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Information on EC 3.4.23.38 - plasmepsin I
for references in articles please use BRENDA:EC3.4.23.38
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EC Tree 3 Hydrolases
3.4 Acting on peptide bonds (peptidases)
3.4.23 Aspartic endopeptidases
3.4.23.38 plasmepsin I
IUBMB Comments
Known from the malaria organism, Plasmodium. About 37 kDa. In peptidase family A1 (pepsin A family), closest to cathepsin D and renin in structure. Inhibited by pepstatin. Formerly included in EC 3.4.23.6
The expected taxonomic range for this enzyme is: Plasmodium falciparum
- 3.4.23.38
-
plasmepsins
- falciparum
- plasmodium
-
malarial
-
antimalarial
- cathepsin
- vacuole
-
aspartyl
- proteinases
-
hemoglobin-degrading
-
intraerythrocytic
-
autocatalytic
-
proplasmepsins
Reaction Schemes
showhydrolysis of the -Phe33-/-Leu- bond in the alpha-chain of hemoglobin, leading to denaturation of the molecule
Synonyms
plasmepsin i, plm i, pfpm1, plasmepsin-i, more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
AH I
-
-
-
-
aspartic hemoglobinase I
-
-
-
-
malaria aspartic hemoglobinase
-
-
-
-
PFAPG
-
-
-
-
PfPM1
PLm I
PMI
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
hydrolysis of the -Phe33-/-Leu- bond in the alpha-chain of hemoglobin, leading to denaturation of the molecule
-
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
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PATHWAY SOURCE
PATHWAYS
MetaCyc
hemoglobin degradation
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CAS REGISTRY NUMBER
COMMENTARY
180189-87-1
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Met-Phe + Leu-Ser-Phe-Pro-(gamma-aminobutyryl)-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid + H2O
?
-
Substrates: -
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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
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Met-Phe + Leu-Ser-Phe-Pro-(gamma-aminobutyryl)-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
-
Substrates: -
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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
?
-
Substrates: -
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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
-
Substrates: -
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?
Ala-Leu-Glu-Arg-Thr-Phe-Leu-Ser-Phe-Pro-Thr + H2O
Ala-Leu-Glu-Arg-Thr-Phe + Leu-Ser-Phe-Pro-Thr
-
Substrates: -
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?
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH + H2O
?
-
Substrates: -
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?
hemoglobin beta-chain + H2O
?
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Substrates: cleavage sites: Leu31-/-Leu32, Phe41-/-Phe43, Ala129-/-Tyr130
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?
Leu-Glu-Arg-Ile-Phe-(p-nitro)Phe-Ser-Phe + H2O
Leu-Glu-Arg-Ile-Phe + (p-nitro)Phe-Ser-Phe
Substrates: -
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?
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe + H2O
Leu-Glu-Arg-Ile-Phe + Phe(NO2)-Ser-Phe
-
Substrates: -
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?
Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe + H2O
Leu-Glu-Arg-Val-Phe + Phe(NO2)-Ser-Phe
-
Substrates: -
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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
Substrates: -
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?
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys + H2O
Lys-Glu-Leu-Val-Phe + Phe(NO2)-Ala-Leu-Lys
-
Substrates: -
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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
-
Substrates: -
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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
-
Substrates: -
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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
-
Substrates: -
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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
Substrates: -
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?
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Lys-Phe + Phe(NO2)-Arg-Leu
-
Substrates: -
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?
Hemoglobin + H2O
?
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Substrates: enzyme is involved in initial steps of Plasmodium hemoglobin degradation
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?
Hemoglobin + H2O
?
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Substrates: the enzyme initiates the hemoglobin degradation pathway in Plasmodium
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?
Hemoglobin + H2O
?
-
Substrates: during the infection of erythrocytes by the human malaria parasite Plasmodium falciparum, up to 80% of the host cell hemoglobin is degraded to provide amino acids for parasite nutrition. Plasmepsin I and plasmepsin II are believed to be responsible for initiating the catabolic process
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?
hemoglobin alpha-chain + H2O
?
-
Substrates: cleavage of the Phe33-/-Leu34- bond
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?
hemoglobin alpha-chain + H2O
?
