosphaheptadecan-14-yl]-L-alpha-asparagine
-
-
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 99.7% inhibition
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 98.3% inhibition
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carbamoylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 29.2% inhibition; 0.002 mM, 62.1% inhibition
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 83.7% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-([3-(4-methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]amino)-3-oxopropyl]-L-leucinamide
-
0.002 mM, 74.2% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide
-
0.002 mM, 92.2% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
0.002 mM, 94.4% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-thiadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
0.002 mM, 91.9% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
-
luteolin
-
isolated from methanolic extracts of Perilla frutescens
LY2039911
LY2811376
-
LY2886721
-
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-(statine)-Val-Ala-Glu-Phe-OH
-
-
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe
-
complete inhibition at 0.1 mM
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-[statine(3S,4S)]-Val-Ala-Glu-Phe-OH
-
-
magnesium lithospermate
-
memantine
-
-
methyl (1R,4S,5R,7R)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxylate
16% inhibition at 0.01 mM
methyl (1R,5R,7R)-3-benzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxylate
16% inhibition at 0.01 mM
methyl (1S,4R,5S,7S)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxylate
16% inhibition at 0.01 mM
methyl tanshinonate
-
methyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
-
-
morusin
-
prenylated flavone from the stem bark of Morus lhou, noncompetitive
N'-[(2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-[(3-iodobenzyl)amino]butan-2-yl]-5-methyl-N,N-dipropylbenzene-1,3-dicarboxamide
-
-
N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-N-methyl-5-[methyl(methylsulfonyl)amino]-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxohexan-2-yl]amino)-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxohexan-2-yl]amino)-1-phenylbutan-2-yl]-N-methyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-[(3-iodobenzyl)amino]-1-phenylbutan-2-yl]-N,N-dipropylbenzene-1,3-dicarboxamide
-
-
N'-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-N,N-dipropylbenzene-1,3-dicarboxamide
-
-
N,N'-bis(3-cyano-4,5,6,7,8,9-hexahydrocycloocta[b]thiophen-2-yl)-2,2,3,3,4,4,5,5-octafluorohexanediamide
-
87% inhibition at 0.1 mM
N- [N-(3,5-difluorophenacetyl-L-alanyl)]-S-phenylglycine tert-butyl ester
-
complete inhibition at 0.1 mM
N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
N-((4aRS,6RS,8aSR)-2-amino-5,6,7,8-tetrahydro-4H-4a,8a-(methanooxymethano)benzo[d][1,3]thiazin-6-yl)-3-chlorobenzamide
-
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)-3-chlorobenzamide
-
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)-5-fluoropyridine-2-carboxamide
-
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)benzamide
-
N-(2-methyl-5-[(6-phenylpyrimidin-4-yl)amino]phenyl)methanesulfonamide
-
-
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
-
-
N-(3-((4R,5R)-2-amino-5-methoxy-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
N-(3-((4S,5R)-2-amino-4-methyl-5-(tetrahydro-2H-pyran-4-yl)-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
N-(3-((4S,5R)-2-amino-4-methyl-5-phenyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
N-(3-((4S,5S)-2-amino-4-methyl-5-phenyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
N-(4-(3-bromophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
90.4% inhibition at 0.05 mM
N-(4-(4-acetamido-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
4.7% inhibition at 0.05 mM
N-(4-(4-acetamido-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
1.4% inhibition at 0.05 mM
N-(4-(4-amino-3,5-dichlorophenyl)-1H-imidazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
87.7% inhibition at 0.01 mM
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
79.9% inhibition at 0.05 mM
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
91.8% inhibition at 0.05 mM
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-6-oxo-4-(3-(trifluoromethoxy)phenyl)-1,6-dihydropyrimidin-2-yl)thio)acetamide
39.6% inhibition at 0.05 mM
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)acetamide
86.1% inhibition at 0.05 mM
N-(4-([4-(cyclohexylamino)-1-(3-fluorophenyl)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-8-yl]methyl)phenyl)acetamide
