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(1S,2aR,3aR,3bS,4R,9aR,11aS)-2-(((1-(2-cyanophenyl)-1H-1,2,3-triazol-4-yl)methoxy)imino)-1-(furan-3-yl)-3b,6,6,9a,11a-pentamethyl-7-oxo-1,2,2a,3b,4,5,5a,6,7,9a,9b,10,11,11a-tetradecahydronaphtho(1,2':6,7)indeno(1,7a-b)oxiren-4-yl acetate
most active compound
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxyindan-1-yl)-butyramide
-
0.005 mM, 48% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 35% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
0.005 mM, 98% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 85% of maximal activity
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 25% inhibition
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 36% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 35% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 44% inhibition
(2R,3R)-4-[N-benzyl-N'-((S)-2-benzyloxycarbonylamino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 48% inhibition
(2R,3R)-4-[N-benzyl-N'-((S)-2-tert-butyloxycarbonyl-amino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxy-indan-1-yl)-butyramide
-
0.005 mM, 57% inhibition
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
-
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
-
-
(2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(1,3-benzodioxol-5-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-6-[2-[(4-tert-butylphenyl)carbonyl]hydrazino]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-N'1,N'6-bis[(4-tert-butylphenyl)carbonyl]-3,4-dihydroxyhexanedihydrazide
-
-
(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-en-1-yloxy)hexanediamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,4-dimethoxy-3,5-pyrimidin)-2-propenyl-oxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,5-dimethyl-3,4-oxazol)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3,4-methylenedioxyphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3-thienyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-acetylphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-fluorophenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-tolyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-bromo-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-phenyl-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-phenyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-trimethylsilyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-(methoxycarbonyl)-pent-2,4-dienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-phenyl-pentadienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 55% inhibition
(2S,3S)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 57% inhibition
(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
-
-
(2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-3-hydroxy-4-(2-thiophen-2-ylacetylamino)pentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-4-(3,3-diphenylpropionylamino)-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-4-diphenylacetylamino-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(4R)-3-[(2S,3S)-3-{[(2,6-dimethylphenoxy)acetyl]amino}-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
i.e. KNI-10006, crystallization data
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-([N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl]amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide
-
-
(5E)-5-[[2,5-dimethyl-1-(4-methylphenyl)-1H-pyrrol-3-yl]methylidene]-2,6-dihydroxypyrimidin-4(5H)-one
-
(5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
-
(5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
-
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-propyl)amide
-
-
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
-
1-[2-hydroxy-3-(1,2,3,4,5,6,7,8-octahydrophenanthren-9-yloxy)propyl]-4-(3-methoxyphenyl)piperazin-1-ium
-
-
17-benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16-tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
-
2,3-difluoro-4-methyl-N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]benzamide
-
-
2,5-Bis-allyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
2,5-Bis-benzyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
3'-(((1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-ylamino)methyl)biphenyl-2-ol
-
-
3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl 3,4-di-O-acetyl-2,6-dideoxyhexopyranoside
-
-
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
-
-
4-(1,3-benzodioxol-5-yl)-Nalpha-[(2S,3S)-2-hydroxy-3-([N-[3-(1H-indol-3-yl)propanoyl]-L-valyl]amino)-4-phenylbutyl]-L-phenylalaninamide
-
-
4-(1-benzofuran-2-yl)-Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
5-[bis[(benzyloxy)carbonyl]amino]-6-[[1-hydrazinyl-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-oxohexan-1-aminium
-
-
benzo[1,3]dioxole-5-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-amide
-
-
benzyl 2-benzyl-2-[(2S,3R)-3-[(4-bromobenzyl)oxy]-2-hydroxy-4-oxo-4-[(2-piperidin-1-ylethyl)amino]butyl]hydrazinecarboxylate
-
-
benzyl 3-benzyl-4-([2-[(1-formyl-3-methylbutyl)amino]-2-oxo-1-phenylethyl]amino)-4-oxobutanoate
-
-
benzyl [(1S,4S,5R,6R,7S,10S)-4,7-bis[(4-cyanophenoxy)methyl]-5,6-dihydroxy-1,10-bis(1-methylethyl)-2,9,12-trioxo-14-phenyl-13-oxa-3,8,11-triazatetradec-1-yl]carbamate
-
-
isovaleryl-pepstatin
-
-
-
Iva-Val-Val-Sta-Ala-Sta
-
-
KNI-10333
-
nanomolar inhibition activity
KNI-10743
-
nanomolar inhibition activity
KPFEL-PSI(CH2-NH)-AWT
combinatorial chemistry derived peptide inhibitor
