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Information on EC 3.4.23.B14 - plasmepsin IV
for references in articles please use BRENDA:EC3.4.23.B14preliminary BRENDA-supplied EC number
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3.4.23.B14 plasmepsin IVSpecify your search results
Word Map
- 3.4.23.B14
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plasmepsins
- plasmodium
- falciparum
- malaria
- vacuole
- hemoglobin
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antimalarial
- cathepsin
- vivax
- ovale
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intraerythrocytic
- medicine
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peptidomimetic
- berghei
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hydroxyethylamine
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allophenylnorstatine
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histo-aspartic
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proplasmepsins
- analysis
The expected taxonomic range for this enzyme is: Plasmodium
Reaction Schemes
cleavage of hemoglobin. In the S3 and S2 subsites, the plasmepsin 4 orthologs all prefer hydrophobic amino acid residues, Phe or Ile, but reject charged residues such as Lys or Asp. In S2' and S3' subsites these plasmepsins tolerate both hydrophobic and hydrophilic residues.
cleavage of hemoglobin. In the S3 and S2 subsites, the plasmepsin 4 orthologs all prefer hydrophobic amino acid residues, Phe or Ile, but reject charged residues such as Lys or Asp. In S2' and S3' subsites these plasmepsins tolerate both hydrophobic and hydrophilic residues
Synonyms
plasmepsin 4, pvpm4, plasmepsin iv, plm iv, pm iv, pfpm4, pmpm4, pm-iv, pgpm4, ppm iv, 
more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
A01.059
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PfPM4
plasmepsin 4
Plm IV
PM IV
PM4
PmPM4
PfPM4
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plasmepsin 4
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cleavage of hemoglobin. In the S3 and S2 subsites, the plasmepsin 4 orthologs all prefer hydrophobic amino acid residues, Phe or Ile, but reject charged residues such as Lys or Asp. In S2' and S3' subsites these plasmepsins tolerate both hydrophobic and hydrophilic residues
cleavage of hemoglobin. In the S3 and S2 subsites, the plasmepsin 4 orthologs all prefer hydrophobic amino acid residues, Phe or Ile, but reject charged residues such as Lys or Asp. In S2' and S3' subsites these plasmepsins tolerate both hydrophobic and hydrophilic residues.
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cleavage of hemoglobin. In the S3 and S2 subsites, the plasmepsin 4 orthologs all prefer hydrophobic amino acid residues, Phe or Ile, but reject charged residues such as Lys or Asp. In S2' and S3' subsites these plasmepsins tolerate both hydrophobic and hydrophilic residues
residues D34 and D214 form the catalytic dyad
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cleavage of hemoglobin. In the S3 and S2 subsites, the plasmepsin 4 orthologs all prefer hydrophobic amino acid residues, Phe or Ile, but reject charged residues such as Lys or Asp. In S2' and S3' subsites these plasmepsins tolerate both hydrophobic and hydrophilic residues
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
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CAS REGISTRY NUMBER
COMMENTARY
429673-77-8
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
denatured human hemoglobin + H2O
?
preferred over native human hemoglobin. PvPM4 acts synergistically with cysteine proteases vivapain-2 and vivapain-3 in the hydrolysis of hemoglobin
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EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH + H2O
?
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?
Lys-Pro-Ile-Gln-Phe-4-nitrophenylalanine-Arg-Leu + H2O
Lys-Pro-Ile-Gln-Phe + 4-nitrophenylalanine-Arg-Leu
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?
Lys-Pro-Ile-Glu-Phe-NO2Phe-Arg-Leu + H2O
Lys-Pro-Ile-Glu-Phe + NO2Phe-Arg-Leu
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?
Lys-Pro-Ile-Leu-Phe-4-nitrophenylalanine-Arg-Leu + H2O
Lys-Pro-Ile-Leu-Phe + 4-nitrophenylalanine-Arg-Leu
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?
haemoglobin + H2O
?
human haemoglobin. At pH 4.7, the enzyme is able to degrade hemoglobin so that no bands remain visible on SDS-PAGE. When excess of hemoglobin is used a 14000 Da band is detected, consistent with a cleavage of the alpha-globin chain at the Phe33-Leu34 bond in the hinge region of the molecule
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?
haemoglobin + H2O
?
human haemoglobin. The enzyme may play a crucial role in the critical process which yields nutrients from parasite growth, the enzyme may have the potential to initiate the vacuolar haemoglobin digestion pathway
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Hemoglobin + H2O
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the enzyme is involved in host hemoglobin degradation
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Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Nle-Phe + Phe(NO2)-Arg-Leu
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?
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Nle-Phe + Phe(NO2)-Arg-Leu
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?
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Nle-Phe + Phe(NO2)-Arg-Leu
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?
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Nle-Phe + Phe(NO2)-Arg-Leu
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?
additional information
?
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the enzyme cleaves preferably behind phenylalanine. The hydrolysis rates of the leucine and norleucine pools are 34% and 42% of that of the phenylalanine pool, respectively. In addition, no levels of hydrolysis are also detected for peptide pools containing four other P1 amino acid substitutes, asparagine (25%), glutamine (20%), tyrosine (18%) and tryptophan (17%). Hydrolyzed peptide products from the other 12 peptide pools, however, were barely detected
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?
additional information
?
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the plasmepsin 4 zymogen exhibits catalytic activity regardless of the presence of the pro-segment. Auto-maturation of the zymogen to mature enzyme is carried out at pH 4.5, 5.0, and 5.5
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?
additional information
?
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since plasmepsin IV clearly can cleave within the -Ser-(Phe/Leu)-Lys-Phe-Phe-Lys-(Ser/Thr)-Gly- sequence it may be possible that plasmepsin IV initiates cleavage of the proplasmepsin I precursor
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?
additional information
?
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since plasmepsin IV clearly can cleave within the -Ser-(Phe/Leu)-Lys-Phe-Phe-Lys-(Ser/Thr)-Gly- sequence it may be possible that plasmepsin IV initiates cleavage of the proplasmepsin I precursor
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?
additional information
?
