| 8,8-Diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine | IC50 | 38000.0 [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-carboxamide | IC50 | 3.3 [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-carboxamide | Ki | 0.22 [1] |
| Verubecestat | IC50 | 0.38 [1] |
| Verubecestat | Ki | 0.37 [1], 0.47 [2] |
| (2e)-2-Imino-3-Methyl-5,5-Diphenylimidazolidin-4-One | IC50 | 770.0 [1] |
| 3-(1,1-Dioxothiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]benzamide | IC50 | 1160.0 [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-carboxamide | IC50 | 263.0 [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)benzamide | IC50 | 1810.0 [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-carboxamide | IC50 | 59.0 [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-carboxamide | IC50 | 10.2 [1], 17.8 [2], 42.9 [3] |
| Bace-1 inhibitor | IC50 | 132.0 [1] |
| Bace-1 inhibitor | Ki | 240.0 [1] |
| Lanabecestat | IC50 | 0.9 [1] |
| Lanabecestat | Ki | 372.0 [1] |
| N-[Amino(imino)methyl]-2-(2,5-diphenyl-1H-pyrrol-1-yl)acetamide | IC50 | 50000.0 [1] |
| 2-Amino-4-(4-methoxy-3-methylphenyl)-1-methyl-4-(3-(pyridin-3-yl)phenyl)-1H-imidazol-5(4H)-one | IC50 | 780.0 [1], 790.0 [2] |
| N-Carbamimidoyl-2-[2-(2-Chlorophenyl)-5-[4-(4-Ethanoylphenoxy)phenyl]pyrrol-1-Yl]ethanamide | IC50 | 2300.0 [1], 3200.0 [2] |
| 2-Amino-1-methyl-4-(3-(pyridin-3-yl)phenyl)-4-(pyridin-4-yl)-1H-imidazol-5(4H)-one | IC50 | 480.0 [1] |
| 2-Amino-1-methyl-4-phenyl-4-(pyridin-4-yl)-1H-imidazol-5(4H)-one | IC50 | 2010.0 [1] |
| 2-Amino-4-(biphenyl-3-yl)-1-methyl-4-(pyridin-4-yl)-1H-imidazol-5(4H)-one | IC50 | 140.0 [1] |
| 2-Amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methylimidazol-4-one | IC50 | 780.0 [1] |
| (1S)-1-(2-(Difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine | IC50 | 0.9 [1] |
| (1S)-1-(2-(Difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine | Ki | 370.0 [1] |
| 3-(Ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]-5-(2-oxopyrrolidin-1-yl)benzamide | IC50 | 4070.0 [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-dicarboxamide | IC50 | 45.0 [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-dicarboxamide | IC50 | 54.0 [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-carboxamide | IC50 | 210.0 [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]benzamide | IC50 | 2950.0 [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-carboxamide | IC50 | 28.0 [1] |
| N-[(2S,3R)-4-[[(2S)-1-(Cyclohexylamino)-1-oxopropan-2-yl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-methylsulfonylbenzamide | IC50 | 41770.0 [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)benzamide | IC50 | 78530.0 [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-carboxamide | IC50 | 114.0 [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-carboxamide | IC50 | 110.0 [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-carboxamide | IC50 | 1260.0 [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-carboxamide | IC50 | 194.0 [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-carboxamide | IC50 | 20.0 [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-carboxamide | IC50 | 57.0 [1], 70.5 [2] |
| N-[(2S,3R)-4-(Benzylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-(1,1-dioxothiazinan-2-yl)-5-(ethylamino)benzamide | IC50 | 32360.0 [1] |
| N-[(2S,3R)-4-(Cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-(1,1-dioxothiazinan-2-yl)-5-(ethylamino)benzamide | IC50 | 19500.0 [1] |
| 6-Fluoro-2-[3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl]-1H-benzimidazole | IC50 | 3675.0 [1] |
| 6-Fluoro-2-[3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl]-1H-benzimidazole | Ki | 3568.0 [1] |
| 2-[4-(1H-Benzimidazol-2-yl)phenyl]-N-tert-butylimidazo[1,2-a]pyridin-3-amine | IC50 | 5675.0 [1] |
| 2-[4-(1H-Benzimidazol-2-yl)phenyl]-N-tert-butylimidazo[1,2-a]pyridin-3-amine | Ki | 5509.0 [1] |
| N-Tert-butyl-2-[4-(6-fluoro-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amine | IC50 | 3725.0 [1] |
| N-Tert-butyl-2-[4-(6-fluoro-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amine | Ki | 3617.0 [1] |
| N-Tert-butyl-2-[4-(6-methoxy-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amine | IC50 | 2895.0 [1] |
| N-Tert-butyl-2-[4-(6-methoxy-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amine | Ki | 2810.0 [1] |
| 2-[3-(1H-Benzimidazol-2-yl)phenyl]-N-tert-butylimidazo[1,2-a]pyridin-3-amine | IC50 | 3785.0 [1] |
| 2-[3-(1H-Benzimidazol-2-yl)phenyl]-N-tert-butylimidazo[1,2-a]pyridin-3-amine | Ki | 3674.0 [1] |