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Substrates: cleavage sites: Phe33-/-Leu34, Phe46-/-Asp47, Phe98-/-Lys99
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?
additional information
?
-
-
Substrates: plasmepsin I is 5 to 9times less effective than plasmepsin II at cleaving substrates which mimic the proposed initial cleavage site in the alpha-chain of hemoglobin
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?
additional information
?
-
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Substrates: plasmepsin I is synthesized and processed to the mature form soon after the parasite invades the red blood cell
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?
additional information
?
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Substrates: S1' subsite prefers hydrophobic residues and the S2' subsite shifts its preferences more to polar residues. Serine is a preferred P1' substitution
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?
additional information
?
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Substrates: S1' subsite prefers hydrophobic residues and the S2' subsite shifts its preferences more to polar residues. Serine is a preferred P1' substitution
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?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
additional information
?
-
-
Substrates: plasmepsin I is synthesized and processed to the mature form soon after the parasite invades the red blood cell
Products: -
Products: -
?
Hemoglobin + H2O
?
-
Substrates: enzyme is involved in initial steps of Plasmodium hemoglobin degradation
Products: -
Products: -
?
Hemoglobin + H2O
?
-
Substrates: the enzyme initiates the hemoglobin degradation pathway in Plasmodium
Products: -
Products: -
?
Hemoglobin + H2O
?
-
Substrates: during the infection of erythrocytes by the human malaria parasite Plasmodium falciparum, up to 80% of the host cell hemoglobin is degraded to provide amino acids for parasite nutrition. Plasmepsin I and plasmepsin II are believed to be responsible for initiating the catabolic process
Products: -
Products: -
?
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1S,2aR,3aR,3bS,4R,9aR,11aS)-2-(((1-(2-cyanophenyl)-1H-1,2,3-triazol-4-yl)methoxy)imino)-1-(furan-3-yl)-3b,6,6,9a,11a-pentamethyl-7-oxo-1,2,2a,3b,4,5,5a,6,7,9a,9b,10,11,11a-tetradecahydronaphtho(1,2':6,7)indeno(1,7a-b)oxiren-4-yl acetate
most active compound
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxyindan-1-yl)-butyramide
-
0.005 mM, 48% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 35% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
0.005 mM, 98% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 85% of maximal activity
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 25% inhibition
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 36% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 35% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 44% inhibition
(2R,3R)-4-[N-benzyl-N'-((S)-2-benzyloxycarbonylamino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 48% inhibition
(2R,3R)-4-[N-benzyl-N'-((S)-2-tert-butyloxycarbonyl-amino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxy-indan-1-yl)-butyramide
-
0.005 mM, 57% inhibition
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
-
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
-
-
(2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(1,3-benzodioxol-5-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-6-[2-[(4-tert-butylphenyl)carbonyl]hydrazino]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-N'1,N'6-bis[(4-tert-butylphenyl)carbonyl]-3,4-dihydroxyhexanedihydrazide
-
-
(2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,4-dimethoxy-3,5-pyrimidin)-2-propenyl-oxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,5-dimethyl-3,4-oxazol)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3,4-methylenedioxyphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3-thienyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-acetylphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-fluorophenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-tolyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-bromo-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-phenyl-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-phenyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-trimethylsilyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-(methoxycarbonyl)-pent-2,4-dienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-phenyl-pentadienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 55% inhibition
(2S,3S)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 57% inhibition
(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
-
-
(2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-3-hydroxy-4-(2-thiophen-2-ylacetylamino)pentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-4-(3,3-diphenylpropionylamino)-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-4-diphenylacetylamino-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(4R)-3-[(2S,3S)-3-{[(2,6-dimethylphenoxy)acetyl]amino}-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
i.e. KNI-10006, crystallization data
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-([N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl]amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide
-
-
(5E)-5-[[2,5-dimethyl-1-(4-methylphenyl)-1H-pyrrol-3-yl]methylidene]-2,6-dihydroxypyrimidin-4(5H)-one