KPFSL-PSI(CH2-NH)-LQF
combinatorial chemistry derived peptide inhibitor, 5fold selectivity over human cathepsin D
KPLEF-PSI(CH2-NH)-FRV
combinatorial chemistry derived peptide inhibitor
KPLEF-PSI(CH2-NH)-YRV
combinatorial chemistry derived peptide inhibitor
KPnorLSnorL-PSI(CH2-NH)-LQI
combinatorial chemistry derived peptide inhibitor
KPVEF-PSI(CH2-NH)-RQT
combinatorial chemistry derived peptide inhibitor
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
-
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
-
-
N-((1S,2S)-1-(4-benzo[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamid
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
-
-
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
-
-
N-butyl-N-[2-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-hydroxyethyl]butan-1-aminium
-
-
N-hexyl-N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]hexan-1-aminium
-
-
N-hexyl-N-[2-hydroxy-2-(phenanthren-9-yl)ethyl]hexan-1-aminium
-
-
N-[(1S)-1-([(1S,2S)-3-[(2-amino-2-oxoethyl)(benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl)-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-([[4-(1,3-benzodioxol-5-yl)benzyl]oxy]methyl)-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-benzyl-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-([(1S)-2-amino-1-[(4'-methylbiphenyl-4-yl)methyl]-2-oxoethyl]amino)-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-3-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl](benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-cyclo-hexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-3-cyclohexylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butyl-carbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
N-[(3S)-3-[(2S,5S,14S)-14-[(3,3-dimethylbutanoyl)amino]-2-(1-methylethyl)-3,11,15-trioxo-1,4,10-triazacyclopentadecan-5-yl]-3-hydroxypropanoyl]-L-valyl-L-leucylglycinamide
-
-
N-[(3S,4S)-3-hydroxy-6-phenyl-4-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]hexanoyl]-L-alanyl-L-leucinamide
-
-
N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentyl-N-[4-[(pyridin-3-ylmethyl)carbamoyl]benzyl]benzamide
-
-
N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentyl-N-[[4'-(piperidin-1-ylcarbonyl)biphenyl-4-yl]methyl]pyridine-2-carboxamide
-
-
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)amino]benzyl]-4-pentylbenzamide
-
-
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[methyl(pyridin-4-yl)amino]benzyl]-4-pentylbenzamide
-
-
N-[1-Benzyl-3-(2-biphenyl-4-yl-1-carbamoyl-ethylamino)-2-hydroxy-propyl]-2-(3-1H-indol-3-yl-propionylamino)-3-methyl-butyramide
-
-
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-4-methyl-N-(4-methylpentyl)pentan-1-aminium
-
-
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-N-pentylpentan-1-aminium
-
-
N-[3-(2,7-dichloro-9H-fluoren-4-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[3-(9H-fluoren-2-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[3-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
-
-
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(4-chlorophenyl)isoxazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N2-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-leucinamide
-
-
Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
pyridine-2-carboxylic acid ((R)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(3-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-(3-methoxyphenyl)ethylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-3-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcar-bamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcarbamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-benzyloxymethyl-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-3-((S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl)-2-hydroxy-1-phenethylpropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-phenylaminoethyl-carbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-phenylpropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(4-cyanobenzylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(cyclohexylmethylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-butylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methylpropyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-butylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(3-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
Ro 40-4388
-
aspartic protease peptidomimetic compound that potently inhibits plasmepsin I. Antimalarial activity is not exerted through inhibition of plasmepsins
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
-
-
pepstatin
-
IC50: about 5 nM
pepstatin A
-
-
Ro40-4388
-
-
SC-50083
-
most selective inhibitor
SC-50083
-
IC50: 0.000132 mM
additional information
-
inhibition of the enzyme blocks the essential pathway of hemoglobin degradation, leading to death of the organism
-
additional information
-
none of the inhibitors analyzed to date have sufficient selectivity for plasmepsin I and II, compared to their human counterparts
-
additional information
-
plasmepsin I is a valid antimalarial drug target on two counts. First, inhibition of the enzyme correlates with inhibition of parasite growth. Second, specificity of inhibition over human aspartic proteinases is possible
-
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0.00025
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
-
0.0013
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
-
0.00018