-
-
N-(4-fluorophenyl)-11-oxo-10,11-dihydro-5H-dibenzo[b,e]-[1,4]diazepine-3-carboxamide
-
-
N-(4-[1-[(6-aminopyridin-2-yl)methyl]-5-(2-chlorophenyl)-1H-pyrrol-2-yl]phenyl)pyrimidin-5-amine
-
9.8% inhibition at 0.0125 mM
N-(5-([6-(4-(N,N-dimethyl)aminophenyl)pyrimidin-4-yl]amino)-2-methylphenyl)-N-methylmethanesulfonamide
-
-
N-(5-[[6-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-4-yl]amino]-2-methylphenyl)-N-methylmethanesulfonamide
-
-
N-(tert-butoxycarbonyl)-L-isoleucyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
no inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-isoleucyl-N-[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-phenylalaninamide
-
no inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-leucyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
54.57% inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-leucyl-N-[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-phenylalaninamide
-
0.91% inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-valyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
no inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-valyl-N-[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-phenylalaninamide
-
no inhibition at 0.01 mg/ml
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
-
-
N-acetyl-beta-alanyl-3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
-
-
N-acetyl-L-alanyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
-
-
N-acetyl-L-leucyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-alaninamide
-
-
N-acetyl-L-leucyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
-
-
N-acetyl-L-valyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
-
-
N-benzyloxycarbonyl-Val-Leu-leucinal
-
-
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
-
-
N-[(1S)-1-[(butylsulfonyl)methyl]-2-([1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl]amino)-2-oxoethyl]benzamide
-
-
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(3-ethoxybenzyl)amino]propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
N-[(1S,2R,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-4-methoxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-4-oxo-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]-1,4-dihydropyridine-2-carboxamide
i.e. KMI-1030, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-4-oxo-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]-4H-pyran-2-carboxamide
i.e. KMI-1027, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]pyridine-2-carboxamide
i.e. KMI-1023, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
N-[(1S,2S,4R)-2-azido-4-((S)-1-benzylcarbamoyl-2-methyl-propylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-4-methoxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-4-(2-methoxy-ethoxy)-butyl]-5-(methanesulfonyl-methylamino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-4-propyloxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-4-ethyloxy-2-hydroxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-2-amino-1-(3,5-difluoro-phenoxymethyl)-4-methoxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-4-allyloxy-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-4-benzyloxy-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-4-cyclopropylmethoxy-1-(3,5-difluorophenoxymethyl)-2-hydroxy-butyl]-5-(methanesulfonylmethyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-4-methoxybutyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenylethyl)-isophthalamide
-
N-[(1Z)-amino(butylamino)methylidene]-2-[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]acetamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-2-methylbenzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-3-hydroxybenzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-(trifluoromethyl)benzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-methoxybenzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-methylbenzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]benzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]pyridine-2-carboxamide
-
-
N-[(2R)-2-amino-1-benzyl-3-fluoropropyl]-2-[[(2-methylcyclopropyl)methyl]amino]-6-[methyl[(1-methylethyl)sulfonyl]amino]pyridine-4-carboxamide
-
-
N-[(2S)-1-([(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]amino)-1-oxo-3-phenylpropan-2-yl]naphthalene-1-carboxamide
-
no inhibition at 0.01 mg/ml
N-[(2S)-1-([(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]amino)-3-(4-nitrophenyl)-1-oxopropan-2-yl]naphthalene-1-carboxamide
-
no inhibition at 0.01 mg/ml
