3.4.23.39: plasmepsin II
This is an abbreviated version!
For detailed information about plasmepsin II, go to the full flat file.
Word Map on EC 3.4.23.39
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3.4.23.39
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plasmepsins
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plasmodium
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falciparum
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antimalarial
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piperaquine
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artemisinin
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pfmdr1
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cambodia
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proplasmepsins
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hemoglobin-degrading
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pfcrt
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artemisinin-based
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dihydroartemisinin-piperaquine
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prosegment
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molecular biology
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falcipains
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analysis
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medicine
- 3.4.23.39
-
plasmepsins
- plasmodium
- falciparum
-
antimalarial
-
piperaquine
- artemisinin
-
pfmdr1
-
cambodia
-
proplasmepsins
-
hemoglobin-degrading
-
pfcrt
-
artemisinin-based
-
dihydroartemisinin-piperaquine
- prosegment
- molecular biology
-
falcipains
- analysis
- medicine
Reaction
Hydrolysis of the bonds linking certain hydrophobic residues in hemoglobin or globin. Also cleaves the small molecule substrates such as Ala-Leu-Glu-Arg-Thr-Phe!Phe(NO2)-Ser-Phe-Pro-Thr =
Synonyms
AH II, aspartic hemoglobinase II, malarial aspartic protease, PFAPD, pfpm2, plasmepsin 2, plasmepsin II, PLm II, PLMII, PM II, PMII, PSM2
ECTree
3.4.23.39 plasmepsin IIAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.4.23.39 - plasmepsin II
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(1R,2R,3R,4R)-1,4-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-1,4-bis[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]butane-2,3-diol
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(1R,2R,3R,4S)-3-[(4-butylphenyl)sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[(4-heptylphenyl)sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[(4-hexylphenyl)sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(2-cyclobutylethyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(2-cyclopentylethyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(3-cyclohexylpropyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(3-cyclopentylpropyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(3-ethoxypropyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(4,4-dimethylpentyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(4-fluorobutyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(4-methoxybutyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-3-[[4-(6-fluorohexyl)phenyl]sulfonyl]-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-N-(naphthalen-2-ylmethyl)-3-[[4-(2-propoxyethyl)phenyl]sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S)-N-(naphthalen-2-ylmethyl)-3-[[4-(pentyloxy)phenyl]sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S,5R)-5-[(cyclobutylamino)methyl]-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S,5R)-5-[(cyclopentylamino)methyl]-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S,6R)-6-[(cyclobutylamino)methyl]-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3R,4S,6R)-6-[(cyclopentylamino)methyl]-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
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(1R,2R,3S,4S)-2,3-bis(naphthalen-2-ylmethoxy)-7-azabicyclo[2.2.1]heptane
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(1R,4S)-6-[2-(1,3-benzothiazol-2-ylsulfanyl)ethoxy]-7-(naphthalen-1-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
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(1R,4S)-6-[2-(1,3-benzothiazol-2-ylsulfanyl)ethoxy]-7-(naphthalen-2-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
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(1R,4S)-6-[2-(1,3-benzothiazol-2-ylsulfanyl)ethoxy]-7-[2-(naphthalen-1-yl)ethoxy]-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
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(1R,4S)-6-[2-[(6-chloro-1,3-benzothiazol-2-yl)sulfanyl]ethoxy]-7-(naphthalen-1-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
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(1R,4S)-6-[2-[(6-chloro-1,3-benzothiazol-2-yl)sulfanyl]ethoxy]-7-(naphthalen-2-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
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(1R,4S)-6-[2-[(6-chloro-1,3-benzothiazol-2-yl)sulfanyl]ethoxy]-7-[2-(naphthalen-1-yl)ethoxy]-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
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(1R,4S)-6-[3-(1,3-benzothiazol-2-ylsulfanyl)propyl]-7-(naphthalen-1-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