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the four plasmepsins have overlapping roles in the hemoglobin degradation pathway
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?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
haemoglobin + H2O
?
human haemoglobin. The enzyme may play a crucial role in the critical process which yields nutrients from parasite growth, the enzyme may have the potential to initiate the vacuolar haemoglobin digestion pathway
-
-
?
additional information
?
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since plasmepsin IV clearly can cleave within the -Ser-(Phe/Leu)-Lys-Phe-Phe-Lys-(Ser/Thr)-Gly- sequence it may be possible that plasmepsin IV initiates cleavage of the proplasmepsin I precursor
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?
additional information
?
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since plasmepsin IV clearly can cleave within the -Ser-(Phe/Leu)-Lys-Phe-Phe-Lys-(Ser/Thr)-Gly- sequence it may be possible that plasmepsin IV initiates cleavage of the proplasmepsin I precursor
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?
additional information
?
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the four plasmepsins have overlapping roles in the hemoglobin degradation pathway
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?
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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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(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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(1Z)-(3,4-dimethoxyphenyl)-N'-[[(3,4,5-trichlorophenoxy)acetyl]oxy]ethanimidamide
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(2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R)-3-oxo-1-oxa-4-aza-cyclotridec-2-yl]butyramide
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(2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-aza-cyclo-tridec-11-en-2-yl]butyramide
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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-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)-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-6-oxo-1-oxa-7-aza-cyclohexadec-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
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(2R,3R,4R,5R,14E)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-14-ene-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]-3-methylbutanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]-3-methylpentanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]-3-phenylpropanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]-4-methylpentanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]-3-methylbutanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]-3-methylpentanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]-3-phenylpropanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]-4-methylpentanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-3-methylbutanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-3-methylpentanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-3-phenylpropanamide
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(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-4-methylpentanamide
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(2S)-N-[(2R,3S)-4-(1,4'-bipiperidin-1'-yl)-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanamide
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(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylbutanamide
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(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylpentanamide
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(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanamide
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(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-4-methylpentanamide
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(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylbutanamide]
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(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylpentanamide]
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(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanamide]
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(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-4-methylpentanamide]
-
-
(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
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
(4R)-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-N-(2-methylbenzyl)-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
-
-
(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
-
-
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(5-[[(1H-indol-3-ylacetyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
-
-
(5-[[(1H-indol-3-ylacetyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-nitrobenzoate
-
-
(5-[[(4-bromobenzoyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
-
-
(5-[[(phenylcarbonyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
-
-
(5-[[(phenylcarbonyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-nitrobenzoate
-
-
(6-[[(phenylcarbonyl)oxy]methyl]-2,5,6,7-tetrahydro-1H-azepin-4-yl)methyl 4-aminobenzoate
-
-
(6-[[(phenylcarbonyl)oxy]methyl]-2,5,6,7-tetrahydro-1H-azepin-4-yl)methyl 4-nitrobenzoate
-
-
(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
-
-
1-[3-chloro-6-(trifluoromethyl)phenanthren-9-yl]-3-(dibutylamino)propan-1-ol
-
i.e. halofantrine
1-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-(dibutylamino)ethanol
-
-
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-aminobenzoate)
-
-
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-nitrobenzoate)
-
-
2,3,4-trifluoro-N-([[1-(3-methylbutyl)piperidin-4-yl](4-pentylbenzoyl)amino]methyl)benzamide
-
-
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-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-[bis(4-methylpentyl)amino]-1-(1,2,3,4-tetrahydrophenanthren-9-yl)ethanol
-
-
3-amino-N-[(4S,6S,7S)-7-[[(2,6-dimethylphenoxy)acetyl]amino]-6-hydroxy-2-methyl-8-phenyloctan-4-yl]benzamide
-
-
4-(1-benzofuran-2-yl)-Na-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
4-amino-N'-(benzyloxy)-N-(2-methylphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N'-[(2,4-dichlorophenyl)methoxy]-N-(2-methylphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-[(4S,6S,7S)-7-[[(2,6-dimethylphenoxy)acetyl]amino]-6-hydroxy-2-methyl-8-phenyloctan-4-yl]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
-
-
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
-
-
di-tert-butyl [piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]biscarbamate
-
-
L-lysyl-L-prolyl-L-norleucyl-N-[(1S)-1-([[(1S)-1-[[(1S)-4-amino-1-[[(1R)-1-carboxy-2-methylbutyl]carbamoyl]pent-4-en-1-yl]carbamoyl]-3-methylbutyl]amino]methyl)pentyl]-L-serinamide
-
-
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
-
-
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl](4-pentylbenzoyl)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'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-phenylacetamide)
-
-
N-(3,4-dichlorophenyl)-2-[(4,6-dimethylpyrimidin-2-yl)amino]-3a,4,5,6,7,7a-hexahydro-1H-benzimidazole-1-carboxamide
-
-
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
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](3-phenylpropyl)amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
-
-
N-benzyl-2-bromo-N-[[4-([[2-(2,4-dichlorophenyl)ethyl][2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]amino]methyl)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-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(cyclohexa-1,3-dien-1-yloxy)acetyl]-L-valinamide
-
-
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-valinamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
N-[(3-ethyl-1,2-oxazol-5-yl)methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
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]-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-[[methyl(pyridin-3-yl)amino]methyl]-4-pentylbenzamide
-
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
-
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
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
-
-
N1-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-aspartamide
-
-
N2-(3-bromophenyl)-N-[4-[(phenylsulfanyl)methyl]phenyl]-N2-(phenylsulfonyl)glycinamide
-
-
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
tert-butyl [(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]carbamate
-
-
tert-butyl [(2R,3S)-4-(1,4'-bipiperidin-1'-yl)-3-hydroxy-1-phenylbutan-2-yl]carbamate
-
-
tert-butyl [(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]carbamate
-
-
tert-butyl [(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate
-
-
tert-butyl [(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate
-
-
[5-([[(4-bromophenyl)carbonyl]oxy]methyl)-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
-
-
[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 naphthalene-1-carboxylate
-
-
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl 4-bromobenzoate
-
-
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
-
-
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
-
-
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
pepstatin A
-
inhibits autocatalytic processing and proteolytic activity of plasmepsin IV
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
-
-
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
-
-
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
-
-
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
-
-
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
-
-
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
-
-
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
-
-
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
-
-
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
-
-
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
-
-
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
-
-
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
-
-
additional information
-
computer-aided design and synthesis of nonpeptidic plasmepsin II and IV inhibitors
-
additional information
-
pyrrolidine derivatives as plasmepsin inhibitors, binding mode analysis assisted by molecular dynamics simulations, for pyrrolidine-3,4-diester derivatives and a substituted 3,4-diaminopyrrolidine inhibitor by using a crystal structure of inhibitor-bound Plm II, PDB ID 1LEE, and for 3,4-bis(aminomethylene)pyrrolidines, docking studies and modelling, detailed overview. Opening of the S1 and S2 pockets suggests the design of inhibitors with extended P1 and P2' residues
-
additional information
-
peptidomimetic and natural product aspartic protease inhibitors, calpain inhibitors, and anti-PgPM4 monoclonal antibodies significantly reduce parasite infectivity for mosquitoes
-
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DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Infections
Distinct placental malaria pathology caused by different Plasmodium berghei lines that fail to induce cerebral malaria in the C57Bl/6 mouse.