-
(5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
-
(5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
-
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-propyl)amide
-
-
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
-
1-[2-hydroxy-3-(1,2,3,4,5,6,7,8-octahydrophenanthren-9-yloxy)propyl]-4-(3-methoxyphenyl)piperazin-1-ium
-
-
17-benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16-tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
-
2,3-difluoro-4-methyl-N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]benzamide
-
-
2,5-Bis-allyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
2,5-Bis-benzyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
3'-(((1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-ylamino)methyl)biphenyl-2-ol
-
-
3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl 3,4-di-O-acetyl-2,6-dideoxyhexopyranoside
-
-
3-ethyl-3-hydroxy-5-alpha-androstan-17-one
compound isolated from betel fruit, binds to both plasmepsin I and plasmepsin II. Binding free enrgy is -9.1 kcal/mol
-
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
-
-
4-(1,3-benzodioxol-5-yl)-Nalpha-[(2S,3S)-2-hydroxy-3-([N-[3-(1H-indol-3-yl)propanoyl]-L-valyl]amino)-4-phenylbutyl]-L-phenylalaninamide
-
-
4-(1-benzofuran-2-yl)-Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
5-[bis[(benzyloxy)carbonyl]amino]-6-[[1-hydrazinyl-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-oxohexan-1-aminium
-
-
benzo[1,3]dioxole-5-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-amide
-
-
benzyl 2-benzyl-2-[(2S,3R)-3-[(4-bromobenzyl)oxy]-2-hydroxy-4-oxo-4-[(2-piperidin-1-ylethyl)amino]butyl]hydrazinecarboxylate
-
-
benzyl 3-benzyl-4-([2-[(1-formyl-3-methylbutyl)amino]-2-oxo-1-phenylethyl]amino)-4-oxobutanoate
-
-
benzyl [(1S,4S,5R,6R,7S,10S)-4,7-bis[(4-cyanophenoxy)methyl]-5,6-dihydroxy-1,10-bis(1-methylethyl)-2,9,12-trioxo-14-phenyl-13-oxa-3,8,11-triazatetradec-1-yl]carbamate
-
-
KPFEL-PSI(CH2-NH)-AWT
combinatorial chemistry derived peptide inhibitor
KPFSL-PSI(CH2-NH)-LQF
combinatorial chemistry derived peptide inhibitor, 5fold selectivity over human cathepsin D
KPLEF-PSI(CH2-NH)-FRV
combinatorial chemistry derived peptide inhibitor
KPLEF-PSI(CH2-NH)-YRV
combinatorial chemistry derived peptide inhibitor
KPnorLSnorL-PSI(CH2-NH)-LQI
combinatorial chemistry derived peptide inhibitor
KPVEF-PSI(CH2-NH)-RQT
combinatorial chemistry derived peptide inhibitor
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
-
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
-
-
N-((1S,2S)-1-(4-benzo[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamid
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
-
-
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
-
-
N-butyl-N-[2-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-hydroxyethyl]butan-1-aminium
-
-
N-hexyl-N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]hexan-1-aminium
-
-
N-[(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-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
-
-
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[5-(4-chlorophenyl)isoxazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N2-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-leucinamide
-
-
Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
pyridine-2-carboxylic acid ((R)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(3-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-(3-methoxyphenyl)ethylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-3-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcar-bamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcarbamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-benzyloxymethyl-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-3-((S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl)-2-hydroxy-1-phenethylpropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-phenylaminoethyl-carbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-phenylpropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(4-cyanobenzylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(cyclohexylmethylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-butylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methylpropyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-butylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(3-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
Ro 40-4388
-
aspartic protease peptidomimetic compound that potently inhibits plasmepsin I. Antimalarial activity is not exerted through inhibition of plasmepsins
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
-
-
additional information
-
inhibition of the enzyme blocks the essential pathway of hemoglobin degradation, leading to death of the organism
-
additional information
-
none of the inhibitors analyzed to date have sufficient selectivity for plasmepsin I and II, compared to their human counterparts
-
additional information
-
plasmepsin I is a valid antimalarial drug target on two counts. First, inhibition of the enzyme correlates with inhibition of parasite growth. Second, specificity of inhibition over human aspartic proteinases is possible
-
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DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Malaria
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.
Malaria
Disulfide linkages in Plasmodium falciparum plasmepsin-i are essential elements for its processing activity and multi-milligram recombinant production yield.