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(1R,4S)-6-[3-[(6-chloro-1,3-benzothiazol-2-yl)sulfanyl]propyl]-7-(naphthalen-1-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
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(1RS) 3,3-difluoro-N-[2-(2-naphthyl)ethyl]-4-oxo-N-(4-pentylphenyl)cyclohexanecarboxamide
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(1RS,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
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(1S)-3,3-difluoro-4,4-dihydroxy-N-(naphthalen-2-ylmethyl)-N-(4-pentylphenyl)cyclohexanecarboxamide
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(1S,2S,3R,4R)-2-([4-[3-(1,3-benzodioxol-5-yl)propyl]benzyl]oxy)-3-(naphthalen-2-ylmethoxy)-7-azabicyclo[2.2.1]heptane
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(1S,2S,3R,4R)-2-[(4-bromobenzyl)oxy]-3-(naphthalen-2-ylmethoxy)-7-azabicyclo[2.2.1]heptane
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(1S,2S,3S,4R)-3-(4-bromophenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
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(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
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(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
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(1SR,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
-
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(1Z)-(3,4-dimethoxyphenyl)-N'-[[(3,4,5-trichlorophenoxy)acetyl]oxy]ethanimidamide
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(1Z)-N'-{[(4-chloro-3,5-dimethylphenoxy)acetyl]oxy}-2-(3,4-dimethoxyphenyl)ethanimidamide
-
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(2E)-2-[(2H-1,3-benzodioxol-5-yl)methylidene]hydrazine-1-carboximidamide
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(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxyindan-1-yl)-butyramide
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0.005 mM, 25% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
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0.005 mM, 68% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
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0.005 mM, 74% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
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0.005 mM, 39% of maximal activity
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
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0.005 mM, 40% inhibition
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
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0.005 mM, 54% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
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0.005 mM, 43% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
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0.005 mM, 64% 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
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0.005 mM, 50% 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
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0.005 mM, 49% 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
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(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
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(2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S)-2-methyl-1-(methylcarbamoyl)propyl]hexanediamide
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(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
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(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
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(3,5-dimethylisoxazol-4-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
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(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
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(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
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
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(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]-5-(5-methyl-1,3,4-oxadiazol-2-yl)pentanamide
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(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]-5-[5-(2-phenylethyl)-1,3,4-oxadiazol-2-yl]pentanamide
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(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
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-5-[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]pentanamide
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(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
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(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
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(2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S)-2-methyl-1-(methylcarbamoyl)propyl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
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(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
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(2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis[[(2E)-3-phenylprop-2-en-1-yl]oxy]hexanediamide
