Information on EC 3.4.23.39 - plasmepsin II

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The expected taxonomic range for this enzyme is: Plasmodium

EC NUMBER
COMMENTARY hide
3.4.23.39
-
RECOMMENDED NAME
GeneOntology No.
plasmepsin II
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Hydrolysis of the bonds linking certain hydrophobic residues in hemoglobin or globin. Also cleaves the small molecule substrates such as Ala-Leu-Glu-Arg-Thr-Phe!Phe(NO2)-Ser-Phe-Pro-Thr
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
hemoglobin degradation
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CAS REGISTRY NUMBER
COMMENTARY hide
159447-18-4
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
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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
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid + H2O
?
show the reaction diagram
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-
-
-
?
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid + H2O
?
show the reaction diagram
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-
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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
?
show the reaction diagram
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-
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?
Abz-Thr-Ile-Nle-(4-nitro)Phe-Gln-Arg-NH2 + H2O
Abz-Thr-Ile-Nle + (4-nitro)Phe-Gln-Arg-NH2
show the reaction diagram
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?
actin + H2O
?
show the reaction diagram
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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
show the reaction diagram
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?
Ala-Leu-Glu-Arg-Thr-Phe-Phe(NO2)-Ser-Phe-Pro-Thr + H2O
Ala-Leu-Glu-Arg-Thr-Phe + Phe(NO2)-Ser-Phe-Pro-Thr
show the reaction diagram
Ala-Leu-Glu-Arg-Thr-Phe-Phe(p-NO2)-Ser-Phe-Pro-Thr + H2O
Ala-Leu-Glu-Arg-Thr-Phe + Phe(p-NO2)-Ser-Phe-Pro-Thr
show the reaction diagram
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?
Arg-Gln-Phe-Phe(p-NO2)-Ile-Thr + H2O
Arg-Gln-Phe + Phe(p-NO2)-Ile-Thr
show the reaction diagram
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?
DABCYL-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-EDANS + H2O
?
show the reaction diagram
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FRET substrate, substrate is designed to mimic the hemoglobin cleavage site. The substrate is conjugated with the fluorescent donor EDANS and the quencher DABCYL
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?
DABCYL-L-Glu-L-Arg-L-Nle-L-Phe-L-Leu-L-Ser-L-Phe-L-Pro-EDANS + H2O
?
show the reaction diagram
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FRET-based substrate
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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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quenched fluorescent peptide substrate
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?
EDANS-CO-CH2-CH2-CO-L-Ala-L-Leu-L-Glu-L-Arg-L-Met-L-Phe-L-Leu-L-Ser-L-Phe-L-Pro-Dap(DABCYL)-OH + H2O
?
show the reaction diagram
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?
EDANS-CO-CH2-CH2-COALERMFLSFP-diaminopimelate-(DABCYL)OH + H2O
?
show the reaction diagram
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?
GST-SH3 peptide + H2O
?
show the reaction diagram
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Y-/-V and L-/-L are major cleavage sites
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?
Hemoglobin + H2O
?
show the reaction diagram
hemoglobin alpha-chain + H2O
?
show the reaction diagram
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cleavage sites: Phe33-/-Leu34, Thr108-/-Leu109, Leu136-/-Thr137
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?
hemoglobin beta-chain + H2O
?
show the reaction diagram
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cleavage site: Leu32-/-Val33
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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
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?
Leu-Ser-Phe(NO2)-Nle-Ala-Leu-OMe + H2O
?
show the reaction diagram
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?
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Ala-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Asp-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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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
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-4-nitrophenylalanine-Ala-Leu-Lys + H2O
?
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-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Lys-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Phe-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ala-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Asp-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Ala-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Asp-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ala-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Ala-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Arg + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Arg
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Asp + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Asp
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ile + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Ile
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ser + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Ser
show the reaction diagram
-
-
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Val + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Val
show the reaction diagram
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-
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Glu-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Glu-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Lys-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Lys-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ser-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Ser-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Val-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Val-Leu
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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chromogenic peptide substrate
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?
Lys-Pro-Ile-Leu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Leu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Lys-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Nle-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Ser-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ile-Val-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Val-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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-
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?
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Lys-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Phe-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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?
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ser-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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-
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?
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Ser-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
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-
-
-
?