Malaria
Expression and enzymatic characterization of the soluble recombinant plasmepsin I from Plasmodium falciparum.
Malaria
Flap flexibility amongst plasmepsins I, II, III, IV, and V: Sequence, structural, and molecular dynamics analyses.
Malaria
High-affinity inhibition of a family of Plasmodium falciparum proteases by a designed adaptive inhibitor.
Malaria
Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity.
Malaria
Recombinant plasmepsin 1 from the human malaria parasite plasmodium falciparum: enzymatic characterization, active site inhibitor design, and structural analysis.
Malaria
Solid-phase library synthesis of reversed-statine type inhibitors of the malarial aspartyl proteases plasmepsin I and II.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
0.0086
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
0.005
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
0.0132
Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.006
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37°C, naturally occuring enzyme
0.008
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37°C, naturally occuring enzyme
0.01
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37°C, recombinant enzyme
0.015
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, naturally occuring enzyme
0.02
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
0.005
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
0.01
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, naturally occuring enzyme
0.006
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
-
pH 4.4, 37°C, naturally occuring
0.01
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
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
10
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
1.1
Lys-Pro-Ile-Leu-Phe-(p-nitro)Phe-Arg-Leu
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
2.1
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37°C, recombinant enzyme
16
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37°C, naturally occuring enzyme
2
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
12
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, naturally occuring enzyme
3.5
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
18
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37°C, naturally occuring enzyme
1.6
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
-
pH 4.4, 37°C, recombinant enzyme
10
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
-
pH 4.4, 37°C, naturally occuring enzyme
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
-
-
0.042
KPFEL-PSI(CH2-NH)-AWT
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000043
KPFSL-PSI(CH2-NH)-LQF
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0055
KPLEF-PSI(CH2-NH)-FRV
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.038
KPLEF-PSI(CH2-NH)-YRV
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000073
KPnorLSnorL-PSI(CH2-NH)-LQI
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.031
KPVEF-PSI(CH2-NH)-RQT
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0003
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0000033
N-((1S,2S)-1-(4-benzo[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.619
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
0.0034
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
0.032
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
0.000116
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
0.0000059
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.000221
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
0.000033
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000001
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000074
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000058
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000765
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000081
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
-
-
0.000031
N-[(1S)-1-([(1S,2S)-3-[(2-amino-2-oxoethyl)(benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl)-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000004
N-[(1S)-1-[[(1S,2S)-1-([[4-(1,3-benzodioxol-5-yl)benzyl]oxy]methyl)-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000016
N-[(1S)-1-[[(1S,2S)-1-benzyl-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000005
N-[(1S)-1-[[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000115
N-[(1S)-1-[[(1S,2S)-3-([(1S)-2-amino-1-[(4'-methylbiphenyl-4-yl)methyl]-2-oxoethyl]amino)-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.001
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-3-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.00022
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl](benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000068
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.822
N-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.000188
N-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-cyclo-hexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.0000034
N-[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]-2,4,6-trifluorobenzamide
-
-
0.000278
N-[(1S,2S)-3-cyclohexylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.0000021
N-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butyl-carbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.000022
N-[(3S)-3-[(2S,5S,14S)-14-[(3,3-dimethylbutanoyl)amino]-2-(1-methylethyl)-3,11,15-trioxo-1,4,10-triazacyclopentadecan-5-yl]-3-hydroxypropanoyl]-L-valyl-L-leucylglycinamide
-
-
0.000027
N-[(3S,4S)-3-hydroxy-6-phenyl-4-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]hexanoyl]-L-alanyl-L-leucinamide
-
-
0.0000026
N-[1-Benzyl-3-(2-biphenyl-4-yl-1-carbamoyl-ethylamino)-2-hydroxy-propyl]-2-(3-1H-indol-3-yl-propionylamino)-3-methyl-butyramide
-
-
0.0029
N2-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-leucinamide
-
-
0.0021
Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.0064
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
-
-
0.00023
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
-
-
additional information
additional information
-
Ki-value for Ro17-7109 is above 0.05 mM
-
0.00016
(2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
-
0.000163
(2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
-
0.0000005
Iva-Val-Val-Sta-Ala-Sta
-
pH 4.4, 37°C, naturally occuring enzyme
0.0003
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
-
0.0003
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
pH 4.4
0.0000014
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
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0017
(1S,2aR,3aR,3bS,4R,9aR,11aS)-2-(((1-(2-cyanophenyl)-1H-1,2,3-triazol-4-yl)methoxy)imino)-1-(furan-3-yl)-3b,6,6,9a,11a-pentamethyl-7-oxo-1,2,2a,3b,4,5,5a,6,7,9a,9b,10,11,11a-tetradecahydronaphtho(1,2':6,7)indeno(1,7a-b)oxiren-4-yl acetate
Plasmodium falciparum
pH and temperature not specified in the publication
0.0021
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00037