Malaria
Activity and inhibition of plasmepsin IV, a new aspartic proteinase from the malaria parasite, Plasmodium falciparum.
Malaria
alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases.
Malaria
Apical surface expression of aspartic protease Plasmepsin 4, a potential transmission-blocking target of the plasmodium ookinete.
Malaria
Enzymatic Characterization of Recombinant Food Vacuole Plasmepsin 4 from the Rodent Malaria Parasite Plasmodium berghei.
Malaria
Inhibitor binding to the plasmepsin IV aspartic protease from Plasmodium falciparum.
Malaria
Plasmepsin 4-deficient Plasmodium berghei are virulence attenuated and induce protective immunity against experimental malaria.
Malaria
Structure of the aspartic protease plasmepsin 4 from the malarial parasite Plasmodium malariae bound to an allophenylnorstatine-based inhibitor.
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0038
Lys-Pro-Ile-Gln-Phe-4-nitrophenylalanine-Arg-Leu
-
at pH 5.5 and 37°C
0.0021
Lys-Pro-Ile-Leu-Phe-4-nitrophenylalanine-Arg-Leu
-
at pH 5.5 and 37°C
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
24.5
Lys-Pro-Ile-Gln-Phe-4-nitrophenylalanine-Arg-Leu
-
at pH 5.5 and 37°C
34.9
Lys-Pro-Ile-Leu-Phe-4-nitrophenylalanine-Arg-Leu
-
at pH 5.5 and 37°C
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kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
6400
Lys-Pro-Ile-Gln-Phe-4-nitrophenylalanine-Arg-Leu
-
at pH 5.5 and 37°C
16500
Lys-Pro-Ile-Leu-Phe-4-nitrophenylalanine-Arg-Leu
-
at pH 5.5 and 37°C
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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000035
(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
-
-
0.0002
(2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R)-3-oxo-1-oxa-4-aza-cyclotridec-2-yl]butyramide
-
-
0.0068
(2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-aza-cyclo-tridec-11-en-2-yl]butyramide
-
-
0.000397
(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
-
-
0.01
(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
-
-
0.012
(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
-
-
0.002
(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
-
-
0.0012
(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
-
-
0.014
(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
-
-
0.000478
(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
-
-
0.002
(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
-
-
0.0022
(2R,3R,4R,5R)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
-
-
0.002
(2R,3R,4R,5R,14E)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-14-ene-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
-
-
0.0274
(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylpentanamide
-
at pH 4.5, temperature not specified in the publication
0.0033
(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylbutanamide]
-
at pH 4.5, temperature not specified in the publication
0.05
(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylpentanamide]
-
at pH 4.5, temperature not specified in the publication
0.05
(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-4-methylpentanamide]
-
at pH 4.5, temperature not specified in the publication
0.00000052
(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
-
-
0.000017 - 0.0013
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
0.00011
(4R)-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-N-(2-methylbenzyl)-1,3-thiazolidine-4-carboxamide
-
-
0.000015
(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
-
-
0.00074
(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
-
-
0.003
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.0159
(5-[[(1H-indol-3-ylacetyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
-
plasmepsin IV
0.0434
(5-[[(1H-indol-3-ylacetyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-nitrobenzoate
-
plasmepsin IV
0.0072
(5-[[(phenylcarbonyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
-
plasmepsin IV
0.0386
(5-[[(phenylcarbonyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-nitrobenzoate
-
plasmepsin IV
0.0099
(6-[[(phenylcarbonyl)oxy]methyl]-2,5,6,7-tetrahydro-1H-azepin-4-yl)methyl 4-aminobenzoate
-
plasmepsin IV
0.029
(6-[[(phenylcarbonyl)oxy]methyl]-2,5,6,7-tetrahydro-1H-azepin-4-yl)methyl 4-nitrobenzoate
-
plasmepsin IV
0.000023
(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
-
-
0.0032
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-aminobenzoate)
-
plasmepsin IV
0.0221
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-nitrobenzoate)
-
plasmepsin IV
0.211
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl dibenzoate
-
plasmepsin IV
0.000041
4-(1-benzofuran-2-yl)-Na-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.000022
L-lysyl-L-prolyl-L-norleucyl-N-[(1S)-1-([[(1S)-1-[[(1S)-4-amino-1-[[(1R)-1-carboxy-2-methylbutyl]carbamoyl]pent-4-en-1-yl]carbamoyl]-3-methylbutyl]amino]methyl)pentyl]-L-serinamide
-
-
0.000000026
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
-
-
0.000375
Lys-Pro-norleucine-Ser-norleucine-CH2-NH-Leu-Gln-Ile
-
at pH 5.0 and 37°C
0.00005
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
pH 4.7
0.0000014 - 0.00026
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
0.0000006 - 0.000021
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.000002 - 0.00003
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
0.00016
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(cyclohexa-1,3-dien-1-yloxy)acetyl]-L-valinamide
-
-
0.000025 - 0.003
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-valinamide
0.0000007 - 0.000058
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
0.0000003 - 0.00025
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
0.0000005 - 0.000038
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.00000009 - 0.000017
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.0000045 - 0.000044
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
0.00000024 - 0.0000025
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
0.0000005 - 0.00001
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.000707
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
-
0.0000021 - 0.00016
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.00000014 - 0.000006
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
0.0071
N1-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-aspartamide
-
-
0.0000015 - 0.000087
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
0.0000014 - 0.000019
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
0.00000029 - 0.00052
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
0.0057
[5-([[(4-bromophenyl)carbonyl]oxy]methyl)-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
-
plasmepsin IV
0.0015
[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
plasmepsin IV
0.0688
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl 4-bromobenzoate
-
plasmepsin IV
0.0039
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
plasmepsin IV
0.000017
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
-
37°C, pH 4.4
0.000019
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
-
37°C, pH 4.4
0.00099
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
-
37°C, pH 4.4
0.0013
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-([N-[(naphthalen-2-yloxy)acetyl]isoleucyl]amino)heptanamide
-
37°C, pH 4.4
0.00000011
Lys-Pro-Ile-Glu-Phe-Phe-Ala-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000021
Lys-Pro-Ile-Glu-Phe-Phe-Ala-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000025
Lys-Pro-Ile-Glu-Phe-Phe-Ala-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.0000022
Lys-Pro-Ile-Glu-Phe-Phe-Ala-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000053