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(2R,3R,4R,5R)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]-2,5-bis(prop-2-en-1-yloxy)hexanamide
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(2R,3R,4R,5R)-5-(5-benzyl-1,3,4-oxadiazol-2-yl)-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]pentanamide
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(2R,3R,4R,5R)-5-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-1-oxa-7-azacyclohexadecane-2-carboxamide
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(2R,3R,4R,5R)-6-(2-acetylhydrazino)-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-oxohexanamide
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(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
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(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
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-
(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
-
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(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
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(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
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(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
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-
(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(2R,3R,4R,5R,14E)-5-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-1-oxa-7-azacyclohexadec-14-ene-2-carboxamide
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-
(2R,3R,4S,6R)-6-[[(E)-2-(4-acetylphenyl)ethenyl]oxy]-2-[[(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]heptanediamide
-
inhibitor candidate, designed according to inhibitor modeling. Selectivity index Ki value Cathepsin D to Ki value PlmII is 333
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
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0.005 mM, 35% inhibition
(2S,3S)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 20% 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
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-
(2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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-
(2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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-
(2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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-
(2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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-
(2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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(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)-4-[([4-[4-amino-3-(4-chlorophenyl)butanoyl]-1-(biphenyl-4-ylmethyl)piperazin-2-yl]acetyl)amino]-N-butyl-3-hydroxy-5-phenylpentanamide
-
-
(3S,4S)-4-[[(2S)-2-(benzylamino)-3-methylbutanoyl]amino]-N-[(1S)-1-(cyclohexylmethyl)-2-[[3-(1H-imidazol-1-yl)propyl]amino]-2-oxoethyl]-3-hydroxy-5-phenylpentanamide
-
-
(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,3R)-3-methyl-2-(2-(naphthalen-2-yl)acetamido)pentanamido)heptanamide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
(3S,6S,9S,12S,15S,18S)-15-(3-amino-3-oxopropyl)-18-sec-butyl-3,9-dibutyl-1-((S)-1-((S)-2,6-diaminohexanoyl)pyrrolidin-2-yl)-6-(hydroxymethyl)-12-isobutyl-1,4,7,13,16-pentaoxo-2,5,8,11,14,17-hexaazanonadecan-19-oic acid
-
-
(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)-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
-
-
(5-[[(4-bromobenzoyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
-
(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
-
-
(5S,8S,12S,13S,16S,19S)-13-benzyl-12-hydroxy-8,23,23-trimethyl-16,19-bis(1-methylethyl)-5-(2-methylpropyl)-4,7,10,15,18,21-hexaoxo-3,6,9,14,17,20-hexaazatetracosan-1-amide
-
-
(6S,9S,12R,13S,17S,20R,21S)-13,21-dihydroxy-2,17-dimethyl-6,9-bis(1-methylethyl)-4,7,10,15,18-pentaoxo-12,20-bis(trifluoromethyl)-5,8,11,16,19-pentaazatricosan-23-oic acid
-
-
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-(pyridine-2-ylmethyl)amino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.00030 mM
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-(pyridine-4-ylmethyl)amino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.00049 mM
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-ethylamino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.00072 mM
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-methylamino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.00045 mM
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(4-hydroxymethylphenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.0011 mM
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)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-(3-methylbutyl)-N-(4-pentylbenzyl)-N-(4-pyridin-3-ylbenzyl)piperidin-4-amine
-
-
1-(4-chlorophenyl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
-
IC50 700 nM for antiplasmodial activity
1-(4-nitrophenyl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
-
IC50 2100 nM for antiplasmodial activity