Myoglobin + H2O
?
show the reaction diagram
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horse myoglobin is used
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?
p47phox-PX + H2O
?
show the reaction diagram
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PX domain of p47phox, a cytosolic factor of the neutrophil NADPH oxydase is digested
-
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?
plasmepsin 2 + H2O
?
show the reaction diagram
-
PSM2 auto-cleavage after F112 is complete after 20 min in 10 mM citrate pH 4.5
-
-
?
protein 4.1 + H2O
?
show the reaction diagram
-
-
-
-
?
spectrin + H2O
?
show the reaction diagram
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
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
plasmepsin 2 + H2O
?
show the reaction diagram
-
PSM2 auto-cleavage after F112 is complete after 20 min in 10 mM citrate pH 4.5
-
-
?
spectrin + H2O
?
show the reaction diagram
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1R,2R,3R,4R)-1,4-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-1,4-bis[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]butane-2,3-diol
-
-
(1RS) 3,3-difluoro-N-[2-(2-naphthyl)ethyl]-4-oxo-N-(4-pentylphenyl)cyclohexanecarboxamide
-
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(1RS,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
-
-
(1S,2S,3S,4R)-3-(4-bromophenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
(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
-
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(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
(1SR,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
-
-
(1Z)-N'-{[(4-chloro-3,5-dimethylphenoxy)acetyl]oxy}-2-(3,4-dimethoxyphenyl)ethanimidamide
-
-
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxyindan-1-yl)-butyramide
-
0.005 mM, 25% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 68% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
0.005 mM, 74% inhibition
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 39% of maximal activity
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 40% inhibition
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 54% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 43% inhibition
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 64% inhibition
(2R,3R)-4-[N-benzyl-N'-((S)-2-benzyloxycarbonylamino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
0.005 mM, 50% inhibition
(2R,3R)-4-[N-benzyl-N'-((S)-2-tert-butyloxycarbonyl-amino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxy-indan-1-yl)-butyramide
-
0.005 mM, 49% inhibition
(2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
-
(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)-2-methyl-1-(methylcarbamoyl)propyl]hexanediamide
-
-
(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-(3,5-dimethylisoxazol-4-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
(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
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-(5-methyl-1,3,4-oxadiazol-2-yl)pentanamide
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-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-[5-(2-phenylethyl)-1,3,4-oxadiazol-2-yl]pentanamide
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-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
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-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-5-[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]pentanamide
-
-
(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)-2-methyl-1-(methylcarbamoyl)propyl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
-
(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)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis[[(2E)-3-phenylprop-2-en-1-yl]oxy]hexanediamide
-
-
(2R,3R,4R,5R)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]-2,5-bis(prop-2-en-1-yloxy)hexanamide
-
-
(2R,3R,4R,5R)-5-(5-benzyl-1,3,4-oxadiazol-2-yl)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]pentanamide
-
-
(2R,3R,4R,5R)-5-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-1-oxa-7-azacyclohexadecane-2-carboxamide
-
-
(2R,3R,4R,5R)-6-(2-acetylhydrazino)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
-
-