Lys-Pro-Ile-Ile-Phe-Phe-Arg-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.0000012
Lys-Pro-Ile-Ile-Phe-Phe-Arg-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.0000055
Lys-Pro-Ile-Ile-Phe-Phe-Arg-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.0000058
Lys-Pro-Ile-Ile-Phe-Phe-Arg-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000006
Lys-Pro-Ile-Nle-Phe-Phe-Arg-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.000000083
Lys-Pro-Ile-Nle-Phe-Phe-Arg-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000019
Lys-Pro-Ile-Nle-Phe-Phe-Arg-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000041
Lys-Pro-Ile-Nle-Phe-Phe-Arg-Leu
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000014
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Arg
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000021
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Arg
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000024
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Arg
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.0000006
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Arg
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.000000026
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Ser
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000008
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Ser
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.0000001
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Ser
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00000071
Lys-Pro-Phe-Nle-Phe-Phe-Ser-Ser
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.0000014
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
-
37°C, pH 4.4
0.000047
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
-
37°C, pH 4.4
0.00026
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucine
-
37°C, pH 4.4
0.0000006
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.0000015
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.0000017
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.000021
N-([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.000002
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
37°C, pH 4.4
0.000003
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
37°C, pH 4.4
0.0000052
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
37°C, pH 4.4
0.00003
N-[(1R)-1-[[(1S,2S)-4-[[(1S)-5-amino-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)pentyl]amino]-1-benzyl-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
37°C, pH 4.4
0.000025
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-valinamide
-
-
0.003
N-[(1S,2S)-1-benzyl-3-[(4R)-4-(tert-butylcarbamoyl)-5,5-dimethyl-1,3-thiazolidin-3-yl]-2-hydroxy-3-oxopropyl]-N2-[(isoquinolin-5-yloxy)acetyl]-L-valinamide
-
-
0.0000007
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
-
37°C, pH 4.4
0.0000022
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
-
37°C, pH 4.4
0.000003
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
-
37°C, pH 4.4
0.000058
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-([4-[4-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)phenoxy]phenyl]carbonyl)isoleucinamide
-
37°C, pH 4.4
0.0000003
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
-
37°C, pH 4.4
0.000015
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
-
37°C, pH 4.4
0.000021
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
-
37°C, pH 4.4
0.00025
N-[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]-N2-[[4-(4-[[(1R)-1-([4-[(6-methoxyquinolin-8-yl)amino]pentyl]carbamoyl)-3-methylbutyl]carbamoyl]phenoxy)phenyl]carbonyl]isoleucinamide
-
37°C, pH 4.4
0.0000005
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.000016
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.000029
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.000038
N-[(4-[2-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-2-oxoethyl]phenyl)acetyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.00000009
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.00000028
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.0000012
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.000017
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-alanyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.0000045
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
-
-
0.00001
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
-
-
0.000039
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
-
-
0.000044
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucine
-
-
0.00000024
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
-
37°C, pH 4.4
0.00000051
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
-
37°C, pH 4.4
0.00000051
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
-
37°C, pH 4.4
0.0000025
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-alaninamide
-
37°C, pH 4.4
0.0000005
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.0000012
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.0000012
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.00001
N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.0000021
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.000014
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.00012
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.00016
N-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)amino]-4-oxobutanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
37°C, pH 4.4
0.00000014
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
0.0000002
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
0.0000004
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
0.000006
N-[4-[([6-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]naphthalen-2-yl]carbonyl)oxy]butanoyl]-L-leucyl-N-[4-[(6-methoxyquinolin-8-yl)amino]pentyl]-L-lysinamide
-
-
0.0000015
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
-
37°C, pH 4.4
0.000011
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
-
37°C, pH 4.4
0.000017
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
-
37°C, pH 4.4
0.000087
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-L-lysinate
-
37°C, pH 4.4
0.0000014
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
-
37°C, pH 4.4
0.000002
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
-
37°C, pH 4.4
0.000004
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
-
37°C, pH 4.4
0.000019
propyl N-[(4-[4-[(1-[[(1S,2S)-4-(butylamino)-2-hydroxy-1-(2-methylpropyl)-4-oxobutyl]carbamoyl]-2-methylbutyl)carbamoyl]phenoxy]phenyl)carbonyl]-L-leucyl-N6-(tert-butoxycarbonyl)-L-lysinate
-
37°C, pH 4.4
0.00000029
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.0000007
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.000001
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
0.00052
tert-butyl [(1S)-1-[[(3S,7S,10S,19S)-19-[(2-amino-2-oxoethyl)carbamoyl]-7-benzyl-6-hydroxy-3-(1-methylethyl)-2,9,16-trioxo-1,4,8,15-tetraazacyclononadecan-10-yl]carbamoyl]-2-methylpropyl]carbamate
-
37°C, pH 4.4, substrate: KPIEFF(NO2)RL
additional information
additional information
the Ki-value for isobutyl-Val-Val-Sta-Ala-Sta is below 0.1 nM
-
additional information
additional information
-
the Ki-value for isobutyl-Val-Val-Sta-Ala-Sta is below 0.1 nM
-
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000018
(1R,2R,3R,4S,5R)-5-[(cyclobutylamino)methyl]-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.000011
(1R,2R,3R,4S,5R)-5-[(cyclopentylamino)methyl]-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.000228
(1R,2R,3R,4S,6R)-6-[(cyclobutylamino)methyl]-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.000139
