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Cathepsin D Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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PepstatinIC501.0 [1]
PepstatinKi0.01 [1]
Grassystatin AIC5040.0 [1]
Hydroxyethylamine-based inhibitor 3Ki63.0 [1]
Statine-like inhibitor AIC5021.0 [1]
Statine-like inhibitor AKi21.0 [1]
Methyl (2S)-1-[(2R)-2-[[(2S)-2-[[(2S,3S)-2-[[(3S,4S)-4-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[(2S)-2-(dimethylamino)-3-phenylpropanoyl]oxypropanoyl]amino]-4-methylpentanoyl]-methylamino]-5-oxopentanoyl]amino]-3-hydroxy-6-methylheptanoyl]amino]-3-methylpentanoyl]amino]propanoyl]-methylamino]-3-phenylpropanoyl]pyrrolidine-2-carboxylateIC505.5 [1], 50.0 [2], 100.0 [3], 10000.0 [4]
(5Z)-5-[[4-[(4-Benzoyl-3-hydroxy-2-propylphenoxy)methyl]phenyl]methylidene]-2-sulfanylidene-1,3-thiazolidin-4-oneIC50210.0 [1], 340.0 [2], 1300.0 [3]
2-Bromo-N-[(2S,3S)-4-[2-(2,4-dichlorophenyl)ethyl-[3-(1,3-dioxoisoindol-2-yl)propanoyl]amino]-3-hydroxy-1-(3-phenoxyphenyl)butan-2-yl]-4,5-dimethoxybenzamideIC500.7 [1], 85.0 [2]
2-Bromo-N-[(2S,3S)-4-[2-(2,4-dichlorophenyl)ethyl-[3-(1,3-dioxoisoindol-2-yl)propanoyl]amino]-3-hydroxy-1-(3-phenoxyphenyl)butan-2-yl]-4,5-dimethoxybenzamideKi0.07 [1]
N-[(2S,3R)-4-[[1-(3-Tert-butylphenyl)cyclohexyl]amino]-1-(3,5-difluorophenyl)-3-hydroxybutan-2-yl]acetamideIC5024.0 [1], 25.0 [2]
3-(1,1-Dioxothiazinan-2-yl)-5-(ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]benzamideIC503570.0 [1], 3900.0 [2], 6760.0 [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-carboxamideIC507930.0 [1], 7933.0 [2]
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)benzamideIC502695.0 [1]
Hydroxyethylamine-based inhibitor 2IC50320.0 [1]
Hydroxyethylamine-based inhibitor 2Ki320.0 [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-carboxamideIC501259.0 [1], 1260.0 [2]
Methyl (2S)-1-[(2R)-2-[[(2S)-2-[[(2S,3S)-2-[[(3S,4S)-4-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-hydroxypropanoyl]amino]-4-methylpentanoyl]-methylamino]-5-oxopentanoyl]amino]-3-hydroxy-6-methylheptanoyl]amino]-3-methylpentanoyl]amino]propanoyl]-methylamino]-3-phenylpropanoyl]pyrrolidine-2-carboxylateIC50100.0 [1], 2000.0 [2], 5500.0 [3]
(4R,4Ar,6R,8aS)-8a-(2,4-difluorophenyl)-4-methyl-6-(3-methyl-1,2-oxazol-5-yl)-4a,5,6,8-tetrahydro-4H-pyrano[3,4-d][1,3]thiazin-2-amineIC50140.0 [1], 12000.0 [2], 14200.0 [3]
Bace-1 inhibitorIC507620.0 [1]
Bace-1 inhibitorKi448.0 [1]
(2e)-2-Imino-3-Methyl-5,5-Diphenylimidazolidin-4-OneIC50100000.0 [1]
N-[Amino(imino)methyl]-2-(2,5-diphenyl-1H-pyrrol-1-yl)acetamideIC5060000.0 [1]
8,8-Diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amineIC50100000.0 [1]
Statine deriv. 47IC50380.0 [1]
2-Amino-4-(4-methoxy-3-methylphenyl)-1-methyl-4-(3-(pyridin-3-yl)phenyl)-1H-imidazol-5(4H)-oneIC5012500.0 [1]
N-Carbamimidoyl-2-[2-(2-Chlorophenyl)-5-[4-(4-Ethanoylphenoxy)phenyl]pyrrol-1-Yl]ethanamideIC508200.0 [1], 18900.0 [2]
2-Amino-4-(biphenyl-3-yl)-1-methyl-4-(pyridin-4-yl)-1H-imidazol-5(4H)-oneIC5030000.0 [1], 30100.0 [2]
N-[(2S,3R)-1-(3,5-Difluorophenyl)-3-hydroxy-4-[[1-(3-pyrazol-1-ylphenyl)cyclohexyl]amino]butan-2-yl]acetamideIC5022.0 [1]
2-Amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methylimidazol-4-oneIC502580.0 [1], 2600.0 [2]
Statine-like inhibitor 16Ki4.9 [1]
N-[(2S,3R)-4-[[4-(3-Tert-butylphenyl)oxan-4-yl]amino]-1-(3,5-difluorophenyl)-3-hydroxybutan-2-yl]acetamideIC50230.0 [1]