(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
-
-
(2R,3R,4R,5R,14E)-5-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-1-oxa-7-azacyclohexadec-14-ene-2-carboxamide
-
-
(2R,3R,4S,6R)-6-[[(E)-2-(4-acetylphenyl)ethenyl]oxy]-2-[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]heptanediamide
-
inhibitor candidate, designed according to inhibitor modeling. Selectivity index Ki value Cathepsin D to Ki value PlmII is 333
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 35% inhibition
(2S,3S)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
0.005 mM, 20% inhibition
(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
-
-
(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)-4-[([4-[4-amino-3-(4-chlorophenyl)butanoyl]-1-(biphenyl-4-ylmethyl)piperazin-2-yl]acetyl)amino]-N-butyl-3-hydroxy-5-phenylpentanamide
-
-
(3S,4S)-4-[[(2S)-2-(benzylamino)-3-methylbutanoyl]amino]-N-[(1S)-1-(cyclohexylmethyl)-2-[[3-(1H-imidazol-1-yl)propyl]amino]-2-oxoethyl]-3-hydroxy-5-phenylpentanamide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-3-hydroxy-4-(2-thiophen-2-ylacetylamino)pentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-4-(3,3-diphenylpropionylamino)-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-5-(4-bromobenzyloxy)-4-diphenylacetylamino-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3R)-3-methyl-2-(2-(naphthalen-2-yl)acetamido)pentanamido)heptanamide
-
-
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
(3S,4S)-pyrrolidine-3,4-diyl bis(3,3-dimethylbutanoate)
-
-
(3S,4S)-pyrrolidine-3,4-diyl bis(3-methylbutanoate)
-
-
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-1-ylacetate)
-
-
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-2-ylacetate)
-
-
(3S,4S)-pyrrolidine-3,4-diyl bis(phenylacetate)
-
-
(3S,4S)-pyrrolidine-3,4-diyl dibenzoate
-
-
(3S,4S)-pyrrolidine-3,4-diyl dicyclohexanecarboxylate
-
-
(3S,6S,9S,12S,15S,18S)-15-(3-amino-3-oxopropyl)-18-sec-butyl-3,9-dibutyl-1-((S)-1-((S)-2,6-diaminohexanoyl)pyrrolidin-2-yl)-6-(hydroxymethyl)-12-isobutyl-1,4,7,13,16-pentaoxo-2,5,8,11,14,17-hexaazanonadecan-19-oic acid
-
-
(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-([N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl]amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide
-
-
(5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
-
(5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
-
(5S,8S,12S,13S,16S,19S)-13-benzyl-12-hydroxy-8,23,23-trimethyl-16,19-bis(1-methylethyl)-5-(2-methylpropyl)-4,7,10,15,18,21-hexaoxo-3,6,9,14,17,20-hexaazatetracosan-1-amide
-
-
(6S,9S,12R,13S,17S,20R,21S)-13,21-dihydroxy-2,17-dimethyl-6,9-bis(1-methylethyl)-4,7,10,15,18-pentaoxo-12,20-bis(trifluoromethyl)-5,8,11,16,19-pentaazatricosan-23-oic acid
-
-
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-(pyridine-2-ylmethyl)amino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.00030 mM
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-(pyridine-4-ylmethyl)amino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.00049 mM
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-ethylamino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.00072 mM
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-methylamino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.00045 mM
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(4-hydroxymethylphenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
anti-malarial activity, EC50 value 0.0011 mM
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)amide
-
-
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
-
1-(3-methylbutyl)-N-(4-pentylbenzyl)-N-(4-pyridin-3-ylbenzyl)piperidin-4-amine
-
-
1-(4-chlorophenyl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
-
IC50 700 nM for antiplasmodial activity
1-(4-nitrophenyl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
-
IC50 2100 nM for antiplasmodial activity
1-(biphenyl-4-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
-
highest antiplasmodial activity among compounds tested with IC50 of 160 nM
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-amide
-
-
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
-
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenylamino)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
-
1-Acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
