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Information on EC 3.4.23.38 - plasmepsin I and Organism(s) Plasmodium falciparum and UniProt Accession P39898

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     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.23 Aspartic endopeptidases
                3.4.23.38 plasmepsin I
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Select one or more organisms in this record:
This record set is specific for:
Plasmodium falciparum
UNIPROT: P39898 not found.
Word Map
The expected taxonomic range for this enzyme is: Plasmodium falciparum
The taxonomic range for the selected organisms is: Plasmodium falciparum
Reaction Schemes
hydrolysis of the -Phe33-/-Leu- bond in the alpha-chain of hemoglobin, leading to denaturation of the molecule
Synonyms
AH I, aspartic hemoglobinase I, malaria aspartic hemoglobinase, PFAPG, PfPM1, plasmepsin I, PLm I, PM I, PMI, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
AH I
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aspartic hemoglobinase I
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malaria aspartic hemoglobinase
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PFAPG
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plasmepsin I
1455
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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-
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PATHWAY SOURCE
PATHWAYS
CAS REGISTRY NUMBER
COMMENTARY hide
180189-87-1
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SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe + H2O
Leu-Glu-Arg-Ile-Phe + (p-nitro)Phe-Ser-Phe
show the reaction diagram
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-
-
-
?
Lys-Glu-Leu-Val-Phe-(p-nitro)Phe-Ala-Leu-Lys + H2O
Lys-Glu-Leu-Val-Phe + (p-nitro)Phe-Ala-Leu-Lys
show the reaction diagram
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-
-
-
?
Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu + H2O
Lys-Pro-Ile-Leu-Phe + (p-nitro)Phe-Arg-Leu
show the reaction diagram
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-
-
-
?
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Met-Phe + Leu-Ser-Phe-Pro-(gamma-aminobutyryl)-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid + H2O
?
show the reaction diagram
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-
-
-
?
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid + H2O
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Nle-Phe + Leu-Ser-Phe-Pro-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
show the reaction diagram
-
-
-
-
?
Ala-Leu-Glu-Arg-Thr-Phe-Leu-Ser-Phe-Pro-Thr + H2O
Ala-Leu-Glu-Arg-Thr-Phe + Leu-Ser-Phe-Pro-Thr
show the reaction diagram
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-
-
-
?
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH + H2O
?
show the reaction diagram
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-
?
Hemoglobin + H2O
?
show the reaction diagram
hemoglobin alpha-chain + H2O
?
show the reaction diagram
hemoglobin beta-chain + H2O
?
show the reaction diagram
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cleavage sites: Leu31-/-Leu32, Phe41-/-Phe43, Ala129-/-Tyr130
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-
?
human hemoglobin + H2O
?
show the reaction diagram
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-
?
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe + H2O
Leu-Glu-Arg-Ile-Phe + Phe(NO2)-Ser-Phe
show the reaction diagram
Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe + H2O
Leu-Glu-Arg-Val-Phe + Phe(NO2)-Ser-Phe
show the reaction diagram
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys + H2O
Lys-Glu-Leu-Val-Phe + Phe(NO2)-Ala-Leu-Lys
show the reaction diagram
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-
-
?
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys + H2O
Lys-Glu-Phe-Asn-Phe + Phe(NO2)-Ala-Leu-Lys
show the reaction diagram
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-
-
-
?
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys + H2O
Lys-Glu-Phe-Val-Phe + Phe(NO2)-Ala-Leu-Lys
show the reaction diagram
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-
-
-
?
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys + H2O
Lys-Glu-Phe-Val-Phe + Phe(NO2)-Arg-Leu-Lys
show the reaction diagram
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?
Lys-Pro-Ile-Leu-Phe-Nph-Arg-Leu + H2O
?
show the reaction diagram
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-
?
additional information
?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Hemoglobin + H2O
?
show the reaction diagram
additional information
?
