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Beta secretase 2 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
8,8-Diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amineIC5038000.0 [1], 38300.0 [2]
N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-chloropyridine-2-carboxamideIC503.3 [1], 4.5 [2]
N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-chloropyridine-2-carboxamideKi0.22 [1]
VerubecestatIC500.38 [1]
VerubecestatKi0.37 [1], 0.47 [2]
(2e)-2-Imino-3-Methyl-5,5-Diphenylimidazolidin-4-OneIC50770.0 [1]
3-(1,1-Dioxothiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]benzamideIC501160.0 [1], 1430.0 [2], 4260.0 [3]
N-[(2S,3R)-4-(Cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-ethyl-9-methyl-10,10-dioxo-10lambda6-thia-1,9-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraene-6-carboxamideIC50263.0 [1]
N-[(2S,3R)-4-[[(2S)-1-(Cyclohexylamino)-1-oxopropan-2-yl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(ethylamino)-5-(2-oxopyrrolidin-1-yl)benzamideIC501810.0 [1]
3-Ethyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]-9-methyl-10,10-dioxo-10lambda6-thia-1,9-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraene-6-carboxamideIC5059.0 [1]
N-[3-[(4Ar,7aS)-2-amino-4a,5,6,7-tetrahydro-4H-cyclopenta[d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamideIC5010.2 [1], 17.8 [2], 42.9 [3]
Bace-1 inhibitorIC50132.0 [1]
Bace-1 inhibitorKi240.0 [1]
LanabecestatIC500.9 [1]
LanabecestatKi372.0 [1]
N-[Amino(imino)methyl]-2-(2,5-diphenyl-1H-pyrrol-1-yl)acetamideIC5050000.0 [1]
2-Amino-4-(4-methoxy-3-methylphenyl)-1-methyl-4-(3-(pyridin-3-yl)phenyl)-1H-imidazol-5(4H)-oneIC50780.0 [1], 790.0 [2]
N-Carbamimidoyl-2-[2-(2-Chlorophenyl)-5-[4-(4-Ethanoylphenoxy)phenyl]pyrrol-1-Yl]ethanamideIC502300.0 [1], 3200.0 [2]
2-Amino-1-methyl-4-(3-(pyridin-3-yl)phenyl)-4-(pyridin-4-yl)-1H-imidazol-5(4H)-oneIC50480.0 [1]
2-Amino-1-methyl-4-phenyl-4-(pyridin-4-yl)-1H-imidazol-5(4H)-oneIC502010.0 [1]
2-Amino-4-(biphenyl-3-yl)-1-methyl-4-(pyridin-4-yl)-1H-imidazol-5(4H)-oneIC50140.0 [1]
2-Amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methylimidazol-4-oneIC50780.0 [1]
(1S)-1-(2-(Difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amineIC500.9 [1]
(1S)-1-(2-(Difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amineKi370.0 [1]
3-(Ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]-5-(2-oxopyrrolidin-1-yl)benzamideIC504070.0 [1], 4485.0 [2]
1-N-[(1R,2S)-3-(3,5-Difluorophenyl)-1-hydroxy-1-[(2R,4R)-4-phenylmethoxypyrrolidin-2-yl]propan-2-yl]-5-methyl-3-N,3-N-dipropylbenzene-1,3-dicarboxamideIC5045.0 [1]
1-N-[(1R,2S)-3-(3,5-Difluorophenyl)-1-hydroxy-1-[(2R,4R)-4-phenoxypyrrolidin-2-yl]propan-2-yl]-5-methyl-3-N,3-N-dipropylbenzene-1,3-dicarboxamideIC5054.0 [1]
3-Ethyl-N-[(2S,3R)-3-hydroxy-4-(oxan-4-ylamino)-1-phenylbutan-2-yl]-9-methyl-10,10-dioxo-10lambda6-thia-1,9-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraene-6-carboxamideIC50210.0 [1], 490.0 [2]
3-(1,1-Dioxothiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-4-[(6-methoxy-2,3-dihydro-1H-inden-1-yl)amino]-1-phenylbutan-2-yl]benzamideIC502950.0 [1]
3-Ethyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-(3,3,3-trifluoropropylamino)butan-2-yl]-9-methyl-10,10-dioxo-10lambda6-thia-1,9-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraene-6-carboxamideIC5028.0 [1]
N-[(2S,3R)-4-[[(2S)-1-(Cyclohexylamino)-1-oxopropan-2-yl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-methylsulfonylbenzamideIC5041770.0 [1], 42000.0 [2]
N-[(2S,3R)-4-[[(2S)-1-(Cyclohexylamino)-1-oxopropan-2-yl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2-oxopyrrolidin-1-yl)benzamideIC5078530.0 [1], 79000.0 [2]
N-[(2S,3R)-4-(Cyclohexylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-ethyl-9-methyl-10,10-dioxo-10lambda6-thia-1,9-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraene-6-carboxamideIC50114.0 [1], 210.0 [2]