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
-
0.0005
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
-
-
0.000025
(2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
0.000006
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(1,3-benzodioxol-5-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000008
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
0.000038
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000009
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000198
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-6-[2-[(4-tert-butylphenyl)carbonyl]hydrazino]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
-
-
0.001837
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-N'1,N'6-bis[(4-tert-butylphenyl)carbonyl]-3,4-dihydroxyhexanedihydrazide
-
-
0.00016 - 0.000163
(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-en-1-yloxy)hexanediamide
0.0000084
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,4-dimethoxy-3,5-pyrimidin)-2-propenyl-oxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000023
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,5-dimethyl-3,4-oxazol)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000005
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3,4-methylenedioxyphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000013
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3-thienyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000008
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-acetylphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
the best dual inhibitor for EC 3.4.23.38 and EC 3.4.23.39
0.0000025
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-fluorophenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000058
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-tolyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000027
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-bromo-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000014
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-phenyl-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000072
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-phenyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-trimethylsilyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-(methoxycarbonyl)-pent-2,4-dienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000044
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-phenyl-pentadienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.00082
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
-
0.00001
(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
-
-
0.000098
(2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.00053
(2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.0011
(2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000063
(2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000115
(2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.0013
(2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000438
(2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.001
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000068
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000469
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
-
0.024
(3S,4S)-5-(4-bromobenzyloxy)-3-hydroxy-4-(2-thiophen-2-ylacetylamino)pentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.04
(3S,4S)-5-(4-bromobenzyloxy)-4-(3,3-diphenylpropionylamino)-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.057
(3S,4S)-5-(4-bromobenzyloxy)-4-diphenylacetylamino-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.000727
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
0.00028
(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.00091
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-([N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl]amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide
-
-
0.002046
(5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
-
0.0019
(5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
-
0.059
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-propyl)amide
-
-
0.000017
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000011
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
-
0.00000001
17-Benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
-
0.000163
2,5-Bis-allyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
0.000025
2,5-Bis-benzyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
0.0000048
4-(1,3-benzodioxol-5-yl)-Nalpha-[(2S,3S)-2-hydroxy-3-([N-[3-(1H-indol-3-yl)propanoyl]-L-valyl]amino)-4-phenylbutyl]-L-phenylalaninamide
-
-
0.000013
4-(1-benzofuran-2-yl)-Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.029
benzo[1,3]dioxole-5-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-amide
-
-
0.00025
benzyl 2-benzyl-2-[(2S,3R)-3-[(4-bromobenzyl)oxy]-2-hydroxy-4-oxo-4-[(2-piperidin-1-ylethyl)amino]butyl]hydrazinecarboxylate
-
-
0.000009
benzyl 3-benzyl-4-([2-[(1-formyl-3-methylbutyl)amino]-2-oxo-1-phenylethyl]amino)-4-oxobutanoate
-
-
0.0000027
benzyl [(1S,4S,5R,6R,7S,10S)-4,7-bis[(4-cyanophenoxy)methyl]-5,6-dihydroxy-1,10-bis(1-methylethyl)-2,9,12-trioxo-14-phenyl-13-oxa-3,8,11-triazatetradec-1-yl]carbamate
-
-
0.0000005 - 0.0000007
Iva-Val-Val-Sta-Ala-Sta
0.042
KPFEL-PSI(CH2-NH)-AWT
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000043
KPFSL-PSI(CH2-NH)-LQF
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0055