1-(biphenyl-4-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
-
highest antiplasmodial activity among compounds tested with IC50 of 160 nM
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-amide
-
-
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
-
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenylamino)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
-
1-Acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
-
1-Acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenylamino)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
-
1-methyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-(3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl)-amide
-
-
1-Methyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
-
1-Methyl-piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
1-methyl-piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
1-Methyl-piperidine-4-carboxylic acid {3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
1-[2-hydroxy-3-(1,2,3,4,5,6,7,8-octahydrophenanthren-9-yloxy)propyl]-4-(3-methoxyphenyl)piperazin-1-ium
-
-
1-[3-chloro-6-(trifluoromethyl)phenanthren-9-yl]-3-(dibutylamino)propan-1-ol
-
1-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-(dibutylamino)ethanol
-
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
-
-
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
-
-
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-aminobenzoate)
Ki value for human cathepsin D 0.142 mM
2,3,4-trifluoro-N-([[1-(3-methylbutyl)piperidin-4-yl](4-pentylbenzoyl)amino]methyl)benzamide
-
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]
-
-
2-(1,3-benzothiazol-2-ylamino)-N-(2-chlorophenyl)-6-oxo-1,4,5,6tetrahydro-4-pyrimidinecarboxamide
-
-
2-(2-naphthyl)-N-(4-pentylphenyl)-N-piperidin-4-ylacetamide hydrochloride
-
-
2-(dihexylamino)-1-(1,2,3,4-tetrahydrophenanthren-9-yl)ethanol
-
2-([2-[4-([[(1S,2S,3R,4R)-3-(naphthalen-2-ylmethoxy)-7-azabicyclo[2.2.1]hept-2-yl]oxy]methyl)phenoxy]ethyl]sulfanyl)-1,3-benzothiazole
-
2-([2-[4-([[3-(naphthalen-2-ylmethoxy)-7-azabicyclo[2.2.1]hept-2-yl]oxy]methyl)phenoxy]ethyl]sulfanyl)-1,3-benzothiazole
-
-
2-([4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-yl]oxy)ethanol
-
IC50: 441 nM
2-([N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-(methylsulfonyl)glycyl]amino)-N-isobutylbenzamide
-
-
2-amino-7-(4-butylphenyl)-3-[(5-phenyltetrahydrofuran-2-yl)methyl]quinazolin-4(3H)-one
-
2-amino-7-(4-pentylphenyl)-3-[(5-phenyltetrahydrofuran-2-yl)methyl]quinazolin-4(3H)-one
-
2-amino-7-phenyl-3-(tetrahydrofuran-2-ylmethyl)quinazolin-4(3H)-one
-
2-amino-7-phenyl-3-[(5-phenyltetrahydrofuran-2-yl)methyl]quinazolin-4(3H)-one
-
2-amino-7-[4-(4-phenylbutyl)phenyl]-3-[(5-phenyltetrahydrofuran-2-yl)methyl]quinazolin-4(3H)-one
-
2-[(Z)-1-(4-chlorophenyl)-2-[3-(pyridin-2-yl)isoquinolin-1-yl]ethenyl]hydrazine-1-carboximidothioic acid
-
2-[4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-yl]ethanol
-
IC50: 0.00147 mM
2-[bis(4-methylpentyl)amino]-1-(1,2,3,4-tetrahydrophenanthren-9-yl)ethanol
-
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-amino-N-[(1S,3S,4S)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-1-(2-methylpropyl)-5-phenylpentyl]benzamide
-
-
3-amino-N-[(4S,6S,7S)-7-[[(2,6-dimethylphenoxy)acetyl]amino]-6-hydroxy-2-methyl-8-phenyloctan-4-yl]benzamide
-
3-chloro-N-([2-(2-methoxybenzoyl)hydrazino]carbonothioyl)-1-benzothiophene-2-carboxamide
-
-
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
-
-
4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-carbonitrile
-
IC50: 713 nM; IC50: 918 nM
4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-3-carboxylic acid
-
IC50: 208 nM
4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-carboxylic acid
-
IC50: 495 nM
4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)-N,N-dimethylbiphenyl-4-carboxamide
-
IC50: 77 nM
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
-
-
4-(benzyloxy)-N-[(1S,2S)-3-[(1-benzylpiperidin-4-yl)amino]-1-(cyclohexylmethyl)-2-hydroxypropyl]-3,5-dimethoxybenzamide
-
-
4-amino-N'-(benzyloxy)-N-(2-methylphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
4-amino-N'-(benzyloxy)-N-(2-methylphenyl)-1,2,5-oxadiazole-3carboximidamide
-
-
4-amino-N'-(benzyloxy)-N-(4-methylphenyl)-1,2,5-oxadiazole-3carboximidamide
-
-
4-amino-N'-[(2,4-dichlorobenzyl)oxy]-N-(2-methylphenyl)-1,2,5oxadiazole-3-carboximidamide
-
-
4-amino-N'-[(2,4-dichlorophenyl)methoxy]-N-(2-methylphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
4-amino-N'-[(2-methyl-1-naphthyl)methoxy]-1,2,5-oxadiazole-3carboximidamide
-
-
4-amino-N-[(1S,3S,4S)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-1-(2-methylpropyl)-5-phenylpentyl]benzamide
-
-
4-amino-N-[(4S,6S,7S)-7-[[(2,6-dimethylphenoxy)acetyl]amino]-6-hydroxy-2-methyl-8-phenyloctan-4-yl]benzamide
-
4-butoxy-N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)benzamide
-
IC50: 0.0059 mM
4-butoxy-N-[2-(dibutylamino)ethyl]-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 0.0103 mM
4-butyl-N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)benzamide
-
IC50: 0.0023 mM
4-butyl-N-[2-(dibutylamino)ethyl]-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 0.0039 mM