N-[(2S)-1-[[(2S,3S)-1-(butan-2-ylamino)-3-hydroxy-1-oxohexan-2-yl]amino]-3-phenylpropan-2-yl]-7-ethyl-1-methyl-3,4-dihydro-1H-[1,2,5]thiadiazepino[3,4,5-hi]indole-9-carboxamide 2,2-dioxide
compound designed specifically to interact with S1' active site residues to provide selectivity over memapsin 1 and cathepsin D. Inhibitor exhibits exceedingly potent inhibitory activity and high selectivity over BACE 2 and cathepsin D
N-[(2S)-1-[[(3S)-1-(butan-2-ylamino)-3-hydroxy-1-oxobutan-2-yl]amino]-3-phenylpropan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
compound designed specifically to interact with S1' active site residues to provide selectivity over memapsin 1 and cathepsin D. Inhibitor exhibits exceedingly potent inhibitory activity and high selectivity over BACE 2 and cathepsin D
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-1H-imidazole-2-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-4-hydroxypyridine-3-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-5-methyl-1H-pyrazole-3-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyrazine-2-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyridine-3-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyridine-4-carboxamide
-
-
N-[(2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-[(3-iodobenzyl)amino]butan-2-yl]-3-methylbenzamide
-
-
N-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-5-methyl-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-(phenylsulfonyl)propanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-(piperidin-1-ylsulfonyl)propanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-[(3-methylbutyl)sulfamoyl]propanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-[(3-methylbutyl)sulfonyl]propanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-4-(phenylsulfonyl)butanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-4-(piperidin-1-ylsulfonyl)butanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N-[(2S,3S)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-N'-[(1R)-1-(4-fluorophenyl)ethyl]-5-[(methylsulfonyl)amino]benzene-1,3-dicarboxamide
-
-
N-[(2S,3S,5R)-6-[[(2S)-1-(benzylamino)-3-methyl-1-oxobutan-2-yl]amino]-1-(3,5-difluorophenoxy)-3-hydroxy-5-methoxy-6-oxohexan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
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
-
-
N-[(3S,6S,13R)-13-[(3-[[(2S)-1-[[(1S)-1-(carboxymethoxy)-2-[[(1S)-1-carboxy-2-phenylethyl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl)(hydroxy)phosphoryl]-3-(carboxymethyl)-2,5-dioxo-1,4-diazacyclotridecan-6-yl]-L-alpha-glutamine
-
-
N-[(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-2-oxo-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-19-yl]-N-methylpropane-1-sulfonamide
-
-
N-[(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-2-oxo-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-19-yl]-N-methylpropane-1-sulfonamide
-
-
N-[(4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]methylcarbamoyl-5-hydroxy-2-methyloct-4-yl]-N'-[(R)-1-(4-fluorophenyl)ethyl-5-methyl(methylsulfonyl)amino]isophthalamide
-
-
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-Nalpha-(4-nitrobenzoyl)-L-phenylalaninamide
-
10.48% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-Nalpha-[(2Z)-3-phenylprop-2-enoyl]-L-phenylalaninamide
-
37.22% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-Nalpha-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-phenylalaninamide
-
0.13% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-Nalpha-(4-nitrobenzoyl)-L-phenylalaninamide
-
1.47% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-Nalpha-[(2Z)-3-phenylprop-2-enoyl]-L-phenylalaninamide
-
22.83% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-Nalpha-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-phenylalaninamide
-
59.66% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-Nalpha-(tert-butoxycarbonyl)-L-phenylalaninamide
-
22.96% inhibition at 0.01 mg/ml
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
-
-
N-[(Z)-[(4,6-dimethylpyrimidin-2-yl)amino][(3-nitrophenyl)amino]methylidene]-10H-phenothiazine-10-carboxamide
-
80% inhibition at 0.1 mM
N-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-iodobenzyl)amino]propyl]-5-methyl-N'-propylbenzene-1,3-dicarboxamide
-
-
N-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]-5-methyl-N'-propylbenzene-1,3-dicarboxamide
-
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]acetamide
N-[2-[(4aR,6S,8aR)-2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl]-1,3-thiazol-4-yl]-5-(difluoromethoxy)pyridine-2-carboxamide