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plasmepsin I is synthesized and processed to the mature form soon after the parasite invades the red blood cell
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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
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i.e. KNI-10006, crystallization data
KPFEL-PSI(CH2-NH)-AWT
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combinatorial chemistry derived peptide inhibitor
KPFSL-PSI(CH2-NH)-LQF
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combinatorial chemistry derived peptide inhibitor, 5fold selectivity over human cathepsin D
KPLEF-PSI(CH2-NH)-FRV
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combinatorial chemistry derived peptide inhibitor
KPLEF-PSI(CH2-NH)-YRV
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combinatorial chemistry derived peptide inhibitor
KPnorLSnorL-PSI(CH2-NH)-LQI
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combinatorial chemistry derived peptide inhibitor
KPVEF-PSI(CH2-NH)-RQT
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combinatorial chemistry derived peptide inhibitor
pepstatin A
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(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
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(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxyindan-1-yl)-butyramide
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0.005 mM, 48% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
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0.005 mM, 35% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
0.005 mM, 98% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
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0.005 mM, 85% of maximal activity
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
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0.005 mM, 25% inhibition
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
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0.005 mM, 36% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
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0.005 mM, 35% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
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0.005 mM, 44% inhibition
(2R,3R)-4-[N-benzyl-N'-((S)-2-benzyloxycarbonylamino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
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0.005 mM, 48% inhibition
(2R,3R)-4-[N-benzyl-N'-((S)-2-tert-butyloxycarbonyl-amino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxy-indan-1-yl)-butyramide
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0.005 mM, 57% inhibition
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
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(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
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(2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(1,3-benzodioxol-5-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
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-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
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-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(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]-6-[2-[(4-tert-butylphenyl)carbonyl]hydrazino]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
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(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-N'1,N'6-bis[(4-tert-butylphenyl)carbonyl]-3,4-dihydroxyhexanedihydrazide
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(2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,4-dimethoxy-3,5-pyrimidin)-2-propenyl-oxy]-3,4-dihydroxyhexane-1,6-diamide
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-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,5-dimethyl-3,4-oxazol)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3,4-methylenedioxyphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3-thienyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-acetylphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-fluorophenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-tolyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-bromo-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-phenyl-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
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-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-phenyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-trimethylsilyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
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(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-(methoxycarbonyl)-pent-2,4-dienyloxy]-3,4-dihydroxyhexane-1,6-diamide
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-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-phenyl-pentadienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 55% inhibition
(2S,3S)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 57% inhibition
(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
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(2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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(2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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(2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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(2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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-
(2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
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(2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
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(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-3-hydroxy-4-(2-thiophen-2-ylacetylamino)pentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-4-(3,3-diphenylpropionylamino)-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-4-diphenylacetylamino-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(4R)-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
-
-
(5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
-
(5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
-
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-propyl)amide
-
-
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
-
1-[2-hydroxy-3-(1,2,3,4,5,6,7,8-octahydrophenanthren-9-yloxy)propyl]-4-(3-methoxyphenyl)piperazin-1-ium
-
-
17-benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16-tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
-
2,3-difluoro-4-methyl-N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]benzamide
-
-
2,5-Bis-allyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
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2,5-Bis-benzyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
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-
3'-(((1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-ylamino)methyl)biphenyl-2-ol
-
-
3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl 3,4-di-O-acetyl-2,6-dideoxyhexopyranoside
-
-
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
-
-
4-(1,3-benzodioxol-5-yl)-Nalpha-[(2S,3S)-2-hydroxy-3-([N-[3-(1H-indol-3-yl)propanoyl]-L-valyl]amino)-4-phenylbutyl]-L-phenylalaninamide
-
-
4-(1-benzofuran-2-yl)-Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
5-[bis[(benzyloxy)carbonyl]amino]-6-[[1-hydrazinyl-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-oxohexan-1-aminium
-
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benzo[1,3]dioxole-5-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-amide
-
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benzyl 2-benzyl-2-[(2S,3R)-3-[(4-bromobenzyl)oxy]-2-hydroxy-4-oxo-4-[(2-piperidin-1-ylethyl)amino]butyl]hydrazinecarboxylate