(1R,2R,3R,4S,6R)-6-[(cyclopentylamino)methyl]-N-(naphthalen-2-ylmethyl)-3-[(4-pentylphenyl)sulfonyl]-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.07
(1R,4S)-6-[2-(1,3-benzothiazol-2-ylsulfanyl)ethoxy]-7-(naphthalen-1-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.085
(1R,4S)-6-[2-(1,3-benzothiazol-2-ylsulfanyl)ethoxy]-7-(naphthalen-2-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.06
(1R,4S)-6-[2-(1,3-benzothiazol-2-ylsulfanyl)ethoxy]-7-[2-(naphthalen-1-yl)ethoxy]-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.017
(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
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.05
(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
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.015
(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
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.033
(1R,4S)-6-[3-(1,3-benzothiazol-2-ylsulfanyl)propyl]-7-(naphthalen-1-ylmethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.01
(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
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.073
(1S)-3,3-difluoro-4,4-dihydroxy-N-(naphthalen-2-ylmethyl)-N-(4-pentylphenyl)cyclohexanecarboxamide
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.00458
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]-3-methylbutanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00633
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]-3-methylpentanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00341
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]-3-phenylpropanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00461
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-3-hydroxy-4-(4-methylpiperazin-1-yl)-1-phenylbutan-2-yl]-4-methylpentanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.0038
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]-3-methylbutanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00437
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]-3-methylpentanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00296
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]-3-phenylpropanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00213
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]-4-methylpentanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00459
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-3-methylbutanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00336
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-3-methylpentanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00133
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-3-phenylpropanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00527
(2S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-[(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-4-methylpentanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00854
(2S)-N-[(2R,3S)-4-(1,4'-bipiperidin-1'-yl)-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00125
(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylbutanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00328
(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylpentanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00314
(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00696
(2S)-N-[(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-4-methylpentanamide
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00728
(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylbutanamide]
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00324
(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-methylpentanamide]
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.0013
(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanamide]
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00512
(2S,2'S)-N,N'-[piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]bis[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-4-methylpentanamide]
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.0412
(3S,4S)-pyrrolidine-3,4-diyl bis(3,3-dimethylbutanoate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.168
(3S,4S)-pyrrolidine-3,4-diyl bis(3-methylbutanoate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0008
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-2-ylacetate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0074
(3S,4S)-pyrrolidine-3,4-diyl bis(phenylacetate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.134
(3S,4S)-pyrrolidine-3,4-diyl dicyclohexanecarboxylate
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0094
(5-[[(4-bromobenzoyl)oxy]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl)methyl 4-aminobenzoate
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.005
1-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-(dibutylamino)ethanol
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.021
2-(dihexylamino)-1-(1,2,3,4-tetrahydrophenanthren-9-yl)ethanol
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.039
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
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.009
2-[bis(4-methylpentyl)amino]-1-(1,2,3,4-tetrahydrophenanthren-9-yl)ethanol
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.00311
di-tert-butyl [piperazine-1,4-diylbis[(2R,3S)-3-hydroxy-1-phenylbutane-4,2-diyl]]biscarbamate
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00035
N-benzyl-2-bromo-N-[[4-([[2-(2,4-dichlorophenyl)ethyl](3-phenylpropyl)amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.00018
N-benzyl-2-bromo-N-[[4-([[2-(2,4-dichlorophenyl)ethyl][2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.00058
N-benzyl-2-bromo-N-[[4-([[3-(2,4-dichlorophenyl)propyl](3-phenylpropyl)amino]methyl)pyrrolidin-3-yl]methyl]-4,5-dimethoxybenzamide
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.0003
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
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.057
N-[[(1S)-3,3-difluoro-4,4-dihydroxycyclohexyl]methyl]-N-(4-pentylphenyl)naphthalene-2-carboxamide
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.00116
tert-butyl [(2R,3S)-4-(1,4'-bipiperidin-1'-yl)-3-hydroxy-1-phenylbutan-2-yl]carbamate
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.0054
tert-butyl [(2R,3S)-4-(4-ethylpiperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl]carbamate
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.0049
tert-butyl [(2R,3S)-4-[4-(4-bromobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.00256
tert-butyl [(2R,3S)-4-[4-(4-fluorobenzyl)piperazin-1-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate
Plasmodium falciparum
-
at pH 4.5, temperature not specified in the publication
0.0118
[5-[(benzoyloxy)methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.00009
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-1-ylacetate)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0013
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-1-ylacetate)
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.0538
(3S,4S)-pyrrolidine-3,4-diyl dibenzoate
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0884
(3S,4S)-pyrrolidine-3,4-diyl dibenzoate
Plasmodium falciparum
-
pH and temperature not specified in the publication
0.0015
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-phenylacetamide)
Plasmodium falciparum
-
pH not specified in the publication, temperature not speficied in the publication
0.0025
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-phenylacetamide)
Plasmodium falciparum
-
pH and temperature not specified in the publication
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5
-