-
N-[3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl]-5-chloropyridine-2-carboxamide
-
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-3,4-dichloro-N-phenylbenzamide
-
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-4-methoxy-N-phenylbenzamide
-
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-N-(2-phenylethyl)benzamide
-
N-[3-[(4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl]-5-(1H-1,2,4-triazol-1-yl)pyrazine-2-carboxamide
-
N-[5-(2,3-dichlorobenzyl)-1,3-thiazol-2-yl]-4-([[4-phenyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)benzamide
-
78% inhibition at 0.1 mM
N1-((2S,3R)-3-hydroxy-1-phenyl-4-((3-(trifluoromethyl)benzyl)amino)butan-2-yl)-N3,5-dimethyl-N3-((R)-1-phenylethyl)isophthalamide
more than 500fold selectivity for BACE2 over BACE1
N1-((2S,3S)-4-(4-(diethylcarbamoyl)-1H-pyrazol-1-yl)-3-hydroxy-1-phenylbutan-2-yl)-N3-((R)-1-(4-fluorophenyl)ethyl)-5-(N-methylmethylsulfonamido)isophthalamide
compound exhibits good inhibition effects on amyloid beta production in the cell-based assay
N1-((R)-1-(4-fluorophenyl)ethyl)-N3-((2S,3S)-3-hydroxy-4-(4-((R)-1-hydroxy ethyl)-1H-1,2,3-triazol-1-yl)-1-phenylbutan-2-yl)-5-(N-methylmethylsulfonamido)isophthalamide
-
N1-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]-N3-propylbenzene-1,3,5-tricarboxamide
-
-
N1-[1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl]-N3-propylbenzene-1,3,5-tricarboxamide
-
-
N2-acetyl-3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
-
-
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
-
-
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
-
-
N3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl)-2,4,6-trimethyl-1-(methylsulfonyl)-N5-((R)-1-phenylethyl)-1,4-dihydropyridine-3,5-dicarboxamide
-
-
N3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl)-4-ethyl-2,6-dimethyl-1-(methylsulfonyl)-N5-((R)-1-phenylethyl)-1,4-dihydropyridine-3,5-dicarboxamide
-
-
N3-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(1S,2S)-2-hydroxy-1-(isobutylcarbamoyl)pentyl]amino]propyl]-N1-methyl-N1-[(1R)-1-phenylpropyl]benzene-1,3-dicarboxamide
174000fold selectivity for BACE2 over BACE1
N3-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(1S,2S)-2-hydroxy-1-(isobutylcarbamoyl)propyl]amino]propyl]-5-[methyl(methylsulfonyl)amino]-N1-[(1R)-1-phenylpropyl]benzene-1,3-dicarboxamide
-
Nalpha-(1,3-benzodioxol-5-ylcarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
40.29% inhibition at 0.01 mg/ml
Nalpha-(1,3-benzodioxol-5-ylcarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
16.2% inhibition at 0.01 mg/ml
Nalpha-(2,4-dichlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
22.23% inhibition at 0.01 mg/ml
Nalpha-(2,4-dichlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
20.26% inhibition at 0.01 mg/ml
Nalpha-(3,4-dimethoxybenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
18.3% inhibition at 0.01 mg/ml
Nalpha-(3,5-dinitrobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
7.61% inhibition at 0.01 mg/ml
Nalpha-(3,5-dinitrobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
0.91% inhibition at 0.01 mg/ml
Nalpha-(3-chlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
25.66% inhibition at 0.01 mg/ml
Nalpha-(3-chlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
16.92% inhibition at 0.01 mg/ml
Nalpha-(tert-butoxycarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
30.06% inhibition at 0.01 mg/ml
Nalpha-(tert-butoxycarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
25.76% inhibition at 0.01 mg/ml
Nalpha-benzoyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
11.2% inhibition at 0.01 mg/ml
NB-216
-
-
NB-544
-
-
OM00-3
OM99-2
pepstatin A
-
less potent inhibitor
phlorofurofucoeckol-A
-
significant BACE1 inhibition in a dose-dependent manner
phloroglucinol
-
significant BACE1 inhibition in a dose-dependent manner
pyridin-3-ylmethyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
-
-
pyridin-4-ylmethyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
-
-
quercetin
rebaichromone
-
-
reticulon 3
-
-
-
reticulon 4
-
-
-
rosmarinic acid
S-(tetrahydrofuran-3-yl) [(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]carbamothioate
-
-
salvianolic acid A
competitive type inhibition
salvianolic acid B
-
salvianolic acid C
mixed-type inhibition
tanshinol B
-
tanshinonal
-
tanshinone I
-
tanshinone IIA
-
tanshinone IIB
-
tert-butyl 5-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
-
-
tert-butyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-methyl-1,4-dihydropyridine-3-carboxylate