-
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benzyl 3-benzyl-4-([2-[(1-formyl-3-methylbutyl)amino]-2-oxo-1-phenylethyl]amino)-4-oxobutanoate
-
-
benzyl [(1S,4S,5R,6R,7S,10S)-4,7-bis[(4-cyanophenoxy)methyl]-5,6-dihydroxy-1,10-bis(1-methylethyl)-2,9,12-trioxo-14-phenyl-13-oxa-3,8,11-triazatetradec-1-yl]carbamate
-
-
isovaleryl-pepstatin
-
-
-
Iva-Val-Val-Sta-Ala-Sta
-
-
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
-
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
-
-
N-((1S,2S)-1-(4-benzo[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamid
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
-
-
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
-
-
N-butyl-N-[2-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-hydroxyethyl]butan-1-aminium
-
-
N-hexyl-N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]hexan-1-aminium
-
-
N-hexyl-N-[2-hydroxy-2-(phenanthren-9-yl)ethyl]hexan-1-aminium
-
-
N-[(1S)-1-([(1S,2S)-3-[(2-amino-2-oxoethyl)(benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl)-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-([[4-(1,3-benzodioxol-5-yl)benzyl]oxy]methyl)-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-benzyl-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-([(1S)-2-amino-1-[(4'-methylbiphenyl-4-yl)methyl]-2-oxoethyl]amino)-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-3-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl](benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-cyclo-hexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-3-cyclohexylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butyl-carbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
N-[(3S)-3-[(2S,5S,14S)-14-[(3,3-dimethylbutanoyl)amino]-2-(1-methylethyl)-3,11,15-trioxo-1,4,10-triazacyclopentadecan-5-yl]-3-hydroxypropanoyl]-L-valyl-L-leucylglycinamide
-
-
N-[(3S,4S)-3-hydroxy-6-phenyl-4-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]hexanoyl]-L-alanyl-L-leucinamide
-
-
N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentyl-N-[4-[(pyridin-3-ylmethyl)carbamoyl]benzyl]benzamide
-
-
N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentyl-N-[[4'-(piperidin-1-ylcarbonyl)biphenyl-4-yl]methyl]pyridine-2-carboxamide
-
-
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)amino]benzyl]-4-pentylbenzamide
-
-
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[methyl(pyridin-4-yl)amino]benzyl]-4-pentylbenzamide
-
-
N-[1-Benzyl-3-(2-biphenyl-4-yl-1-carbamoyl-ethylamino)-2-hydroxy-propyl]-2-(3-1H-indol-3-yl-propionylamino)-3-methyl-butyramide
-
-
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-4-methyl-N-(4-methylpentyl)pentan-1-aminium
-
-
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-N-pentylpentan-1-aminium
-
-
N-[3-(2,7-dichloro-9H-fluoren-4-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[3-(9H-fluoren-2-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[3-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
-
-
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(4-chlorophenyl)isoxazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N2-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-leucinamide
-
-
Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
pepstatin
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
pyridine-2-carboxylic acid ((R)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(3-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-(3-methoxyphenyl)ethylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-3-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcar-bamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcarbamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-benzyloxymethyl-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-3-((S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl)-2-hydroxy-1-phenethylpropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-phenylaminoethyl-carbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-phenylpropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(4-cyanobenzylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(cyclohexylmethylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-butylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methylpropyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-butylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(3-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
Ro 40-4388
-
aspartic protease peptidomimetic compound that potently inhibits plasmepsin I. Antimalarial activity is not exerted through inhibition of plasmepsins
SC-50083
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
-
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0086
Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.009
Lys-Glu-Leu-Val-Phe-(p-nitro)Phe-Ala-Leu-Lys
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0132
Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000917
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-(gamma-aminobutyryl)-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
-
pH 5.0, 37°C
0.008 - 0.01
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
0.03
Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37°C
0.005
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
0.015 - 0.02
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys
0.005 - 0.01
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
0.006 - 0.01
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
0.006
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37°C, naturally occuring enzyme
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2.6
Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
2.9
Lys-Glu-Leu-Val-Phe-(p-nitro)Phe-Ala-Leu-Lys
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
1.1
Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.473
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-(gamma-aminobutyryl)-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
-
pH 5.0, 37°C
1.3 - 16
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
1.6
Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37°C
10
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
2 - 12
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys
3.5 - 18
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
1.6 - 10
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.042
KPFEL-PSI(CH2-NH)-AWT
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000043
KPFSL-PSI(CH2-NH)-LQF
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0055
KPLEF-PSI(CH2-NH)-FRV
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.038
KPLEF-PSI(CH2-NH)-YRV
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000073
KPnorLSnorL-PSI(CH2-NH)-LQI
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.031
KPVEF-PSI(CH2-NH)-RQT
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0000014
pepstatin A
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0000014
Ro40-4388
-
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.00025
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
-
0.0013
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
-
0.00018
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
-
0.0005
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
-
-
0.000025
(2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
0.000006
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(1,3-benzodioxol-5-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000008
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
0.000038
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000009
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000198
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-6-[2-[(4-tert-butylphenyl)carbonyl]hydrazino]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
-
-
0.001837