4-chloro-5-(4-chlorophenoxy)-2-[([[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl)amino]benzenesulfonate
-
-
4-methoxy-N-(2-[5-(2-nitrophenyl)-2-furyl]-1-([(4-pyridinylmethyl)amino]carbonyl)vinyl)benzamide
-
-
4-methyl-N-[2-[2-(naphthalen-2-yl)hydrazinyl]phenyl]benzene-1-sulfonamide
-
5-[4-([(1S,2R,3R,4R)-3-[(naphthalen-2-ylmethyl)amino]-7-azabicyclo[2.2.1]hept-2-yl]sulfonyl)phenyl]pentan-1-ol
-
5-[bis[(benzyloxy)carbonyl]amino]-6-[[1-hydrazinyl-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-oxohexan-1-aminium
-
-
6-((2-[(5-chloro-2-methoxyphenyl)amino]-2-oxoethyl)thio)-5-cyano-N-(2-methoxyphenyl)-2-methyl-4-phenyl-1,4-dihydro-3-pyridinecarboxamide
-
-
6-bromo-2,3,4,9-tetrahydro-1H-carbazol-1-one Nphenylthiosemicarbazone
-
-
6-[3-(1,3-benzothiazol-2-ylsulfanyl)propyl]-7-(2-naphthalen-1-ylethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
-
-
6-[4-([(1S,2R,3R,4R)-3-[(naphthalen-2-ylmethyl)amino]-7-azabicyclo[2.2.1]hept-2-yl]sulfonyl)phenyl]hex-5-yn-1-ol
-
6-[4-([(1S,2R,3R,4R)-3-[(naphthalen-2-ylmethyl)amino]-7-azabicyclo[2.2.1]hept-2-yl]sulfonyl)phenyl]hexan-1-ol
-
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
-
-
butyloxycarbonyl-His-Pro-Phe-His-Leu-PSI[CH(OH)-CH2]-Val-Ile-His
-
IC50: 150 nM
extract from Plexaura homomalla
-
black sea rod, extract contains a reversible tight-binding inhibitor
-
extract from Xestospongia muta
-
giant barrel sponge, extract contains a reversible tight-binding inhibitor
-
L-lysyl-L-prolyl-L-phenylalanyl-N-[(1S)-1-benzyl-2-[[(1S)-1-benzyl-2-[[(1S)-2-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-1-(hydroxymethyl)-2-oxoethyl]amino]-2-oxoethyl]amino]ethyl]-L-norleucinamide
-
-
LCu(CH3COO)2
-
copper(II) nanohybrid solids are synthesized and are shown to be capped by a bis(benzimidazole) diamide ligand (L)
LCuCl2
-
copper(II) nanohybrid solids are synthesized and are shown to be capped by a bis(benzimidazole) diamide ligand (L)
methyl 4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-carboxylate
-
-
methyl [4'-(([1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetate
-
-
methyl [4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-yl]acetate
-
IC50: 124 nM
methyl [4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetate
-
IC50: 183 nM
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl](4-pentylbenzoyl)amino]methyl)biphenyl-4-yl]acetate
-
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-pentylcyclohexyl)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',N''-[1,10-phenanthroline-2,9-diyldi(E)methylylidene]bis[N-(2-methylphenyl)pyridine-2-carbohydrazonamide]
-
N'-(4-chlorophenyl)-N'-(2-[[(3-chlorophenyl)carbamoyl]amino]phenyl)urea
-
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
-
N,N'-([(4,6-dimethyl-2-quinazolinyl)amino]methylylidene)dipropanamide
-
-
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
-
-
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyridin-2-ylbenzyl)ethane-1,2-diamine
-
IC50: 0.0013 mM
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyridin-4-ylbenzyl)ethane-1,2-diamine
-
IC50: 0.001603 mM
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyrimidin-5-ylbenzyl)ethane-1,2-diamine
-
IC50: 0.001631 nM
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-([4'-(2-pyrrolidin-1-ylethoxy)biphenyl-4-yl]methyl)ethane-1,2-diamine
-
IC50: 0.002 mM
N,N-dibutyl-N'-[(2'-fluorobiphenyl-4-yl)methyl]-N'-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 0.001022 mM
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-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-methyl-4-oxo-1,4-dihydro-2-pyrimidinyl)amino]methylene)benzamide
-
-
N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-oxo-4-propyl-1,6-dihydro-2-pyrimidinyl)amino]methylene)-4-methoxybenzamide
-
-
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)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-4-methyl-1-oxopentan-2-yl)-4-(4-((2S,3R)-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-(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-((4'-[2-(benzylamino)-2-oxoethyl]biphenyl-4-yl)methyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 46 nM
N-((S)-1-(((2S,3S)-3-hydroxy-5-oxo-5-(((S)-1-oxo-3-phenyl-1-(prop-2-yn-1-ylamino)propan-2-yl)amino)-1-phenylpentan-2-yl)-amino)-3-methyl-1-oxobutan-2-yl)picolinamide
-
-
N-((S)-1-(((2S,3S)-5-(((R)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-chloro-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
-
-
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-1-oxopent-4-yn-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
-
-
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-cyano-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)picolinamide
-
-
N-(([2-(4-ethylphenyl)-6-methyl-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
-
-
N-(([6-methyl-2-(4-methylphenyl)-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
-
-
N-(1,3-benzodioxol-5-ylmethyl)-N'-[4-(2-oxo-2H-chromen-3-yl)-1,3thiazol-2-yl]succinamide
-
-
N-(2-([3-(1,3-benzodioxol-5-yl)-3-oxo-1-propen-1-yl]amino)phenyl)-4-nitrobenzenesulfonamide
-
-
N-(2-aminoethyl)-N-(biphenyl-4-ylmethyl)-4-pentylbenzamide
-
IC50: 0.003329 nM
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(2,5-dimethyl-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