KPLEF-PSI(CH2-NH)-FRV
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.038
KPLEF-PSI(CH2-NH)-YRV
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000073
KPnorLSnorL-PSI(CH2-NH)-LQI
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.031
KPVEF-PSI(CH2-NH)-RQT
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0003
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0000033
N-((1S,2S)-1-(4-benzo[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.619
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
0.0034
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
0.032
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
0.000116
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
0.0000059
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.000221
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
0.000033
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000001
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000074
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000058
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000765
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000081
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
-
-
0.000031
N-[(1S)-1-([(1S,2S)-3-[(2-amino-2-oxoethyl)(benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl)-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000004
N-[(1S)-1-[[(1S,2S)-1-([[4-(1,3-benzodioxol-5-yl)benzyl]oxy]methyl)-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000016
N-[(1S)-1-[[(1S,2S)-1-benzyl-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000005
N-[(1S)-1-[[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000115
N-[(1S)-1-[[(1S,2S)-3-([(1S)-2-amino-1-[(4'-methylbiphenyl-4-yl)methyl]-2-oxoethyl]amino)-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.001
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-3-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.00022
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl](benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000068
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.822
N-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.000188
N-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-cyclo-hexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.0000034
N-[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]-2,4,6-trifluorobenzamide
-
-
0.000278
N-[(1S,2S)-3-cyclohexylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.0000021
N-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butyl-carbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.000022
N-[(3S)-3-[(2S,5S,14S)-14-[(3,3-dimethylbutanoyl)amino]-2-(1-methylethyl)-3,11,15-trioxo-1,4,10-triazacyclopentadecan-5-yl]-3-hydroxypropanoyl]-L-valyl-L-leucylglycinamide
-
-
0.000027
N-[(3S,4S)-3-hydroxy-6-phenyl-4-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]hexanoyl]-L-alanyl-L-leucinamide
-
-
0.0000026
N-[1-Benzyl-3-(2-biphenyl-4-yl-1-carbamoyl-ethylamino)-2-hydroxy-propyl]-2-(3-1H-indol-3-yl-propionylamino)-3-methyl-butyramide
-
-
0.0029
N2-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-leucinamide
-
-
0.0021
Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.000000565
pepstatin
-
pH 5.0, 37°C
0.0000000117 - 0.0000014
pepstatin A
0.0064
pyridine-2-carboxylic acid ((R)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.000001
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(3-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methyl-propyl)-amide
-
-
0.0000004
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)-amide
-
-
0.0067
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-(3-methoxyphenyl)ethylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
0.049
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
0.0005
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.0000007
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-3-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcar-bamoyl)-2-methyl-propyl)-amide
-
-
0.0000003
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcarbamoyl)-2-methyl-propyl)-amide
-
-
0.0054
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-benzyloxymethyl-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.027
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-1-phenethylpropylcarbamoyl)-2-methylpropyl)amide
-
-
0.0000027
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
0.0089
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-phenylaminoethyl-carbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.0054
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-phenylpropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.053
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(4-cyanobenzylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0039
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(cyclohexylmethylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0081
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-butylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0041
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0000019
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methylpropyl)-amide
-
-
0.000001
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-butylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
0.0000004
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(3-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
0.0000003
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