-
1-Acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenylamino)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
-
1-methyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-(3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl)-amide
-
-
1-Methyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
-
1-Methyl-piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
1-methyl-piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
1-Methyl-piperidine-4-carboxylic acid {3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
1-[2-hydroxy-3-(1,2,3,4,5,6,7,8-octahydrophenanthren-9-yloxy)propyl]-4-(3-methoxyphenyl)piperazin-1-ium
-
-
17-benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16-tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
-
17-Benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
-
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-aminobenzoate)
-
Ki value for human cathepsin D 0.142 mM
2,3-difluoro-4-methyl-N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]benzamide
-
-
2,5-Bis-allyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
2,5-Bis-benzyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
2-(1,3-benzothiazol-2-ylamino)-N-(2-chlorophenyl)-6-oxo-1,4,5,6tetrahydro-4-pyrimidinecarboxamide
-
-
2-(1-naphthyl)-N'-[(4-nitrobenzoyl)oxy]ethanimidamide
-
-
2-(2-naphthyl)-N-(4-pentylphenyl)-N-piperidin-4-ylacetamide hydrochloride
-
-
2-([2-[4-([[3-(naphthalen-2-ylmethoxy)-7-azabicyclo[2.2.1]hept-2-yl]oxy]methyl)phenoxy]ethyl]sulfanyl)-1,3-benzothiazole
-
-
2-([4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-yl]oxy)ethanol
-
IC50: 441 nM
2-([N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-(methylsulfonyl)glycyl]amino)-N-isobutylbenzamide
-
-
2-anilino-3-chloro-N-phenyl-4-(phenylimino)-2-butenamide
-
-
2-anilino-4-(3-furyl)-6-oxo-N-phenyl-1-cyclohexene-1-carboxamide
-
-
2-[4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-yl]ethanol
-
IC50: 0.00147 mM
3'-(((1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-ylamino)methyl)biphenyl-2-ol
-
-
3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,5a,6,11,11a-octahydrotetracen-1-yl 3,4-di-O-acetyl-2,6-dideoxyhexopyranoside
-
-
3-amino-N-[(1S,3S,4S)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-1-(2-methylpropyl)-5-phenylpentyl]benzamide
-
-
3-chloro-N-([2-(2-methoxybenzoyl)hydrazino]carbonothioyl)-1-benzothiophene-2-carboxamide
-
-
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
-
-
4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-carbonitrile
-
IC50: 713 nM; IC50: 918 nM
4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-3-carboxylic acid
-
IC50: 208 nM
4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-carboxylic acid
-
IC50: 495 nM
4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)-N,N-dimethylbiphenyl-4-carboxamide
-
IC50: 77 nM
4-(1,3-benzodioxol-5-yl)-Nalpha-[(2S,3S)-2-hydroxy-3-([N-[3-(1H-indol-3-yl)propanoyl]-L-valyl]amino)-4-phenylbutyl]-L-phenylalaninamide
-
-
4-(1-benzofuran-2-yl)-Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
4-(benzyloxy)-N-[(1S,2S)-3-[(1-benzylpiperidin-4-yl)amino]-1-(cyclohexylmethyl)-2-hydroxypropyl]-3,5-dimethoxybenzamide
-
-
4-([[(4-phenoxyphenyl)amino]carbonyl]amino)benzenecarboximidamide
-
-
4-amino-N'-(benzyloxy)-N-(2-methylphenyl)-1,2,5-oxadiazole-3carboximidamide
-
-
4-amino-N'-(benzyloxy)-N-(4-methylphenyl)-1,2,5-oxadiazole-3carboximidamide
-
-
4-amino-N'-[(2,4-dichlorobenzyl)oxy]-N-(2-methylphenyl)-1,2,5oxadiazole-3-carboximidamide
-
-
4-amino-N'-[(2-methyl-1-naphthyl)methoxy]-1,2,5-oxadiazole-3carboximidamide
-
-
4-amino-N-[(1S,3S,4S)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-1-(2-methylpropyl)-5-phenylpentyl]benzamide
-
-
4-butoxy-N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)benzamide
-
IC50: 0.0059 mM
4-butoxy-N-[2-(dibutylamino)ethyl]-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 0.0103 mM
4-butyl-N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)benzamide
-
IC50: 0.0023 mM
4-butyl-N-[2-(dibutylamino)ethyl]-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 0.0039 mM
4-chloro-5-(4-chlorophenoxy)-2-[([[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl)amino]benzenesulfonate
-
-
4-methoxy-N-(2-[5-(2-nitrophenyl)-2-furyl]-1-([(4-pyridinylmethyl)amino]carbonyl)vinyl)benzamide