N-[(2S,3R)-4-(2,6-Dimethylheptan-2-ylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-ethyl-9-methyl-10,10-dioxo-10lambda6-thia-1,9-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraene-6-carboxamideIC50110.0 [1], 210.0 [2]
3-Ethyl-N-[(2S,3R)-3-hydroxy-4-(methylamino)-1-phenylbutan-2-yl]-9-methyl-10,10-dioxo-10lambda6-thia-1,9-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraene-6-carboxamideIC501260.0 [1]
N-[2-[(4Ar,6S,8aR)-2-amino-6-methyl-4a,5,6,8-tetrahydro-4H-pyrano[3,4-d][1,3]thiazin-8a-yl]-1,3-thiazol-4-yl]-5-(difluoromethoxy)pyridine-2-carboxamideIC50194.0 [1], 238.0 [2]
N-[2-[(4Ar,6S,8aR)-2-amino-6-methyl-4a,5,6,8-tetrahydro-4H-pyrano[3,4-d][1,3]thiazin-8a-yl]-1,3-thiazol-4-yl]-5-chloropyridine-2-carboxamideIC5020.0 [1], 21.6 [2]
N-[2-[(4Ar,6S,8aR)-2-amino-6-methyl-4a,5,6,8-tetrahydro-4H-pyrano[3,4-d][1,3]thiazin-8a-yl]-1,3-thiazol-4-yl]-5-(difluoromethoxy)-3-methylpyridine-2-carboxamideIC5057.0 [1], 70.5 [2]
N-[(2S,3R)-4-(Benzylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-(1,1-dioxothiazinan-2-yl)-5-(ethylamino)benzamideIC5032360.0 [1]
N-[(2S,3R)-4-(Cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-(1,1-dioxothiazinan-2-yl)-5-(ethylamino)benzamideIC5019500.0 [1]
6-Fluoro-2-[3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl]-1H-benzimidazoleIC503675.0 [1]
6-Fluoro-2-[3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl]-1H-benzimidazoleKi3568.0 [1]
2-[4-(1H-Benzimidazol-2-yl)phenyl]-N-tert-butylimidazo[1,2-a]pyridin-3-amineIC505675.0 [1]
2-[4-(1H-Benzimidazol-2-yl)phenyl]-N-tert-butylimidazo[1,2-a]pyridin-3-amineKi5509.0 [1]
N-Tert-butyl-2-[4-(6-fluoro-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amineIC503725.0 [1]
N-Tert-butyl-2-[4-(6-fluoro-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amineKi3617.0 [1]
N-Tert-butyl-2-[4-(6-methoxy-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amineIC502895.0 [1]
N-Tert-butyl-2-[4-(6-methoxy-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amineKi2810.0 [1]
2-[3-(1H-Benzimidazol-2-yl)phenyl]-N-tert-butylimidazo[1,2-a]pyridin-3-amineIC503785.0 [1]
2-[3-(1H-Benzimidazol-2-yl)phenyl]-N-tert-butylimidazo[1,2-a]pyridin-3-amineKi3674.0 [1]
N-Tert-butyl-2-[3-(6-fluoro-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amineIC504234.0 [1]
N-Tert-butyl-2-[3-(6-fluoro-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amineKi4110.0 [1]
N-Tert-butyl-2-[3-(6-methoxy-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amineIC504123.0 [1]
N-Tert-butyl-2-[3-(6-methoxy-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amineKi4003.0 [1]
2-[3-(1H-Benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridineIC503890.0 [1]
2-[3-(1H-Benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridineKi3777.0 [1]
6-Fluoro-2-(3-imidazo[1,2-a]pyridin-2-ylphenyl)-1H-benzimidazoleIC503173.0 [1]
6-Fluoro-2-(3-imidazo[1,2-a]pyridin-2-ylphenyl)-1H-benzimidazoleKi3081.0 [1]
2-(3-Imidazo[1,2-a]pyridin-2-ylphenyl)-6-methoxy-1H-benzimidazoleIC503321.0 [1]
2-(3-Imidazo[1,2-a]pyridin-2-ylphenyl)-6-methoxy-1H-benzimidazoleKi3224.0 [1]
3-[5-(3-Methoxyphenyl)-1H-imidazol-2-yl]-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideIC502350.0 [1]
3-[5-(3-Methoxyphenyl)-1H-imidazol-2-yl]-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideKi2281.0 [1]
3-[Methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]-5-(5-phenyl-1H-imidazol-2-yl)benzamideIC501786.0 [1]
3-[Methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]-5-(5-phenyl-1H-imidazol-2-yl)benzamideKi1733.0 [1]
3-[5-(3-Fluorophenyl)-1H-imidazol-2-yl]-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideIC501873.0 [1]
3-[5-(3-Fluorophenyl)-1H-imidazol-2-yl]-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideKi1818.0 [1]
3-(6-Methoxy-1H-benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideIC502425.0 [1]
3-(6-Methoxy-1H-benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideKi2354.0 [1]
3-(6-Fluoro-1H-benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideIC502127.0 [1]
3-(6-Fluoro-1H-benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideKi2065.0 [1]