-
-
tert-butyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
-
-
tert-butyl [(2S)-1-[[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamate
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50.53% inhibition at 0.01 mg/ml
tert-butyl [(2S)-3-[[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-([(2S)-3-methyl-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-8-oxooctan-4-yl]amino]-3-oxo-2-[[(3aR,6aS)-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazol-3-ylcarbonyl]amino]propyl]carbamate
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tert-butyl [(2S)-3-[[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-([(2S)-3-methyl-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-8-oxooctan-4-yl]amino]-3-oxo-2-[[(3aS,6aR)-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazol-3-ylcarbonyl]amino]propyl]carbamate
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trans-4-[(13S)-15-amino-13-cyclohexyl-11-oxo-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-10-yl]cyclohexanecarboxylic acid
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triphloroethol A
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significant BACE1 inhibition in a dose-dependent manner
Z-DEVD-FMK
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caspase-3 inhibitor Z-DEVD-FMK reduces BACE1 mRNA and protein levels, and inhibits its protease activity, thereby decreasing the amount of amyloid precursor protein C99 and beta-amyloid in ischemic brains
[(1R,2R,4R,5S,6S)-2-hydroxy-7-sulfo-4-[(sulfooxy)methyl]-3-oxa-7-azabicyclo[4.1.0]hept-5-yl 2-O-sulfo-beta-D-glucopyranosiduronic acid]n
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IC50: 0.000031 mg/ml
[(1R,4S,5R,7R)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl](morpholin-4-yl)methanone
61% inhibition at 0.01 mM
[(1R,5R,7R)-3-benzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl](morpholin-4-yl)methanone
15% inhibition at 0.01 mM
[(1S,4R,5S,7S)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl](morpholin-4-yl)methanone
5% inhibition at 0.01 mM
[(1S,5S,6S)-3-amino-5-(2-fluoro-5-[(Z)-2-fluoro-2-[5-(prop-2-yn-1-yloxy)pyrazin-2-yl]ethenyl]phenyl)-5-methyl-2-thia-4-azabicyclo[4.1.0]hept-3-en-1-yl][(3R)-3-methylmorpholin-4-yl]methanone
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[(2R,4S,5S)-5-[N-(3,4-dimethoxy)benzoyl-L-phenylalanylamido]-4-hydroxy-2,7-dimethyloctan] N'-isobutyl amide
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14.66% inhibition at 0.01 mg/ml
[2-(acetylamino)-2-deoxy-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
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IC50: 0.00041 mg/ml
[2-(acetylamino)-2-deoxy-4-O-beta-D-glucopyranuronosyl-6-O-sulfo-beta-D-glucopyranose]n
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IC50: 0.000091 mg/ml
[2-(acetylamino)-2-deoxy-6-O-sulfo-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
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IC50: 0.000031 mg/ml
[2-amino-2-deoxy-6-O-sulfo-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
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IC50: 0.000159 mg/ml
[2-deoxy-2-(butanoylamino)-6-O-sulfo-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
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IC50: 0.000055 mg/ml
[2-deoxy-2-(propanoylamino)-6-O-sulfo-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
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IC50: 0.000053 mg/ml
[2-deoxy-2-(sulfoamino)-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
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IC50: 0.0001 mg/ml
[2-deoxy-4-O-(2,3-di-O-sulfo-beta-D-glucopyranuronosyl)-6-O-sulfo-2-(sulfoamino)-beta-D-glucopyranose]n
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IC50: 0.000053 mg/ml
[2-deoxy-6-O-sulfo-2-(sulfoamino)-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
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porcine mucosal intestinal heparin, IC50: 0.000028 mg/ml
[3-([1-benzyl-2-hydroxy-3-[(1-methylethyl)amino]propyl]carbamoyl)-5-[(1-phenylethyl)carbamoyl]phenyl]methylsulfamic acid
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[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
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[3-[(1-[1-hydroxy-2-[(3-methoxybenzyl)amino]ethyl]-3-methylbutyl)carbamoyl]-5-[(1-phenylethyl)carbamoyl]phenyl]methylsulfamic acid
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additional information
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