0.0000014 - 0.000009
Ro40-4388
0.000006 - 0.000008
Ro40-5576
0.00023
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
-
-
additional information
additional information
-
Ki-value for Ro17-7109 is above 0.05 mM
-
0.00016
(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-en-1-yloxy)hexanediamide
-
-
0.000163
(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-en-1-yloxy)hexanediamide
-
-
0.0000005
Iva-Val-Val-Sta-Ala-Sta
-
pH 4.4, 37°C, naturally occuring enzyme
0.0000007
Iva-Val-Val-Sta-Ala-Sta
-
pH 4.4, 37°C, recombinant enzyme
0.0003
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
-
0.0003
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
pH 4.4
0.0000000117
pepstatin A
-
pH 2.8, mature fusion protein
0.0000000699
pepstatin A
-
pH 5.0, mature fusion protein
0.00000039
pepstatin A
-
-
0.0000014
pepstatin A
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0000014
Ro40-4388
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000004
Ro40-4388
-
pH 4.4, 37°C
0.000009
Ro40-4388
-
naturally occuring enzyme
0.000006
Ro40-5576
-
-
0.000006
Ro40-5576
-
pH 4.4
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.0017
(1S,2aR,3aR,3bS,4R,9aR,11aS)-2-(((1-(2-cyanophenyl)-1H-1,2,3-triazol-4-yl)methoxy)imino)-1-(furan-3-yl)-3b,6,6,9a,11a-pentamethyl-7-oxo-1,2,2a,3b,4,5,5a,6,7,9a,9b,10,11,11a-tetradecahydronaphtho(1,2':6,7)indeno(1,7a-b)oxiren-4-yl acetate
Plasmodium falciparum
pH and temperature not specified in the publication
0.0021
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00037
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00067
(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.000727
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
Plasmodium falciparum
-
-
0.000017
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000011
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
Plasmodium falciparum
-
-
0.022
1-[2-hydroxy-3-(1,2,3,4,5,6,7,8-octahydrophenanthren-9-yloxy)propyl]-4-(3-methoxyphenyl)piperazin-1-ium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000629
2,3-difluoro-4-methyl-N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]benzamide
Plasmodium falciparum
-
-
0.00093
3'-(((1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-ylamino)methyl)biphenyl-2-ol
Plasmodium falciparum
-
-
0.022
3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl 3,4-di-O-acetyl-2,6-dideoxyhexopyranoside
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.028
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.037
5-[bis[(benzyloxy)carbonyl]amino]-6-[[1-hydrazinyl-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-oxohexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000655
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.000441
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.024
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000033
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000001
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000074
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000058
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamid
Plasmodium falciparum
-
-
0.000765
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000081
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000034
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
Plasmodium falciparum
-
-
0.002
N-butyl-N-[2-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-hydroxyethyl]butan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.004
N-hexyl-N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]hexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.023
N-hexyl-N-[2-hydroxy-2-(phenanthren-9-yl)ethyl]hexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.001727
N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentyl-N-[4-[(pyridin-3-ylmethyl)carbamoyl]benzyl]benzamide
Plasmodium falciparum
-
-
0.000711
N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentyl-N-[[4'-(piperidin-1-ylcarbonyl)biphenyl-4-yl]methyl]pyridine-2-carboxamide
Plasmodium falciparum
-
-
0.001162
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)amino]benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.001123
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[methyl(pyridin-4-yl)amino]benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.003
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-4-methyl-N-(4-methylpentyl)pentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.023
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.041
N-[3-(2,7-dichloro-9H-fluoren-4-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.071
N-[3-(9H-fluoren-2-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.003
N-[3-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000123
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
Plasmodium falciparum
-
-
0.000537
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000113
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000104
N-[[5-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.001672
N-[[5-(4-chlorophenyl)isoxazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000001 - 0.000005
pepstatin
0.000132
SC-50083
Plasmodium falciparum
-
IC50: 0.000132 mM
0.00023
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
Plasmodium falciparum
-
-
0.000001
pepstatin
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000005
pepstatin
Plasmodium falciparum
-
IC50: about 5 nM
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