the mature enzyme shows highest catalytic activity at pH 5.0 and pH 5.5 with a 5 min pre-incubation
5.5
-
the zymogen shows highest catalytic activity at pH 5.0 and pH 5.5 with a 5 min pre-incubation
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
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TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
-
brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
a fertilized zygote capable of moving spontaneously, the enzyme is located at the apical surface
brenda
additional information
-
presence of PgPM4 in the different life cycle stages, e.g. in asexual blood stage, overview
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
additional information
-
co-localization of PgPM4 with chitinase, PgCHT2
-
brenda
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
PM4 deficiency results in significantly less virulence than that for the parental parasite. Enzyme-deficient parasites fail to induce experimental cerebral malaria in susceptible mice, and resistant mice are able to clear infections
physiological function
physiological function
-
the enzyme is involved in host hemoglobin degradation
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UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). O60990_PLAMA
451
0
51809
TrEMBL
other Location (Reliability: 2)
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37000
x * 44000, SDs-PAGE of preprotein, x * 37000, SDS-PAGE of mature protein
44000
x * 44000, SDs-PAGE of preprotein, x * 37000, SDS-PAGE of mature protein
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
x * 44000, SDs-PAGE of preprotein, x * 37000, SDS-PAGE of mature protein
monomer
additional information
-
PSM4 is unusable for structural studies by hydrogen/deuterium exchange coupled to mass spectrometry, DXMS, since the method requires the use of proteases working at acidic pH and low temperatures
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
proteolytic modification
proteolytic modification
incubation of the 44000 Da proplasmepsin IV at pH 4.7 results in its conversion to a protein of 38000 Da. Autoactivation site in proplasmepsin IV -KESFKF-/-F-/-KSGYAQ-
proteolytic modification
-
processing of plasmepsin II and plasmepsin IV occurs via an intra- and inter-molecular autocatalytic event as well as via a transcatalytic event between them
proteolytic modification
-
maturation of PSM4 is efficient after 5 min at pH 4.5 and 37°C, PSM4 is partly cleaved after Phe109, Phe110, or Phe81 leading to proteins of 38218 Da, 38071 Da, and 41508 Da, respectively, cleavage is not terminated after 7 h
proteolytic modification
processing of PM4 into a mature enzyme occurrs through autocatalytic activity under acidic conditions in a pepstatin A-sensitive manner, in which process a portion of prodomain is essential for correct folding. Cysteine proteases vivapain-2 and vivapain-3 mediate the processing of PvPM4 into a mature enzyme
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CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
hanging-drop vapor-diffusion method, crystals of PmPM4 in complex with the small-molecule inhibitor AG1776. The crystals are orthorhombic, with space group P2(1)2(1)2 and unit-cell parameters a = 95.88 A, b = 112.58 A, c = 90.40 A, two molecules per asymmetric unit
-
truncated proplasmepsin IV, sitting drop vapor diffusion method, using 100 mM sodium citrate pH 4.7, 25% (w/v) PEG 3350, 200 mM ammonium acetate
hanging-drop vapor-diffusion method, crystal structure of plasmepsin 4 bound to the allophenylnorstatine-based compound KNI-764 at 3.3 A resolution. The PmPM4inhibitor complex crystallized in the ortho-rhombic space group P2(1)2(1)2, with unit-cell parameters a = 95.9 A, b = 112.6 A, c = 90.4 A, with two molecules in the asymmetric unit
-
pKa calculations for PM IV complexed with the inhibitor KNI-764. Residue Asp214 is protonated, while residue Asp34 is deprotonated. In the colmplex, the hydroxyl group interacts with the OD2 oxygen atom of Asp34 through a hydrogen bond. The hydroxyl group also presents a hydrogen bond interaction with acid aspartic protonated Asp214. The amino groups of Gly78 and Ser79 residues interact with KNI-764 forming hydrogen bonds at 2.02 and 2.20 A. The hydroxyl group of Thr217 forms hydrogen bonds with the inhibitor at 2.06 A
analysis of 3D model of PM4 shows a typical aspartic protease structure with bi-lobed, compact and distinct peptide binding cleft
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
construction of 1092cl4 and 1092cl6, two parasite lines deficient in expressing PM4, by gene disruption, and of mutant lines 688cl2 and 688cl3. PM4 deficiency results in significantly less virulence than that for the parental parasite. Enzyme-deficient parasites fail to induce experimental cerebral malaria in susceptible mice, and resistant mice are able to clear infections. The mutant acts as vaccine, immunity through antibody-mediated parasite clearance in the spleen, virulence-attenuated phenotypes, overview
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pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5 - 5.5
-
the enzyme shows 75-90% of the maximal catalytic activity within 30 min pre-incubation at pH 5.0-5.5
755107
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TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli
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RENATURED/Commentary
ORGANISM
UNIPROT
LITERATURE
bacterially expressed recombinant PvPM4 is insoluble, but it is easily refolded into a soluble protein
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
analysis
-
PSM4 is unusable for structural studies by hydrogen/deuterium exchange coupled to mass spectrometry, DXMS, since the method requires the use of proteases working at acidic pH and low temperatures, in contrast to PSM2, EC 3.4.23.39
medicine
medicine
plasmepsin IV appears to be a potential target for the development of new antiparasitic drugs. Plasmepsin I, II and IV might act in concert. While this might suggest that inhibition of individual enzymes might be insufficient to kill the parasite, the broad similarities between the plasmepsins may permit the development of compunds able to inhibit all three enzymes to produce a drug capable of imposing a multiple blockade on the pathway of haemoglobin digestion
medicine
-
plasmepsin 4 is the food vacuole plasmepsin present in all four Plasmodium spp. infecting man, and the only food vacuole plasmepsin in three of the four species. For this reason it represents a potential antimalarial drug target against which one drug may control infections by any of the four species
medicine
-
plasmepsin 4 is the food vacuole plasmepsin present in all four Plasmodium spp. infecting man, and the only food vacuole plasmepsin in three of the four species. For this reason it represents a potential antimalarial drug target against which one drug may control infections by any of the four species
medicine
-
plasmepsin 4 is the food vacuole plasmepsin present in all four Plasmodium spp. infecting man, and the only food vacuole plasmepsin in three of the four species. For this reason it represents a potential antimalarial drug target against which one drug may control infections by any of the four species
medicine
-
plasmepsin 4 is the food vacuole plasmepsin present in all four Plasmodium spp. infecting man, and the only food vacuole plasmepsin in three of the four species. For this reason it represents a potential antimalarial drug target against which one drug may control infections by any of the four species
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REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Wyatt, D.M.; Berry, C.