-
-
5-[bis[(benzyloxy)carbonyl]amino]-6-[[1-hydrazinyl-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-oxohexan-1-aminium
-
-
6-((2-[(5-chloro-2-methoxyphenyl)amino]-2-oxoethyl)thio)-5-cyano-N-(2-methoxyphenyl)-2-methyl-4-phenyl-1,4-dihydro-3-pyridinecarboxamide
-
-
6-bromo-2,3,4,9-tetrahydro-1H-carbazol-1-one Nphenylthiosemicarbazone
-
-
6-[3-(1,3-benzothiazol-2-ylsulfanyl)propyl]-7-(2-naphthalen-1-ylethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
-
-
Ac-Val-Val-Sta-Ala-Sta
-
IC50: 0.6 nM
benzo[1,3]dioxole-5-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-amide
-
-
benzyl 2-benzyl-2-[(2S,3R)-3-[(4-bromobenzyl)oxy]-2-hydroxy-4-oxo-4-[(2-piperidin-1-ylethyl)amino]butyl]hydrazinecarboxylate
-
-
benzyl 3-benzyl-4-([2-[(1-formyl-3-methylbutyl)amino]-2-oxo-1-phenylethyl]amino)-4-oxobutanoate
-
-
benzyl [(1S,4S,5R,6R,7S,10S)-4,7-bis[(4-cyanophenoxy)methyl]-5,6-dihydroxy-1,10-bis(1-methylethyl)-2,9,12-trioxo-14-phenyl-13-oxa-3,8,11-triazatetradec-1-yl]carbamate
-
-
butyloxycarbonyl-His-Pro-Phe-His-Leu-PSI[CH(OH)-CH2]-Val-Ile-His
-
IC50: 150 nM
butyloxycarbonyl-His-Pro-Phe-His-Sta-Leu-Phe-NH2
-
IC50: 1000 nM
Chloroquine-hemin complex
-
-
extract from Plexaura homomalla
-
black sea rod, extract contains a reversible tight-binding inhibitor
-
extract from Xestospongia muta
-
giant barrel sponge, extract contains a reversible tight-binding inhibitor
-
Iva-Val-Val-Sta-Ala-Sta
L-lysyl-L-prolyl-L-phenylalanyl-N-[(1S)-1-benzyl-2-[[(1S)-1-benzyl-2-[[(1S)-2-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-1-(hydroxymethyl)-2-oxoethyl]amino]-2-oxoethyl]amino]ethyl]-L-norleucinamide
-
-
Lac-Val-Sta-Ala-Sta
-
IC50: 100 mM
LCu(CH3COO)2
-
copper(II) nanohybrid solids are synthesized and are shown to be capped by a bis(benzimidazole) diamide ligand (L)
LCuCl2
-
copper(II) nanohybrid solids are synthesized and are shown to be capped by a bis(benzimidazole) diamide ligand (L)
methyl 4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-carboxylate
-
-
methyl [4'-(([1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetate
-
-
methyl [4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-yl]acetate
-
IC50: 124 nM
methyl [4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetate
-
IC50: 183 nM
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylcyclohexyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
N',N'''-1,2-phenylenebis[N-(3-chlorophenyl)urea]
-
-
N'-[(4-methoxy-3-nitrobenzoyl)oxy]-2-(1-naphthyl)ethanimidamide
-
-
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
-
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-phenylacetamide)
-
-
N,N'-([(4,6-dimethyl-2-quinazolinyl)amino]methylylidene)dipropanamide
-
-
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
-
-
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyridin-2-ylbenzyl)ethane-1,2-diamine
-
IC50: 0.0013 mM
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyridin-4-ylbenzyl)ethane-1,2-diamine
-
IC50: 0.001603 mM
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyrimidin-5-ylbenzyl)ethane-1,2-diamine
-
IC50: 0.001631 nM
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-([4'-(2-pyrrolidin-1-ylethoxy)biphenyl-4-yl]methyl)ethane-1,2-diamine
-
IC50: 0.002 mM
N,N-dibutyl-N'-[(2'-fluorobiphenyl-4-yl)methyl]-N'-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 0.001022 mM
N-((1S,2S)-1-(4-benzo[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-methyl-4-oxo-1,4-dihydro-2-pyrimidinyl)amino]methylene)benzamide
-
-
N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-oxo-4-propyl-1,6-dihydro-2-pyrimidinyl)amino]methylene)-4-methoxybenzamide
-
-
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-4-methyl-1-oxopentan-2-yl)-4-(4-((2S,3R)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamid
-
-
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
-
-
N-((4'-[2-(benzylamino)-2-oxoethyl]biphenyl-4-yl)methyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 46 nM
N-((S)-1-(((2S,3S)-3-hydroxy-5-oxo-5-(((S)-1-oxo-3-phenyl-1-(prop-2-yn-1-ylamino)propan-2-yl)amino)-1-phenylpentan-2-yl)-amino)-3-methyl-1-oxobutan-2-yl)picolinamide
-
-
N-((S)-1-(((2S,3S)-5-(((R)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-chloro-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
-
-