3-(Ethylamino)-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)phenyl]methylamino]butan-2-yl]-5-(2-oxopyrrolidin-1-yl)benzamideIC505750.0 [1], 6580.0 [2]
3,5-Dichloro-2-[(3,5-dichloro-2-hydroxyphenyl)sulfonylamino]-N-[4-[(6-ethoxy-1,3-benzothiazol-2-yl)sulfanyl]phenyl]benzamideIC50250.0 [1]
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-dicarboxamideKi36.0 [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-dicarboxamideKi291.0 [1]
2-[2-(1-Adamantyl)-5-phenylpyrrol-1-yl]-N-[N'-(3-hydroxypropyl)carbamimidoyl]acetamideIC5019400.0 [1], 19900.0 [2]
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-carboxamideIC5060.0 [1], 6610.0 [2]
2-Amino-7-(4-pentylphenyl)-3-[[(2S,5R)-5-phenyloxolan-2-yl]methyl]quinazolin-4-oneIC505000.0 [1]
2-Amino-3-[[(2S,5R)-5-phenyloxolan-2-yl]methyl]-7-[4-(3-phenylpropyl)phenyl]quinazolin-4-oneIC506000.0 [1]
N-[2-(1,3-Benzodioxol-5-yl)ethyl]-N-[(2S,3S)-3-[[2-(2,4-dichlorophenoxy)acetyl]amino]-2-hydroxy-4-phenylbutyl]-3-(1,3-dioxoisoindol-2-yl)propanamideKi3.0 [1], 9.0 [2]
N-[2-(2-Adamantan-1-yl-5-phenyl-pyrrol-1-yl)-acetyl]-guanidineIC5025000.0 [1], 30200.0 [2]
(2R,4S,5S)-5-[[(2S)-2-[[(2S)-2-Acetamido-4-methylpentanoyl]amino]propanoyl]amino]-N-butyl-4-hydroxy-2,7-dimethyloctanamideIC50260.0 [1]
(2r,4s,5s)-N-Butyl-4-Hydroxy-2,7-Dimethyl-5-{[n-(4-Methylpentanoyl)-L-Methionyl]amino}octanamideIC50370.0 [1]
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]benzamideIC501070.0 [1]
(2R,4S)-N-Butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,16-dioxo-1,4-diazacyclohexadec-5-yl]-4-hydroxy-2-methylbutanamideIC501700.0 [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-carboxamideIC50890.0 [1]
N-[(2S,3S)-1-[[5-(Butylamino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]-4-(pyrrolidin-1-ylmethyl)benzamideIC501200.0 [1]
N-[(2S,3S)-1-[[5-(Butylamino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]-4-(pyrrolidin-1-ylmethyl)benzamideKi1200.0 [1]
N-[1-[[3-Hydroxy-6-methyl-1-oxo-1-(3-phenylpropylamino)heptan-4-yl]amino]-3-methyl-1-oxopentan-2-yl]-4-(methylaminomethyl)benzamideKi1300.0 [1]
N-[(2S,3R)-4-[[(2S)-1-(Cyclohexylamino)-1-oxopropan-2-yl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-methylsulfonylbenzamideIC507700.0 [1]
N-[(2S,3R)-4-[[(2S)-1-(Cyclohexylamino)-1-oxopropan-2-yl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2-oxopyrrolidin-1-yl)benzamideIC5025630.0 [1], 26000.0 [2]
N-[(2S,3R)-4-[[1-(3-Tert-butylphenyl)cyclopropyl]amino]-1-(3,5-difluorophenyl)-3-hydroxybutan-2-yl]acetamideIC50220.0 [1], 290.0 [2]
N-[(2S,3R)-1-(3,5-Difluorophenyl)-4-[[1-[1-(2,2-dimethylpropyl)pyrazol-4-yl]cyclopropyl]amino]-3-hydroxybutan-2-yl]acetamideIC50720.0 [1]
N-[(2S,3R)-4-[[1-(6-Tert-butylpyrimidin-4-yl)cyclohexyl]amino]-1-(3,5-difluorophenyl)-3-hydroxybutan-2-yl]acetamideIC50245.0 [1], 250.0 [2]
(3S,4S,5R)-3-[[4-Amino-3-fluoro-5-(1,1,1,3,3,3-hexafluoropropan-2-yloxy)phenyl]methyl]-5-[(3-tert-butylphenyl)methylamino]-1,1-dioxothian-4-olIC50450.0 [1]
Statine-like inhibitor 24Ki473.0 [1]
Statine-like inhibitor 27Ki4000.0 [1]
Statine-like inhibitor 33Ki5900.0 [1]
Statine-like inhibitor 34Ki5900.0 [1]
(2R,3R,4R,5R)-3,4-Dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-enoxy)hexanediamideKi2000.0 [1]
(2R,3R,4R,5R)-2,5-Bis[(E)-3-bromoprop-2-enoxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamideKi2000.0 [1]
Methyl (2S)-1-[(2R)-2-[[(2S)-2-[[(2S)-2-[[(3S,4S)-4-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-hydroxypropanoyl]amino]-3-methylbutanoyl]-methylamino]-5-oxopentanoyl]amino]-3-hydroxy-5-phenylpentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]-methylamino]-3-phenylpropanoyl]pyrrolidine-2-carboxylateIC5050.0 [1], 182.0 [2]