Activity and inhibition of plasmepsin IV, a new aspartic proteinase from the malaria parasite, Plasmodium falciparum
FEBS Lett.
513
159-162
2002
Plasmodium falciparum (Q8IM16), Plasmodium falciparum
brenda
Dame, J.B.; Yowell, C.A.; Omara-Opyene, L.; Carlton, J.M.; Cooper, R.A.; Li, T.
Plasmepsin 4, the food vacuole aspartic proteinase found in all Plasmodium spp. Infecting man
Mol. Biochem. Parasitol.
130
1-12
2003
Plasmodium falciparum (Q8IM16), Plasmodium falciparum
brenda
Nezami, A.; Kimura, T.; Hidaka, K.; Kiso, A.; Liu, J.; Kiso, Y.; Goldberg, D.E.; Freire, E.
High-affinity inhibition of a family of Plasmodium falciparum proteases by a designed adaptive inhibitor
Biochemistry
42
8459-8464
2003
Plasmodium falciparum (Q8IM16), Plasmodium falciparum
brenda
Clemente, J.C.; Govindasamy, L.; Madabushi, A.; Fisher, S.Z.; Moose, R.E.; Yowell, C.A.; Hidaka, K.; Kimura, T.; Hayashi, Y.; Kiso, Y.; Agbandje-McKenna, M.; Dame, J.B.; Dunn, B.M.; McKenna, R.
Structure of the aspartic protease plasmepsin 4 from the malarial parasite Plasmodium malariae bound to an allophenylnorstatine-based inhibitor
Acta Crystallogr. Sect. D
D62
246-252
2006
Plasmodium malariae
brenda
Madabushi, A.; Chakraborty, S.; Fisher, S.Z.; Clemente, J.C.; Yowell, C.; Agbandje-McKenna, M.; Dame, J.B.; Dunn, B.M.; McKenna, R.
Crystallization and preliminary X-ray analysis of the aspartic protease plasmepsin 4 from the malarial parasite Plasmodium malariae
Acta Crystallogr. Sect. F
61
228-231
2005
Plasmodium falciparum
brenda
Andrews, K.T.; Fairlie, D.P.; Madala, P.K.; Ray, J.; Wyatt, D.M.; Hilton, P.M.; Melville, L.A.; Beattie, L.; Gardiner, D.L.; Reid, R.C.; Stoermer, M.J.; Skinner-Adams, T.; Berry, C.; McCarthy, J.S.
Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria
Antimicrob. Agents Chemother.
50
639-648
2006
Plasmodium falciparum
brenda
Gutierrez-de-Teran, H.; Nervall, M.; Ersmark, K.; Liu, P.; Janka, L.K.; Dunn, B.; Hallberg, A.; Aqvist, J.
Inhibitor binding to the plasmepsin IV aspartic protease from Plasmodium falciparum
Biochemistry
45
10529-10541
2006
Plasmodium falciparum
brenda
Ersmark, K.; Nervall, M.; Gutierrez-de-Teran, H.; Hamelink, E.; Janka, L.K.; Clemente, J.C.; Dunn, B.M.; Gogoll, A.; Samuelsson, B.; Qvist, J.; Hallberg, A.
Macrocyclic inhibitors of the malarial aspartic proteases plasmepsin I, II, and IV
Bioorg. Med. Chem.
14
2197-2208
2006
Plasmodium falciparum
brenda
Kim, Y.M.; Lee, M.H.; Piao, T.G.; Lee, J.W.; Kim, J.H.; Lee, S.; Choi, K.M.; Jiang, J.H.; Kim, T.U.; Park, H.
Prodomain processing of recombinant plasmepsin II and IV, the aspartic proteases of Plasmodium falciparum, is auto- and trans-catalytic
J. Biochem.
139
189-195
2006
Plasmodium falciparum
brenda
Liu, J.; Gluzman, I.Y.; Drew, M.E.; Goldberg, D.E.
The role of Plasmodium falciparum food vacuole plasmepsins
J. Biol. Chem.
280
1432-1437
2005
Plasmodium falciparum
brenda
Ersmark, K.; Samuelsson, B.; Hallberg, A.
Plasmepsins as potential targets for new antimalarial therapy
Med. Res. Rev.
26
626-666
2006
Plasmodium falciparum
brenda
Li, T.; Yowell, C.A.; Beyer, B.B.; Hung, S.H.; Westling, J.; Lam, M.T.; Dunn, B.M.; Dame, J.B.
Recombinant expression and enzymatic subsite characterization of plasmepsin 4 from the four Plasmodium species infecting man
Mol. Biochem. Parasitol.
135
101-109
2004
Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale
brenda
Luksch, T.; Chan, N.S.; Brass, S.; Sotriffer, C.A.; Klebe, G.; Diederich, W.E.