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-N'1,N'6-bis[(4-tert-butylphenyl)carbonyl]-3,4-dihydroxyhexanedihydrazide
-
-
0.00016 - 0.000163
(2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
0.0000084
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,4-dimethoxy-3,5-pyrimidin)-2-propenyl-oxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000023
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,5-dimethyl-3,4-oxazol)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000005
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3,4-methylenedioxyphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000013
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3-thienyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000008
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-acetylphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
the best dual inhibitor for EC 3.4.23.38 and EC 3.4.23.39
0.0000025
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-fluorophenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000058
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-tolyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000027
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-bromo-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000014
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-phenyl-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000072
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-phenyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-trimethylsilyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-(methoxycarbonyl)-pent-2,4-dienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000044
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-phenyl-pentadienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.00082
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
-
0.00001
(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
-
-
0.000098
(2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.00053
(2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.0011
(2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000063
(2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000115
(2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.0013
(2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000438
(2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.001
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000068
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000469
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
-
0.024
(3S,4S)-5-(4-bromobenzyloxy)-3-hydroxy-4-(2-thiophen-2-ylacetylamino)pentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.04
(3S,4S)-5-(4-bromobenzyloxy)-4-(3,3-diphenylpropionylamino)-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.057
(3S,4S)-5-(4-bromobenzyloxy)-4-diphenylacetylamino-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.000727
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
0.00028
(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.00091
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-([N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl]amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide
-
-
0.002046
(5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
-
0.0019
(5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
-
0.059
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-propyl)amide
-
-
0.000017
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000011
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
-
0.00000001
17-Benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
-
0.000163
2,5-Bis-allyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
0.000025
2,5-Bis-benzyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
0.0000048
4-(1,3-benzodioxol-5-yl)-Nalpha-[(2S,3S)-2-hydroxy-3-([N-[3-(1H-indol-3-yl)propanoyl]-L-valyl]amino)-4-phenylbutyl]-L-phenylalaninamide
-
-
0.000013
4-(1-benzofuran-2-yl)-Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.029
benzo[1,3]dioxole-5-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-amide
-
-
0.00025
benzyl 2-benzyl-2-[(2S,3R)-3-[(4-bromobenzyl)oxy]-2-hydroxy-4-oxo-4-[(2-piperidin-1-ylethyl)amino]butyl]hydrazinecarboxylate
-
-
0.000009
benzyl 3-benzyl-4-([2-[(1-formyl-3-methylbutyl)amino]-2-oxo-1-phenylethyl]amino)-4-oxobutanoate
-
-
0.0000027
benzyl [(1S,4S,5R,6R,7S,10S)-4,7-bis[(4-cyanophenoxy)methyl]-5,6-dihydroxy-1,10-bis(1-methylethyl)-2,9,12-trioxo-14-phenyl-13-oxa-3,8,11-triazatetradec-1-yl]carbamate
-
-
0.0000005 - 0.0000007
Iva-Val-Val-Sta-Ala-Sta
0.0003
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0000033
N-((1S,2S)-1-(4-benzo[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.619
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
0.0034
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
0.032
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
0.000116
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
0.0000059
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.000221
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
0.000033
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000001
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000074
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000058
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000765
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000081
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
-
-
0.000031
N-[(1S)-1-([(1S,2S)-3-[(2-amino-2-oxoethyl)(benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl)-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000004
N-[(1S)-1-[[(1S,2S)-1-([[4-(1,3-benzodioxol-5-yl)benzyl]oxy]methyl)-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000016
N-[(1S)-1-[[(1S,2S)-1-benzyl-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000005
N-[(1S)-1-[[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000115
N-[(1S)-1-[[(1S,2S)-3-([(1S)-2-amino-1-[(4'-methylbiphenyl-4-yl)methyl]-2-oxoethyl]amino)-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.001
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-3-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.00022
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl](benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000068
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.822
N-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.000188
N-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-cyclo-hexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.0000034
N-[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]-2,4,6-trifluorobenzamide
-
-
0.000278
N-[(1S,2S)-3-cyclohexylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.0000021
N-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butyl-carbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.000022
N-[(3S)-3-[(2S,5S,14S)-14-[(3,3-dimethylbutanoyl)amino]-2-(1-methylethyl)-3,11,15-trioxo-1,4,10-triazacyclopentadecan-5-yl]-3-hydroxypropanoyl]-L-valyl-L-leucylglycinamide
-
-
0.000027
N-[(3S,4S)-3-hydroxy-6-phenyl-4-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]hexanoyl]-L-alanyl-L-leucinamide
-
-
0.0000026
N-[1-Benzyl-3-(2-biphenyl-4-yl-1-carbamoyl-ethylamino)-2-hydroxy-propyl]-2-(3-1H-indol-3-yl-propionylamino)-3-methyl-butyramide
-
-
0.0029
N2-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-leucinamide
-
-
0.0021
Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.000000565
pepstatin
-
pH 5.0, 37°C
0.0000000117 - 0.00000039
pepstatin A
0.0064
pyridine-2-carboxylic acid ((R)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.000001
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(3-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methyl-propyl)-amide
-
-
0.0000004
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)-amide
-
-
0.0067
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-(3-methoxyphenyl)ethylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