3-(1H-Benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideIC502130.0 [1]
3-(1H-Benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamideKi2067.0 [1]
(5S)-5-[3-Chloro-5-(5-prop-1-ynylpyridin-3-yl)thiophen-2-yl]-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-3-amineKi0.37 [1]
N-[6-[(4R)-2-Amino-5,5-difluoro-4-methyl-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-3,5-dichloropyridine-2-carboxamideIC504.0 [1]
N-[6-[(4R)-2-Amino-5,5-difluoro-4-(2-methoxyethyl)-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-5-cyano-3-methylpyridine-2-carboxamideIC50580.0 [1]
N-[6-[(4R)-2-Amino-5,5-difluoro-4,6,6-trimethyl-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-3-chloro-5-cyanopyridine-2-carboxamideIC5071.0 [1], 140.0 [2]
N-[6-[(4R)-2-Amino-5,5-difluoro-4-methyl-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-3-chloro-5-cyanopyridine-2-carboxamideIC5071.0 [1]
N-[3-[(4As,7aS)-3-amino-2-methyl-1,1-dioxo-7,7a-dihydro-5H-furo[3,4-e][1,2,4]thiadiazin-4a-yl]-4-fluorophenyl]-5-(difluoromethyl)pyrazine-2-carboxamideKi17.4 [1]
N-[6-[(4R)-2-Amino-5,5-difluoro-4-methyl-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-3-chloro-5-(trifluoromethyl)pyridine-2-carboxamideIC50290.0 [1]
3-Amino-N-[6-[(4R)-2-amino-5,5-difluoro-4-methyl-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-5-(2,2-difluoroethoxy)pyrazine-2-carboxamideIC502900.0 [1]
N-[6-[(4R)-2-Amino-5,5-difluoro-4-methyl-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-4-chloro-1-(difluoromethyl)pyrazole-3-carboxamideIC507.0 [1]
N-[6-[(4R)-2-Amino-5,5-difluoro-4-methyl-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamideIC5066.0 [1], 260.0 [2]
(6R,8As)-8a-(2,4-difluorophenyl)-6-(3-methyl-1,2-oxazol-5-yl)-4a,5,6,8-tetrahydro-4H-pyrano[3,4-d][1,3]thiazin-2-amineIC504550.0 [1]
N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-methylpyrazine-2-carboxamideKi4.85 [1]
N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-methylpyridine-2-carboxamideKi0.45 [1]
N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4,5-difluorophenyl]-5-methoxypyrazine-2-carboxamideKi2.15 [1]
5-[5-[(5S)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]thiophen-3-yl]-2-fluorobenzonitrileKi8.23 [1]
N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-(trifluoromethyl)pyridine-2-carboxamideKi2.46 [1]
N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-methoxypyrazine-2-carboxamideKi1.99 [1]
N-[3-[(7R)-9-Amino-2-hydroxy-7-methyl-5,5-dioxo-5lambda6-thia-8-azaspiro[3.5]non-8-en-7-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamideKi1.7 [1], 3.8 [2]
(S)-4-(2,4-Difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amineIC502880.0 [1]
CID 66665322IC506.0 [1]
Tert-butyl N-[(2S)-1-[[(2S)-1-[[(4S,5S,7R)-8-[[(2S)-1-(benzylamino)-3-methyl-1-oxobutan-2-yl]amino]-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamateIC50500.0 [1]
3-(1,1-Dioxothiazinan-2-yl)-5-(ethylamino)-2-fluoro-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]benzamideIC50177.0 [1]
(4S)-4-Amino-5-[[(2S)-1-[[(2S)-3-carboxy-1-[[(4S,5S,7R)-8-[[(2S)-1-[[(2S)-4-carboxy-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acidKi3.0 [1]
(4S)-7'-(2-Fluoropyridin-3-yl)-3'-[2-(3-methyloxetan-3-yl)ethynyl]spiro[5H-1,3-oxazole-4,5'-chromeno[2,3-b]pyridine]-2-amineIC505.0 [1]
3-[5-[(2R)-2-Amino-1-phenylpropan-2-yl]-1,3,4-oxadiazol-2-yl]-N-[(1R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]benzamideIC50620.0 [1]
[3-[2-(5-Aminopentylamino)-2-oxoethoxy]-5-[[(1R)-1-(4-fluorophenyl)ethyl]carbamoyl]phenyl] phenylmethanesulfonateIC50137000.0 [1]
Example 1 (WO2011029803)IC509.0 [1]
Bace1-IN-1IC5024.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Beta secretase 2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/beta-secretase-2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Beta secretase 2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/beta-secretase-2-inhibitors-ic50-ki.
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