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00067
(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.000727
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
Plasmodium falciparum
-
-
0.000017
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000011
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
Plasmodium falciparum
-
-
0.022
1-[2-hydroxy-3-(1,2,3,4,5,6,7,8-octahydrophenanthren-9-yloxy)propyl]-4-(3-methoxyphenyl)piperazin-1-ium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000629
2,3-difluoro-4-methyl-N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]benzamide
Plasmodium falciparum
-
-
0.00093
3'-(((1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-ylamino)methyl)biphenyl-2-ol
Plasmodium falciparum
-
-
0.022
3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl 3,4-di-O-acetyl-2,6-dideoxyhexopyranoside
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.028
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.037
5-[bis[(benzyloxy)carbonyl]amino]-6-[[1-hydrazinyl-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-oxohexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000655
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.000441
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.024
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000033
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000001
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000074
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000058
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamid
Plasmodium falciparum
-
-
0.000765
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000081
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
Plasmodium falciparum
-
-
0.000034
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
Plasmodium falciparum
-
-
0.002
N-butyl-N-[2-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-hydroxyethyl]butan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.004
N-hexyl-N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]hexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.023
N-hexyl-N-[2-hydroxy-2-(phenanthren-9-yl)ethyl]hexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.001727
N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentyl-N-[4-[(pyridin-3-ylmethyl)carbamoyl]benzyl]benzamide
Plasmodium falciparum
-
-
0.000711
N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentyl-N-[[4'-(piperidin-1-ylcarbonyl)biphenyl-4-yl]methyl]pyridine-2-carboxamide
Plasmodium falciparum
-
-
0.001162
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)amino]benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.001123
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[methyl(pyridin-4-yl)amino]benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.003
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-4-methyl-N-(4-methylpentyl)pentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.023
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.041
N-[3-(2,7-dichloro-9H-fluoren-4-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.071
N-[3-(9H-fluoren-2-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.003
N-[3-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000123
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
Plasmodium falciparum
-
-
0.000537
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000113
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000104
N-[[5-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.001672
N-[[5-(4-chlorophenyl)isoxazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.00023
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
Plasmodium falciparum
-
-
0.000001
pepstatin
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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
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
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
additional information
asexual. The knockout mutants DELTApfpm1 has lower replication rate in the asexual erythrocytic stage than the parental line
brenda
additional information
-
Plasmodium falciparum-infected cultured human erythrocytes
brenda
additional information
-
proplasmepsin I is expressed in the ring stages whereas the proplasmepsin II gene is not transcribed until the later trophozoite stage of parasite growth
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
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
brenda
-
the plasmepsins, although not essential, contribute significantly to the fitness of the parasite and are required for efficient degradation of endosomal vesicles delivered to the digestive vacuole
brenda
Highest Expressing Human Cell Lines
Cell Line LinksPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
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
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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). Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PDB
SCOP
CATH
UNIPROT
ORGANISM
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
proteolytic modification
proteolytic modification
-
the proenzyme has an unusually long propart of 125 amino acid residues that mediates type II membrane anchoring of the proenzyme, activation occurs by removal of the propart
proteolytic modification
-
plasmepsin I is produced as a precursor. The propart region, about 120 residues, is more than twice as long as those of archetypal zymogens
proteolytic modification
-
proplasmepsin maturation appears to require acidic conditions, proplasmepsin maturation may not be autocatalytic in vivo
proteolytic modification
-
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 and is capable of autocatalytic activation at pH 4.05.5, which occurrs at Leu116PSer117P, seven residues upstream of the native cleavage site (Gly123P-Asn1)
proteolytic modification
automaturation of proPfPM1 K110pN mutant at pH 4.0-4.5, with reduction of molecular weight by 5 kDa
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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 PMIKNI-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
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
V110P
-
mutation in proplasmepsin I is responsible for generating a form of proplasmepsin I that is capable of undergoing autoactivation
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PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression and partial characterization of soluble recombinant PM I from Plasmodium falciparum in which a truncated form of PM I (Lys77PLeu329) (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
-
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
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 4.05.5, 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
-
expression of truncated proPfPM1 K110pN mutant 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
-
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REF.