0.049
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
0.0005
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.0000007
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-3-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcar-bamoyl)-2-methyl-propyl)-amide
-
-
0.0000003
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcarbamoyl)-2-methyl-propyl)-amide
-
-
0.0054
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-benzyloxymethyl-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.027
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-1-phenethylpropylcarbamoyl)-2-methylpropyl)amide
-
-
0.0000027
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
0.0089
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-phenylaminoethyl-carbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.0054
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-phenylpropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.053
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(4-cyanobenzylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0039
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(cyclohexylmethylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0081
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-butylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0041
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0000019
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methylpropyl)-amide
-
-
0.000001
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-butylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
0.0000004
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(3-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
0.0000003
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
0.000004 - 0.000009
Ro40-4388
0.000006 - 0.000008
Ro40-5576
0.00023
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
-
-
additional information
additional information
-
Ki-value for Ro17-7109 is above 0.05 mM
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0021
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00037
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00067
(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.000727
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
Plasmodium falciparum
-
-
0.000017
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000011
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
Plasmodium falciparum
-
-
0.022
1-[2-hydroxy-3-(1,2,3,4,5,6,7,8-octahydrophenanthren-9-yloxy)propyl]-4-(3-methoxyphenyl)piperazin-1-ium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000629
2,3-difluoro-4-methyl-N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]benzamide
Plasmodium falciparum
-
-
0.00093
3'-(((1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-ylamino)methyl)biphenyl-2-ol
Plasmodium falciparum
-
-
0.022
3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl 3,4-di-O-acetyl-2,6-dideoxyhexopyranoside
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.028
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.037
5-[bis[(benzyloxy)carbonyl]amino]-6-[[1-hydrazinyl-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-oxohexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000655
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.000441
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.024
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000033
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000001
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000074
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000058
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamid
Plasmodium falciparum
-
-
0.000765
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000081
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000034
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
Plasmodium falciparum
-
-
0.002
N-butyl-N-[2-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-hydroxyethyl]butan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.004
N-hexyl-N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]hexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.023
N-hexyl-N-[2-hydroxy-2-(phenanthren-9-yl)ethyl]hexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.001727
N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentyl-N-[4-[(pyridin-3-ylmethyl)carbamoyl]benzyl]benzamide
Plasmodium falciparum
-
-
0.000711
N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentyl-N-[[4'-(piperidin-1-ylcarbonyl)biphenyl-4-yl]methyl]pyridine-2-carboxamide
Plasmodium falciparum
-
-
0.001162
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)amino]benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.001123
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[methyl(pyridin-4-yl)amino]benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.003
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-4-methyl-N-(4-methylpentyl)pentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.023
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.041
N-[3-(2,7-dichloro-9H-fluoren-4-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.071
N-[3-(9H-fluoren-2-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.003
N-[3-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000123
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
Plasmodium falciparum
-
-
0.000537
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000113
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000104
N-[[5-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.001672
N-[[5-(4-chlorophenyl)isoxazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000001 - 0.000005
pepstatin
0.000132
SC-50083
Plasmodium falciparum
-
IC50: 0.000132 mM
0.00023
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
Plasmodium falciparum
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
4.5
-
recombinant truncated proPfPM1 K110pN mutant
2.5 - 3
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH, and a second optimum at pH 4.5-5.5, mature fusion enzyme
2.8 - 4
-
human hemoglobin, mature fusion enzyme
4
-
hydrolysis of Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
4.5 - 5.5
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH, and a second optimum at pH 2.5-3.0, mature fusion enzyme
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
3 - 7
-
active over the range
3.5 - 6
-
pH 3.5: about 75% of maximal activity, pH 6.0: about 40% of maximal activity, hydrolysis of Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
4 - 6.5
-
pH 4.0: about 20% of maximal activity, pH 4.5: about 90% of maximal activity, pH 6.0: about 60% of maximal activity, pH 6.5: about 30% of maximal activity
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
proplasmepsin I is a type II integral membrane protein that is transported though the secretory pathway before cleavage to the soluble form
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
multiple plasmepsin knockout mutants lacking plasmepsins I-III and I-IV, respectively show a significant increased parasite susceptibility to cyteine protease inhibitors. A ninefold increase in the potency of the calpain inhibitor N-acetyl-leucinyl-leucinyl-norleucinal (ALLN) against parasites lacking all four plasmepsins (I-IV) is observed. It is hypothesized that plasmepsins and some cysteine proteases play redundant or complementary roles in the digestive vacuole and that the absence of all plasmepsins (I-IV) renders these parasites highly susceptible to N-acetyl-leucinyl-leucinyl-norleucinal-mediated inhibition of falcipains
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
Sequence
PLM1_PLAFA
452
1
51461
Swiss-Prot
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37800
-
gel filtration
40000
-
x * 40000, SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
-
x * 37800, calculated
?