Computer-aided design and synthesis of nonpeptidic plasmepsin II and IV inhibitors
ChemMedChem
3
1323-1336
2008
Plasmodium falciparum
brenda
Janka, L.; Clemente, J.; Vaiana, N.; Sparatore, A.; Romeo, S.; Dunn, B.M.
Targeting the plasmepsin 4 orthologs of Plasmodium sp. with "double drug" inhibitors
Protein Pept. Lett.
15
868-873
2008
Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale
brenda
Spaccapelo, R.; Janse, C.J.; Caterbi, S.; Franke-Fayard, B.; Bonilla, J.A.; Syphard, L.M.; Di Cristina, M.; Dottorini, T.; Savarino, A.; Cassone, A.; Bistoni, F.; Waters, A.P.; Dame, J.B.; Crisanti, A.
Plasmepsin 4-deficient Plasmodium berghei are virulence attenuated and induce protective immunity against experimental malaria
Am. J. Pathol.
176
205-217
2010
Plasmodium berghei
brenda
Luksch, T.; Blum, A.; Klee, N.; Diederich, W.E.; Sotriffer, C.A.; Klebe, G.
Pyrrolidine derivatives as plasmepsin inhibitors: binding mode analysis assisted by molecular dynamics simulations of a highly flexible protein
ChemMedChem
5
443-454
2010
Plasmodium falciparum
brenda
Marcoux, J.; Thierry, E.; Vives, C.; Signor, L.; Fieschi, F.; Forest, E.
Investigating alternative acidic proteases for H/D exchange coupled to mass spectrometry: plasmepsin 2 but not plasmepsin 4 is active under quenching conditions
J. Am. Soc. Mass Spectrom.
21
76-79
2010
Plasmodium falciparum
brenda
Li, F.; Patra, K.P.; Yowell, C.A.; Dame, J.B.; Chin, K.; Vinetz, J.M.
Apical surface expression of aspartic protease plasmepsin 4, a potential transmission-blocking target of the Plasmodium ookinete
J. Biol. Chem.
285
8076-8083
2010
Plasmodium gallinaceum
brenda
Silva, N.; Lameira, J.; Alves, C.
A quantum mechanical/molecular mechanical study of the aspartic protease plasmepsin IV complexed with allophenylnorstatine-based inhibitor
Chem. Phys. Lett.
509
169-174
2011
Plasmodium malariae (O60990)
-
brenda
Moon, S.U.; Kang, J.M.; Kim, T.S.; Kong, Y.; Sohn, W.M.; Na, B.K.
Plasmodium vivax: collaborative roles for plasmepsin 4 and vivapains in hemoglobin hydrolysis
Exp. Parasitol.
128
127-132
2011
Plasmodium vivax (O60989), Plasmodium vivax
brenda
Rawat, M.; Vijay, S.; Gupta, Y.; Dixit, R.; Tiwari, P.K.; Sharma, A.
Sequence homology and structural analysis of plasmepsin 4 isolated from Indian Plasmodium vivax isolates
Infect. Genet. Evol.
11
924-933
2011
Plasmodium vivax (D4P4R3), Plasmodium vivax
brenda
Recacha, R.; Jaudzems, K.; Akopjana, I.; Jirgensons, A.; Tars, K.
Crystal structure of Plasmodium falciparum proplasmepsin IV the plasticity of proplasmepsins
Acta Crystallogr. Sect. F
72
659-666
2016
Plasmodium falciparum (Q8IM16), Plasmodium falciparum
brenda
Mishra, V.; Rathore, I.; Arekar, A.; Sthanam, L.K.; Xiao, H.; Kiso, Y.; Sen, S.; Patankar, S.; Gustchina, A.; Hidaka, K.; Wlodawer, A.; Yada, R.Y.; Bhaumik, P.
Deciphering the mechanism of potent peptidomimetic inhibitors targeting plasmepsins - biochemical and structural insights
FEBS J.
285
3077-3096
2018
Plasmodium falciparum
brenda
Huizing, A.P.; Mondal, M.; Hirsch, A.K.
Fighting malaria structureguided discovery of nonpeptidomimetic plasmepsin inhibitors
J. Med. Chem.
58
5151-5163
2015
Plasmodium falciparum
brenda
Rasina, D.; Otikovs, M.; Leitans, J.; Recacha, R.; Borysov, O.V.; Kanepe-Lapsa, I.; Domraceva, I.; Pantelejevs, T.; Tars, K.; Blackman, M.J.; Jaudzems, K.; Jirgensons, A.
Fragment-based discovery of 2-aminoquinazolin-4(3H)-ones as novel class nonpeptidomimetic inhibitors of the plasmepsins I, II, and IV
J. Med. Chem.
59
374-387
2016
Plasmodium falciparum (Q8IM16)
brenda
Singh, A.K.; Rathore, S.; Tang, Y.; Goldfarb, N.E.; Dunn, B.M.; Rajendran, V.; Ghosh, P.C.; Singh, N.; Latha, N.; Singh, B.K.; Rawat, M.; Rathi, B.
Hydroxyethylamine based phthalimides as new class of plasmepsin hits design, synthesis and antimalarial evaluation
PLoS ONE
10
e0139347
2015
Plasmodium falciparum
brenda
Liu, P.; Robbins, A.H.; Marzahn, M.R.; McClung, S.H.; Yowell, C.A.; Stevens, S.M.; Dame, J.B.; Dunn, B.M.
Enzymatic characterization of recombinant food vacuole plasmepsin 4 from the rodent malaria parasite Plasmodium berghei
PLoS ONE
10
e0141758
2015
Plasmodium berghei
brenda
McGillewie, L.; Soliman, M.E.
Flap flexibility amongst plasmepsins I, II, III, IV, and V Sequence, structural, and molecular dynamics analyses
Proteins
83
1693-1705
2015
Plasmodium falciparum (Q8IM16), Plasmodium falciparum
brenda
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