N-(2-Benzo[1,3]dioxol-5-yl-ethyl)-N-{3-[2-(2,5-dimethyl-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
N-(2-Benzo[1,3]dioxol-5-yl-ethyl)-N-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
N-(2-methoxyphenyl)-2-(5H-[1,2,4]triazino[5,6-b]indol-3ylthio)butanamide
-
-
N-(3,4-dichlorophenyl)-2-[(4,6-dimethyl-2-pyrimidinyl)amino]3a,4,5,6,7,7a-hexahydro-1H-benzimidazole-1-carboxamide
-
-
N-(3,4-dichlorophenyl)-2-[(4,6-dimethylpyrimidin-2-yl)amino]-3a,4,5,6,7,7a-hexahydro-1H-benzimidazole-1-carboxamide
-
N-(3,4-dimethylphenyl)-N'-(imino[(4,6,7-trimethyl-2-quinazolinyl)amino]methyl)thiourea
-
-
N-(3-{(2-Benzo[1,3]dioxol-5-yl-ethyl)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionyl]-amino}-1-benzyl-2-hydroxy-propyl)-4-benzyloxy-3,5-dimethoxy-benzamide
-
-
N-(4-hexylphenyl)-2-(2-naphthyl)-N-piperidin-4-ylacetamide hydrochloride
-
-
N-(4-[5-(1,3-benzodioxol-5-yl)pyridin-2-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 1912 nM
N-(4-[6-(1,3-benzodioxol-5-yl)pyridin-3-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 437 nM
N-(4-[benzyl(methyl)amino]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 289 nM
N-(amino[(4,6-dimethyl-2-quinazolinyl)amino]methylene)-2-(4-chlorophenyl)acetamide
-
-
N-(biphenyl-4-ylmethyl)-4-butoxy-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0047 mM
N-(biphenyl-4-ylmethyl)-4-butyl-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0015 mM
N-(biphenyl-4-ylmethyl)-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 0.002067 mM
N-(biphenyl-4-ylmethyl)-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 0.003943 mM
N-(biphenyl-4-ylmethyl)-N-[2-(butylamino)ethyl]-4-pentylbenzamide
-
IC50: 0.001161 mM
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-propylbenzamide
-
IC50: 0.0129 mM
N-(biphenyl-4-ylmethyl)-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
-
IC50: 0.002317 mM
N-([(1RS)-3,3-difluoro-4-oxocyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1RS)-3,3-difluoro-4-oxocyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1RS,4RS)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1RS,4SR)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1SR,4RS)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1SR,4SR)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(2,4-dimethylphenyl)amino][(4-oxo-1,4,5,6,7,8-hexahydro-2-quinazolinyl)amino]methylene)benzamide
-
-
N-([3',5'-bis(trifluoromethyl)biphenyl-4-yl]methyl)-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0017 mM
N-([3',5'-bis(trifluoromethyl)biphenyl-4-yl]methyl)-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
IC50: 0.00119 mM
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
-
-
N-([[1-(3-methylbutyl)piperidin-4-yl](4-pentylbenzoyl)amino]methyl)-1-benzothiophene-2-carboxamide
-
N-([[1-(3-methylbutyl)piperidin-4-yl](4-pentylbenzoyl)amino]methyl)pyridine-3-carboxamide
-
N-benzyl-2-bromo-N-[(4-[[2-(2,4-dichlorophenyl)ethyl](4-phenylbutanoyl)amino]pyrrolidin-3-yl)methyl]-4,5-dimethoxybenzamide
-
N-benzyl-2-bromo-N-[(4-[[2-(2,4-dichlorophenyl)ethyl][3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoyl]amino]pyrrolidin-3-yl)methyl]-4,5-dimethoxybenzamide
-
N-benzyl-2-bromo-N-[[4-([[3-(2,4-dichlorophenyl)propyl](3-phenylpropyl)amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
-
N-benzyl-2-bromo-N-[[4-([[3-(2,4-dichlorophenyl)propyl][2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
-
N-benzyl-4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-carboxamide
-
IC50: 72 nM
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-[(1S)-1-([(1S,2S)-1-([(4-bromobenzyl)oxy]methyl)-4-([(1S)-2-([(1S)-1-carbamoylbutyl]amino)-2-hydroxy-1-methylethyl]amino)-2-hydroxy-4-oxobutyl]carbamoyl)-2-methylpropyl]-4,5-dihydropyridine-2-carboxamide
-
-
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-[(1S,2S)-3-[[2-(1,3-benzodioxol-5-yl)ethyl][3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoyl]amino]-1-benzyl-2-hydroxypropyl]-4-(benzyloxy)-3,5-dimethoxybenzamide
-
-
N-[(1SR,3RS)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-[(1SR,3SR)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-[(2'-chlorobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 191 nM
N-[(2S,3S)-2-hydroxy-3-[(phenoxyacetyl)amino]-4-phenylbutyl]-N-[2-(4-methoxyphenyl)ethyl]piperidine-4-carboxamide
-
inhibitor candidate, designed according to inhibitor modeling. Selectivity index Ki value Cathepsin D to Ki value PlmII is 15
N-[(2S,3S)-3-[[(3-chlorophenoxy)acetyl]amino]-2-hydroxy-4-phenylbutyl]-N-[2-(4-methoxyphenyl)ethyl]piperidine-4-carboxamide
-
-
N-[(2S,3S)-5-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-[(4-bromobenzyl)oxy]-3-hydroxy-5-oxopentan-2-yl]-2,4,6-trifluorobenzamide
-
inhibitor candidate, designed according to inhibitor modeling. Selectivity index Ki value Cathepsin D to Ki value PlmII is above 400
N-[(3-ethyl-1,2-oxazol-5-yl)methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
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-[(4'-butylbiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 591 nM
N-[(4'-chlorobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 446 nM
N-[(4'-chlorobiphenyl-4-yl)methyl]-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
IC50: 407 nM