-
x * 40000, SDS-PAGE
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
proteolytic modification
-
automaturation of proPfPM1 K110pN mutant at pH 4.0-4.5, with reduction of molecular weight by 5 kDa
proteolytic modification
CRYSTALLIZATION/commentary
ORGANISM
UNIPROT
LITERATURE
recombinant PMI as apoenzyme and in complex with the potent peptidic inhibitor, (4R)-3-[(2S,3S)-3-{[(2,6-dimethylphenoxy)acetyl]amino}-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide, i. e. KNI-10006, at the resolution of 2.4 and 3.1 A, respectively. The apoenzyme crystallizes in the orthorhombic space group P212121 with two molecules in the asymmetric unit. The KNI-10006 bound enzyme crystallized in the tetragonal space group P43 with four molecules in the asymmetric unit a. In the PMI–KNI-10006 complex, the inhibitors are bound identically to all four enzyme molecules, with the opposite directionality of the main chain of KNI-10006 relative to the direction of the enzyme substrates
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
V110P
-
mutation in proplasmepsin I is responsible for generating a form of proplasmepsin I that is capable of undergoing autoactivation
PURIFICATION/commentary
ORGANISM
UNIPROT
LITERATURE
recombinant enzyme
-
expression and partial characterization of soluble recombinant PM I from Plasmodium falciparum in which a truncated form of PM I (Lys77P–Leu329) (P indicates a propart residues) is fused to thioredoxin in the pET32b(1) vector, Trx-tPM I and expressed in Escherichia coli Rosetta-gami B (DE3)pLysS. pLysS. The soluble fusion protein is purified from cell culture using a combination of Ni21 affinity and gel filtration chromatography
-
recombinant V110P-proplasmepsin I
-
CLONED/commentary
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli
-
expression of truncated proPfPM1 K110pN mutant in Escherichia coli
-
expression and partial characterization of soluble recombinant PM I from Plasmodium falciparum in which a truncated form of PM I (Lys77P-Leu329) (P indicates a propart residues) is fused to thioredoxin in the pET32b(1) vector, Trx-tPM I and expressed in Escherichia coli Rosetta-gami B (DE3)pLysS. The soluble fusion protein is purified from cell culture using a combination of Ni21 affinity and gel filtration chromatography and is capable of autocatalytic activation at pH 4.0–5.5, which occurrs at Leu116P-Ser117P, seven residues upstream of the native cleavage site (Gly123P-Asn1)
-
expression in Escherichia coli
-
expression of proplasmepsin I and V110P-proplasmepsin in Escherichia coli; initial attempts to express full-length proplasmepsin I gene in Escherichia coli results in very low expression levels, possibly due to the toxic effects of the hydrophobic segment, and no activation to mature plasmepsin I is ever observed. Recombinant proplasmepsin I is expressed from pETPMI, a construct that is prepared from pET3a and contains the last 48 residues of the propart followed by the 328 residues of mature plasmepsin I. It is necessary to introduce a processing site, V110P, into the zymogen that renders the precursor capable of undergoing autoactivation
-
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Goldberg, D.E.; Slater, A.F.G.; Beavis, R.; Chait, B.; Cerami, A.; Henderson, G.B.
Hemoglobin degradation in the human malaria pathogen Plasmodium falciparum: a catabolic pathway initiated by a specific aspartic protease
J. Exp. Med.
173
961-969
1991
Plasmodium falciparum
Manually annotated by BRENDA team
Francis, S.E.; Gluzman, I.Y.; Oksman, A.; Knickerbocker, A.; Mueller, R.; Bryant, M.L.; Sherman, D.R.; Russell, D.G.; Goldberg, D.E.