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PUBMED ID
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New inhibitors of the malaria aspartyl proteases plasmepsin I and II
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272
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Plasmodium falciparum
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Plasmodium falciparum
brenda
Noteberg, D.; Hamelink, E.; Hulten, J.; Wahlgren, M.; Vrang, L.; Samuelsson, B.; Hallberg, A.
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46
734-746
2003
Plasmodium falciparum
brenda
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Active Site Contribution to Specificity of the Aspartic Proteases Plasmepsins I and II
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277
41009-41013
2002
Plasmodium falciparum
brenda
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
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454
210-214
1999
Plasmodium falciparum
brenda
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
brenda
Moon, R.P.; Tyas, L.; Certa, U.; Rupp, K.; Bur, D.; Jacquet, C.; Matile, H.; Loetscher, H.; Grueninger-Leitch, F.; et al.
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244
552-560
1997
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.
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Bioorg. Med. Chem.
14
2197-2208
2006
Plasmodium falciparum
brenda
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
brenda
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
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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
Hof, F.; Schutz, A.; Fah, C.; Meyer, S.; Bur, D.; Liu, J.; Goldberg, D.E.; Diederich, F.
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Angew. Chem.
45
2138-2141
2006
Plasmodium falciparum
brenda
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
brenda
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
brenda
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
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49
7440-7449
2006
Plasmodium falciparum
brenda
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
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Plasmodium falciparum
brenda
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
brenda
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
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2009
Plasmodium falciparum (P39898), Plasmodium falciparum
brenda
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
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Plasmodium falciparum
brenda
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Discovery of plasmepsin inhibitors by fragment-based docking and consensus scoring
ChemMedChem
4
1317-1326
2009
Plasmodium falciparum
brenda
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
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2011
Plasmodium falciparum (P39898), Plasmodium falciparum
brenda
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In silico docking roselle (Hibiscus sabdariffa L.) calyces flavonoids as antimalarial against plasmepsin 1 and plasmepsin 2
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Plasmodium falciparum (P39898)
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Chaudhary, K.K.; Raj, U; Varadwaj, P.K.; MishraNovel, N.
Novel potent plasmepsin-I (PMI) inhibitors an in-silico approach
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Plasmodium falciparum (P39898)
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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
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Plasmodium falciparum
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Thillainayagam, M.; Malathi, K.; Anbarasu, A.; Singh, H.; Bahadur, R.; Ramaiah, S.
Insights on inhibition of Plasmodium falciparum plasmepsin I by novel epoxyazadiradione derivatives - Molecular docking and comparative molecular field analysis
J. Biomol. Struct. Dyn.
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2019
Plasmodium falciparum (P39898), Plasmodium falciparum
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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
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Plasmodium falciparum (P39898)
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McGillewie, L.; Soliman, M.E.
Flap flexibility amongst plasmepsins I, II, III, IV, and V Sequence, structural, and molecular dynamics analyses
Proteins
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2015
Plasmodium falciparum (P39898), Plasmodium falciparum
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Fatimawali, Y.; Tallei, T.E.; Kepel, B.J.; Alorabi, M.; El-Shehawi, A.M.; Bodhi, W.; Tumilaar, S.G.; Celik, I.; Mostafa-Hedeab, G.; Mohamed, A.A.; Emran, T.B.
Appraisal of bioactive compounds of betel fruit as antimalarial agents by targeting plasmepsin 1 and 2 A computational approach
Pharmaceuticals (Basel)
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1285
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Plasmodium falciparum (P39898), Plasmodium falciparum HB3 (P39898)
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