N-[(4'-cyanobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 160 nM
N-[(E)-[(2,4-dimethylphenyl)amino][(4-oxo-1,4,5,6,7,8-hexahydroquinolin-2-yl)amino]methylidene]benzamide
-
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-(2-[4-[methyl(2-methylquinolin-4-yl)amino]phenyl]ethyl)-4-pentylbenzamide
-
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-(3-methylbutyl)piperidin-4-yl]-N-[[methyl(pyridin-3-yl)amino]methyl]-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-(dibutylamino)ethyl]-4-pentyl-N-(3-phenoxybenzyl)benzamide
-
IC50: 469 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-piperidin-1-ylbenzyl)benzamide
-
IC50: 369 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-2-ylbenzyl)benzamide
-
IC50: 380 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-3-ylbenzyl)benzamide
-
IC50: 374 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-4-ylbenzyl)benzamide
-
IC50: 212 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyrimidin-5-ylbenzyl)benzamide
-
IC50: 531 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-thiomorpholin-4-ylbenzyl)benzamide
-
IC50: 188 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-([4'-(thiomorpholin-4-ylcarbonyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 56 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(1H-pyrrol-1-yl)benzyl]benzamide
-
IC50: 240 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(4-phenylpiperazin-1-yl)benzyl]benzamide
-
IC50: 200 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-phenylpyridin-2-yl)benzyl]benzamide
-
IC50: 2345 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-pyrimidin-5-ylpyridin-2-yl)benzyl]benzamide
-
IC50: 8530 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-phenylpyridin-3-yl)benzyl]benzamide
-
IC50: 589 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-pyrimidin-5-ylpyridin-3-yl)benzyl]benzamide
-
IC50: 2229 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(phenylamino)benzyl]benzamide
-
IC50: 224 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(pyridin-4-ylamino)benzyl]benzamide
-
IC50: 1816 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 596 nM
N-[2-(dibutylamino)ethyl]-4-propyl-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 0.0396 mM
N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)-4-propylbenzamide
-
IC50: 0.0159 mM
N-[2-(dibutylamino)ethyl]-N-(4-pyridin-4-ylbenzyl)benzamide
-
IC50: 295 nM
N-[2-(dibutylamino)ethyl]-N-(4-pyrimidin-5-ylbenzyl)benzamide
-
IC50: 204 nM; IC50: 351 nM
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(phenyl)amino]benzyl)-4-pentylbenzamide
-
IC50: 574 nM
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(pyridin-4-yl)amino]benzyl)-4-pentylbenzamide
-
IC50: 3015 nM
N-[2-(dibutylamino)ethyl]-N-([3'-(trifluoromethyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 390 nM
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)-4-pentylbenzamide
-
IC50: 511 nM
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)benzamide
-
IC50: 104 nM
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 151 nM
N-[2-(dibutylamino)ethyl]-N-([4'-(2-morpholin-4-yl-2-oxoethyl)biphenyl-4-yl]methyl)-4-pentylbenzamide
-
IC50: 74 nM; IC50: 91 nM
N-[2-(dibutylamino)ethyl]-N-[(3',4'-dimethoxybiphenyl-4-yl)methyl]benzamide
-
IC50: 428 nM
N-[2-(dibutylamino)ethyl]-N-[(3'-methylbiphenyl-4-yl)methyl]benzamide
-
IC50: 293 nM
N-[2-(dibutylamino)ethyl]-N-[4-(1H-indol-1-yl)benzyl]-4-pentylbenzamide
-
IC50: 670 nM
N-[2-(dibutylamino)ethyl]-N-[4-(4-methylpiperazin-1-yl)benzyl]-4-pentylbenzamide
-
IC50: 2547 nM
N-[2-(dibutylamino)ethyl]-N-[4-(diethylamino)benzyl]-4-pentylbenzamide
-
IC50: 1491 nM
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-(dibutylamino)propyl]-4-pentyl-N-([4'-(2-pyrrolidin-1-ylethoxy)biphenyl-4-yl]methyl)benzamide
-
IC50: 221 nM
N-[3-(dibutylamino)propyl]-N-[(2'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 0.0011 mM; IC50: 322 nM
N-[3-(dibutylamino)propyl]-N-[(2'-methylbiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 597 nM
N-[3-(dibutylamino)propyl]-N-[(3',4'-dimethoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 468 nM
N-[3-(dibutylamino)propyl]-N-[(3'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 580 nM
N-[3-(dibutylamino)propyl]-N-[(4'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 246 nM
N-[3-[(2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionyl]-amino]-1-benzyl-2-hydroxy-propyl]-4-benzyloxy-3,5-dimethoxy-benzamide
-
-
N-[3-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[4,4-difluoro-3-oxocyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)-acetamide
-
-
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]-2-methoxypyridine-4-carboxamide
-
IC50: 154 nM
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-3-carboxamide
-
IC50: 202 nM
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-4-carboxamide
-
IC50: 464 nM
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]pyrazine-2-carboxamide
-
IC50: 243 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-piperidin-1-ylethyl)benzamide
-
IC50: 334 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-[4-(3-phenylpropyl)piperidin-1-yl]ethyl)benzamide
-