Molecular characterization and inhibition of a Plasmodium falciparum aspartic hemoglobinase
EMBO J.
13
306-317
1994
Plasmodium falciparum
Manually annotated by BRENDA team
Gluzman, I.Y.; Francis, S.E.; Oksman, A.; Smith, C.E.; Duffin, K.L.; Goldberg, D.E.
Order and specificity of the Plasmodium falciparum hemoglobin degradation pathway
J. Clin. Invest.
93
1602-1608
1994
Plasmodium falciparum
Manually annotated by BRENDA team
Ersmark, K.; Feierberg, I.; Bjelic, S.; Hamelink, E.; Hackett, F.; Blackman, M.J.; Hulten, J.; Samuelsson, B.; Aqvist, J.; Hallberg, A.
Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity
J. Med. Chem.
47
110-122
2004
Plasmodium falciparum
Manually annotated by BRENDA team
Berry, C.
Plasmepsins as antimalarial targets
Curr. Opin. Drug Discov. Devel.
3
624-629
2000
Plasmodium falciparum
Manually annotated by BRENDA team
Dahlgren, A.; Kvarnstrom, I.; Vrang, L.; Hamelink, E.; Hallberg, A.; Rosenquist, A.; Samuelsson, B.
New inhibitors of the malaria aspartyl proteases plasmepsin I and II
Bioorg. Med. Chem.
11
3423-3437
2003
Plasmodium falciparum
Manually annotated by BRENDA team
Francis, S.E.; Banerjee, R.; Goldberg, D.E.
Biosynthesis and maturation of the malaria aspartic hemoglobinases plasmepsins I and II
J. Biol. Chem.
272
14961-14968
1997
Plasmodium falciparum
Manually annotated by BRENDA team
Moon, R.P.; Bur, D.; Loetscher, H.; D'Arcy, A.; Tyas, L.; Oefner, C.; Grueninger-Leitch, F.; Mona, D.; Rupp, K.; Dorn, A.; Matile, H.; Certa, U.; Berry, C.; Kay, J.; Ridley, R.G.
Studies on plasmepsins I and II from the malarial parasite Plasmodium falciparum and their exploitation as drug targets
Adv. Exp. Med. Biol.
436
397-406
1998
Plasmodium falciparum
Manually annotated by BRENDA team
Noteberg, D.; Hamelink, E.; Hulten, J.; Wahlgren, M.; Vrang, L.; Samuelsson, B.; Hallberg, A.
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes
J. Med. Chem.
46
734-746
2003
Plasmodium falciparum
Manually annotated by BRENDA team
Siripurkpong, P.; Yuvaniyama, J.; Wilairat, P.; Goldberg, D.E.
Active Site Contribution to Specificity of the Aspartic Proteases Plasmepsins I and II
J. Biol. Chem.
277
41009-41013
2002
Plasmodium falciparum
Manually annotated by BRENDA team
Tyas, L.; Gluzman, I.; Moon, R.P.; Rupp, K.; Westling, J.; Ridley, R.G.; Kay, J.; Goldberg, D.E.; Berry, C.
Naturally-occurring and recombinant forms of the aspartic proteinases plasmepsins I and II from the human malaria parasite Plasmodium falciparum
FEBS Lett.
454
210-214
1999
Plasmodium falciparum
Manually annotated by BRENDA team
Tyas, L.; Moon, R.P.; Loetscher, H.; Dunn, B.M.; Kay, J.; Ridley, R.G.; Berry, C.
Plasmepsins I and II from the malarial parasite Plasmodium falciparum
Adv. Exp. Med. Biol.
436
407-411
1998
Plasmodium falciparum
Manually annotated by BRENDA team
Moon, R.P.; Tyas, L.; Certa, U.; Rupp, K.; Bur, D.; Jacquet, C.; Matile, H.; Loetscher, H.; Grueninger-Leitch, F.; et al.
Expression and characterization of plasmepsin I from Plasmodium falciparum
Eur. J. Biochem.
244
552-560
1997
Plasmodium falciparum
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Johansson, P.O.; Chen, Y.; Belfrage, A.K.; Blackman, M.J.; Kvarnstroem, I.; Jansson, K.; Vrang, L.; Hamelink, E.; Hallberg, A.; Rosenquist, A.; Samuelsson, B.
Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs
J. Med. Chem.
47
3353-3366
2004
Plasmodium falciparum
Manually annotated by BRENDA team
Johansson, P.O.; Lindberg, J.; Blackman, M.J.; Kvarnstroem, I.; Vrang, L.; Hamelink, E.; Hallberg, A.; Rosenquist, A.; Samuelsson, B.
Design and synthesis of potent inhibitors of plasmepsin I and II: X-ray crystal structure of inhibitor in complex with plasmepsin II
J. Med. Chem.
48
4400-4409
2005
Plasmodium falciparum
Manually annotated by BRENDA team
Ersmark, K.; Samuelsson, B.; Hallberg, A.
Plasmepsins as potential targets for new antimalarial therapy
Med. Res. Rev.
26
626-666
2006
Plasmodium falciparum
Manually annotated by BRENDA team
Hof, F.; Schutz, A.; Fah, C.; Meyer, S.; Bur, D.; Liu, J.; Goldberg, D.E.; Diederich, F.
Starving the malaria parasite: inhibitors active against the aspartic proteases plasmepsins I, II, and IV
Angew. Chem.
45
2138-2141
2006
Plasmodium falciparum
Manually annotated by BRENDA team
Boss, C.; Corminboeuf, O.; Grisostomi, C.; Meyer, S.; Jones, A.F.; Prade, L.; Binkert, C.; Fischli, W.; Weller, T.; Bur, D.
Achiral, cheap, and potent inhibitors of plasmepsins I, II, and IV
ChemMedChem
1
1341-1345
2006
Plasmodium falciparum
Manually annotated by BRENDA team
Bonilla, J.A.; Moura, P.A.; Bonilla, T.D.; Yowell, C.A.; Fidock, D.A.; Dame, J.B.
Effects on growth, hemoglobin metabolism and paralogous gene expression resulting from disruption of genes encoding the digestive vacuole plasmepsins of Plasmodium falciparum
Int. J. Parasitol.
37
317-327
2007
Plasmodium falciparum (P39898), Plasmodium falciparum
Manually annotated by BRENDA team
DellAgli, M.; Parapini, S.; Galli, G.; Vaiana, N.; Taramelli, D.; Sparatore, A.; Liu, P.; Dunn, B.M.; Bosisio, E.; Romeo, S.
High antiplasmodial activity of novel plasmepsins I and II inhibitors
J. Med. Chem.
49
7440-7449
2006
Plasmodium falciparum
Manually annotated by BRENDA team
Bonilla, J.A.; Bonilla, T.D.; Yowell, C.A.; Fujioka, H.; Dame, J.B.
Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function
Mol. Microbiol.
65
64-75
2007
Plasmodium falciparum
Manually annotated by BRENDA team
Xiao, H.; Tanaka, T.; Ogawa, M.; Yada, R.Y.
Expression and enzymatic characterization of the soluble recombinant plasmepsin I from Plasmodium falciparum
Protein Eng. Des. Sel.
20
625-633
2007
Plasmodium falciparum
Manually annotated by BRENDA team
Liu, P.; Marzahn, M.; Robbins, A.; Gutierrez-de-Teran, H.; Rodriguez, D.; McClung, S.; Stevens, S.; Yowell, C.; Dame, J.; McKenna, R.; Dunn, B.
Recombinant plasmepsin 1 from the human malaria parasite Plasmodium falciparum: Enzymatic characterization, active site inhibitor design, and structural analysis
Biochemistry
48
4086-99
2009
Plasmodium falciparum (P39898), Plasmodium falciparum
Manually annotated by BRENDA team
Moura, P.A.; Dame, J.B.; Fidock, D.A.
Role of Plasmodium falciparum digestive vacuole plasmepsins in the specificity and antimalarial mode of action of cysteine and aspartic protease inhibitors
Antimicrob. Agents Chemother.
53
4968-4978
2009
Plasmodium falciparum
Manually annotated by BRENDA team
Friedman, R.; Caflisch, A.
Discovery of plasmepsin inhibitors by fragment-based docking and consensus scoring
ChemMedChem
4
1317-1326
2009
Plasmodium falciparum
Manually annotated by BRENDA team
Bhaumik, P.; Horimoto, Y.; Xiao, H.; Miura, T.; Hidaka, K.; Kiso, Y.; Wlodawer, A.; Yada, R.Y.; Gustchina, A.
Crystal structures of the free and inhibited forms of plasmepsin I (PMI) from Plasmodium falciparum
J. Struct. Biol.
175
73-84
2011
Plasmodium falciparum (P39898), Plasmodium falciparum
Manually annotated by BRENDA team
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