| N-Tert-butyl-2-[3-(6-fluoro-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amine | IC50 | 4234.0 [1] |
| N-Tert-butyl-2-[3-(6-fluoro-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amine | Ki | 4110.0 [1] |
| N-Tert-butyl-2-[3-(6-methoxy-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amine | IC50 | 4123.0 [1] |
| N-Tert-butyl-2-[3-(6-methoxy-1H-benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridin-3-amine | Ki | 4003.0 [1] |
| 2-[3-(1H-Benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridine | IC50 | 3890.0 [1] |
| 2-[3-(1H-Benzimidazol-2-yl)phenyl]imidazo[1,2-a]pyridine | Ki | 3777.0 [1] |
| 6-Fluoro-2-(3-imidazo[1,2-a]pyridin-2-ylphenyl)-1H-benzimidazole | IC50 | 3173.0 [1] |
| 6-Fluoro-2-(3-imidazo[1,2-a]pyridin-2-ylphenyl)-1H-benzimidazole | Ki | 3081.0 [1] |
| 2-(3-Imidazo[1,2-a]pyridin-2-ylphenyl)-6-methoxy-1H-benzimidazole | IC50 | 3321.0 [1] |
| 2-(3-Imidazo[1,2-a]pyridin-2-ylphenyl)-6-methoxy-1H-benzimidazole | Ki | 3224.0 [1] |
| 3-[5-(3-Methoxyphenyl)-1H-imidazol-2-yl]-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | IC50 | 2350.0 [1] |
| 3-[5-(3-Methoxyphenyl)-1H-imidazol-2-yl]-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | Ki | 2281.0 [1] |
| 3-[Methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]-5-(5-phenyl-1H-imidazol-2-yl)benzamide | IC50 | 1786.0 [1] |
| 3-[Methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]-5-(5-phenyl-1H-imidazol-2-yl)benzamide | Ki | 1733.0 [1] |
| 3-[5-(3-Fluorophenyl)-1H-imidazol-2-yl]-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | IC50 | 1873.0 [1] |
| 3-[5-(3-Fluorophenyl)-1H-imidazol-2-yl]-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | Ki | 1818.0 [1] |
| 3-(6-Methoxy-1H-benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | IC50 | 2425.0 [1] |
| 3-(6-Methoxy-1H-benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | Ki | 2354.0 [1] |
| 3-(6-Fluoro-1H-benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | IC50 | 2127.0 [1] |
| 3-(6-Fluoro-1H-benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | Ki | 2065.0 [1] |
| 3-(1H-Benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | IC50 | 2130.0 [1] |
| 3-(1H-Benzimidazol-2-yl)-5-[methyl(methylsulfonyl)amino]-N-[(1S)-1-phenylethyl]benzamide | Ki | 2067.0 [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-amine | Ki | 0.37 [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-carboxamide | IC50 | 4.0 [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-carboxamide | IC50 | 580.0 [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-carboxamide | IC50 | 71.0 [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-carboxamide | IC50 | 71.0 [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-carboxamide | Ki | 17.4 [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-carboxamide | IC50 | 290.0 [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-carboxamide | IC50 | 2900.0 [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-carboxamide | IC50 | 7.0 [1] |
| N-[6-[(4R)-2-Amino-5,5-difluoro-4-methyl-6H-1,3-oxazin-4-yl]-5-fluoropyridin-2-yl]-5-cyanopyridine-2-carboxamide | IC50 | 66.0 [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-amine | IC50 | 4550.0 [1] |
| N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-methylpyrazine-2-carboxamide | Ki | 4.85 [1] |
| N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-methylpyridine-2-carboxamide | Ki | 0.45 [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-carboxamide | Ki | 2.15 [1] |
| 5-[5-[(5S)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]thiophen-3-yl]-2-fluorobenzonitrile | Ki | 8.23 [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-carboxamide | Ki | 2.46 [1] |
| N-[3-[(5R)-3-Amino-2,5-dimethyl-1,1-dioxo-6H-1,2,4-thiadiazin-5-yl]-4-fluorophenyl]-5-methoxypyrazine-2-carboxamide | Ki | 1.99 [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-carboxamide | Ki | 1.7 [1], 3.8 [2] |
| (S)-4-(2,4-Difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine | IC50 | 2880.0 [1] |
| CID 66665322 | IC50 | 6.0 [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]carbamate | IC50 | 500.0 [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]benzamide | IC50 | 177.0 [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 acid | Ki | 3.0 [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-amine | IC50 | 5.0 [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]benzamide | IC50 | 620.0 [1] |
| [3-[2-(5-Aminopentylamino)-2-oxoethoxy]-5-[[(1R)-1-(4-fluorophenyl)ethyl]carbamoyl]phenyl] phenylmethanesulfonate | IC50 | 137000.0 [1] |
| Example 1 (WO2011029803) | IC50 | 9.0 [1] |
| Bace1-IN-1 | IC50 | 24.0 [1] |