IC50: 165 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 831 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-([2-(diethylamino)ethyl](ethyl)amino)ethyl)-4-pentylbenzamide
-
IC50: 439 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-morpholin-4-ylethyl)-4-pentylbenzamide
-
IC50: 2897 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[benzyl(2-hydroxyethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 334 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 1501 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(3-butylheptyl)-4-pentylbenzamide
-
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(4-benzylpiperidin-1-yl)ethyl]-4-pentylbenzamide
-
IC50: 190 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 101 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 56 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
-
IC50: 1519 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dipropylamino)ethyl]-4-pentylbenzamide
-
IC50: 531 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
IC50:195 nM
N-[4-(2,2'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 587 nM; IC50: 736 nM
N-[4-(2,4'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 642 nM
N-[4-(3,3'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 5266 nM
N-[4-(3,4'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 4553 nM
N-[4-(3,4-diethylisoxazol-5-yl)benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[4-(4-benzylpiperazin-1-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 646 nM
N-[4-(benzylamino)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 429 nM
N-[4-(benzyloxy)benzyl]-4-butoxy-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0034 mM
N-[4-(benzyloxy)benzyl]-4-butyl-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0013 mM
N-[4-(benzyloxy)benzyl]-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 845 nM
N-[4-(benzyloxy)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 112 nM
N-[4-(benzyloxy)benzyl]-N-[2-(dibutylamino)ethyl]-4-propylbenzamide
-
IC50: 0.0089 mM
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-[[(1S)-3,3-difluoro-4,4-dihydroxycyclohexyl]methyl]-N-(4-pentylphenyl)naphthalene-2-carboxamide
-
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-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
N-[[5-(4-chlorophenyl)-1,2-oxazol-3-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-(3-bromophenyl)-N-[4-[(phenylsulfanyl)methyl]phenyl]-N2-(phenylsulfonyl)glycinamide
-
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-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
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)-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
-
-
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
-
-
[4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-yl]acetic acid
-
IC50: 197 nM
[4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetic acid
-
IC50: 463 nM
[5-([[(4-bromophenyl)carbonyl]oxy]methyl)-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
Ki value for human cathepsin D 0.165 mM
[5-[(benzoyloxy)methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
-
[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl 7aH-indole-3-carboxylate
Ki value for human cathepsin D above 0.1 mM
[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
Ki value for human cathepsin D 0.262 mM
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
Ki value for human cathepsin D 0.051 mM
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-1-ylacetate)
-
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-phenylacetamide)
-
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 143 nM
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 252 nM
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]-5-pentyl-N-[[4'-(piperidin-1-ylcarbonyl)biphenyl-4-yl]methyl]pyridine-2-carboxamide
-
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-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-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
additional information
-
none of the inhibitors analyzed to date have sufficient selectivity for plasmepsin I and II, compared to their human counterparts
-
additional information
-
single-digit nanomolar, low-molecular-weight inhibitors
-
additional information
-
plasmepsin is an important target for the development of antimalarial drugs, since its inhibition leads to the starvation of Plasmodium falciparum. A series of substrate-based dipeptide-type plasmepsin II inhibitors containing the hydroxymethylcarbonyl isostere as a transition-state mimic are synthesized
-
additional information
-
advances of computational approaches in inhibitor development
-
additional information
-
generation of an affinity matrix for purification of natural inhibitors by immobilization of the recombinant proenzyme to N-hydroxysuccinimide-activated Sepharose and the activation of the immobilized enzyme by incubation at pH 4.4 and 37°C. The matrices are useful in the affinity purification of the inhibitory activity detected in marine invertebrates, such as Xestospongia muta, giant barrel sponge, and the gorgonian seafan coral Plexaura homomalla, with increases of 10.2- and 5.9fold in the specific inhibitory activity, respectively
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