(4Ar,6S,8aS)-8a-(2,4-difluorophenyl)-6-methyl-4a,5,6,8-tetrahydro-4H-pyrano[3,4-d][1,3]thiazin-2-amineIC5072000.0 [1]
5-[4-(4-Benzoyl-3-hydroxy-2-propyl-benzyloxy)-benzylidene]-2-thioxo-thiazolidin-4-oneIC50210.0 [1]
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-carboxamideIC50660.0 [1], 1000.0 [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-carboxamideIC50660.0 [1], 1000.0 [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-carboxamideIC5058880.0 [1]
N-[(2S,3R)-4-(Benzylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-(1,1-dioxothiazinan-2-yl)-5-(ethylamino)benzamideIC5026300.0 [1]
N-[(2S,3R)-4-(Cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-3-(1,1-dioxothiazinan-2-yl)-5-(ethylamino)benzamideIC5030200.0 [1]
N-[(2S,3R)-4-[[1-(3-Tert-butylphenyl)-4-hydroxycyclohexyl]amino]-1-(3,5-difluorophenyl)-3-hydroxybutan-2-yl]acetamideIC501400.0 [1], 10000.0 [2]
N-[(2S,3R)-4-[[(4S)-6-(2,2-Dimethylpropyl)-3'-hydroxyspiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-1-(4-fluorophenyl)-3-hydroxybutan-2-yl]acetamideIC50577.0 [1], 1650.0 [2]
N-[(2S,3R)-4-[[(4S)-6-(2,2-Dimethylpropyl)-3'-methylspiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-1-(4-fluorophenyl)-3-hydroxybutan-2-yl]acetamideIC508.0 [1], 38.0 [2]
N-[(2S,3R)-4-[[(4S)-6-(2,2-Dimethylpropyl)-3'-fluorospiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-1-(3-fluorophenyl)-3-hydroxybutan-2-yl]acetamideIC5012.0 [1], 22.0 [2]
N-[(2S,3R)-1-(3,4-Difluorophenyl)-4-[[(4S)-6-(2,2-dimethylpropyl)-3'-methylspiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-3-hydroxybutan-2-yl]acetamideIC504.0 [1], 17.0 [2]
N-[(2S,3R)-4-[[(4S)-6-(2,2-Dimethylpropyl)-3'-fluorospiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-1-(4-fluorophenyl)-3-hydroxybutan-2-yl]acetamideIC508.0 [1], 14.0 [2]
ResveratrolIC50138000.0 [1]
Ursolic acidIC5018200.0 [1]
AmprenavirIC5015200.0 [1]
NafamostatIC501000000.0 [1]
PiperineIC5042300.0 [1]
TipranavirKi15000.0 [1]
CID 11199915IC50100000.0 [1]
(2S)-1-[(2S,3S)-3-Methyl-2-[[(2S,3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylic acidIC50100000.0 [1]
EVNLPsiAAEFIC506.0 [1]
VerubecestatIC50100000.0 [1]
(2R,3R,4R,5S)-6-Cyclohexyl-3,4-dihydroxy-5-[[(2S)-3-(1H-imidazol-5-yl)-2-[(2-naphthalen-1-yloxyacetyl)amino]propanoyl]amino]-N-[(2S,3S)-3-methyl-1-oxo-1-(pyridin-2-ylmethylamino)pentan-2-yl]-2-propan-2-ylhexanamideKi1000.0 [1]
(S)-4-(2,4-Difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amineIC5015700.0 [1]
BalicatibKi1.29 [1]
LanabecestatIC5016100.0 [1]
N1,N6-Di[(1S)-indanyl-(2R)-hydroxy]-(2R,3R,4R,5R)-2,5-di(benzyloxy)-3,4-dihydroxyhexanediamideKi2000.0 [1]
Methyl N-[(2S)-1-[[(5S)-5-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-6-hydroxyhexyl]amino]-1-oxo-3,3-diphenylpropan-2-yl]carbamateIC5050000.0 [1]
CID 66665322IC50250000.0 [1]
beta-SitosteroneIC509400.0 [1]
Unii-1NE31CW68SIC5010000.0 [1]
Aliskiren hydrochlorideIC5010000.0 [1]
Tasiamide BIC50251.0 [1]
Unii-114L0XB8FMKi4300.0 [1]
CID 118253852IC5020000.0 [1]
Statine deriv. 50IC501000.0 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Cathepsin D Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/cathepsin-d-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 21). Quest Database™ Cathepsin D Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/cathepsin-d-inhibitors-ic50-ki.
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