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-1-oxopent-4-yn-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
-
-
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-cyano-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)picolinamide
-
-
N-(([2-(4-ethylphenyl)-6-methyl-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
-
-
N-(([6-methyl-2-(4-methylphenyl)-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
-
-
N-(1,3-benzodioxol-5-ylmethyl)-N'-[4-(2-oxo-2H-chromen-3-yl)-1,3thiazol-2-yl]succinamide
-
-
N-(2-([3-(1,3-benzodioxol-5-yl)-3-oxo-1-propen-1-yl]amino)phenyl)-4-nitrobenzenesulfonamide
-
-
N-(2-aminoethyl)-N-(biphenyl-4-ylmethyl)-4-pentylbenzamide
-
IC50: 0.003329 nM
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(2,5-dimethyl-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
N-(2-Benzo[1,3]dioxol-5-yl-ethyl)-N-{3-[2-(2,5-dimethyl-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
N-(2-Benzo[1,3]dioxol-5-yl-ethyl)-N-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
N-(2-methoxyphenyl)-2-(5H-[1,2,4]triazino[5,6-b]indol-3ylthio)butanamide
-
-
N-(3,4-dichlorophenyl)-2-[(4,6-dimethyl-2-pyrimidinyl)amino]3a,4,5,6,7,7a-hexahydro-1H-benzimidazole-1-carboxamide
-
-
N-(3,4-dimethylphenyl)-N'-(imino[(4,6,7-trimethyl-2-quinazolinyl)amino]methyl)thiourea
-
-
N-(3-{(2-Benzo[1,3]dioxol-5-yl-ethyl)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionyl]-amino}-1-benzyl-2-hydroxy-propyl)-4-benzyloxy-3,5-dimethoxy-benzamide
-
-
N-(4-hexylphenyl)-2-(2-naphthyl)-N-piperidin-4-ylacetamide hydrochloride
-
-
N-(4-[5-(1,3-benzodioxol-5-yl)pyridin-2-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 1912 nM
N-(4-[6-(1,3-benzodioxol-5-yl)pyridin-3-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 437 nM
N-(4-[benzyl(methyl)amino]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 289 nM
N-(amino[(4,6-dimethyl-2-quinazolinyl)amino]methylene)-2-(4-chlorophenyl)acetamide
-
-
N-(biphenyl-4-ylmethyl)-4-butoxy-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0047 mM
N-(biphenyl-4-ylmethyl)-4-butyl-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0015 mM
N-(biphenyl-4-ylmethyl)-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 0.002067 mM
N-(biphenyl-4-ylmethyl)-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 0.003943 mM
N-(biphenyl-4-ylmethyl)-N-[2-(butylamino)ethyl]-4-pentylbenzamide
-
IC50: 0.001161 mM
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-propylbenzamide
-
IC50: 0.0129 mM
N-(biphenyl-4-ylmethyl)-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
-
IC50: 0.002317 mM
N-([(1RS)-3,3-difluoro-4-oxocyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1RS)-3,3-difluoro-4-oxocyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1RS,4RS)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1RS,4SR)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1SR,4RS)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(1SR,4SR)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-([(2,4-dimethylphenyl)amino][(4-oxo-1,4,5,6,7,8-hexahydro-2-quinazolinyl)amino]methylene)benzamide
-
-
N-([3',5'-bis(trifluoromethyl)biphenyl-4-yl]methyl)-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0017 mM
N-([3',5'-bis(trifluoromethyl)biphenyl-4-yl]methyl)-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
IC50: 0.00119 mM
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
-
-
N-acetyl-L-leucyl-L-leucyl-norleucinal
-
-
N-benzyl-2-([3-(3-nitrophenyl)acryloyl]amino)benzamide
-
-
N-benzyl-2-bromo-N-[(4-[[2-(2,4-dichlorophenyl)ethyl](4-phenylbutanoyl)amino]pyrrolidin-3-yl)methyl]-4,5-dimethoxybenzamide
-
-
N-benzyl-2-bromo-N-[(4-[[2-(2,4-dichlorophenyl)ethyl][3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoyl]amino]pyrrolidin-3-yl)methyl]-4,5-dimethoxybenzamide
-
-
N-benzyl-4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-carboxamide
-
IC50: 72 nM
N-butyl-N-[2-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-hydroxyethyl]butan-1-aminium
-
-
N-hexyl-N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]hexan-1-aminium
-
-
N-hexyl-N-[2-hydroxy-2-(phenanthren-9-yl)ethyl]hexan-1-aminium
-
-
N-[(1S)-1-([(1S,2S)-1-([(4-bromobenzyl)oxy]methyl)-4-([(1S)-2-([(1S)-1-carbamoylbutyl]amino)-2-hydroxy-1-methylethyl]amino)-2-hydroxy-4-oxobutyl]carbamoyl)-2-methylpropyl]-4,5-dihydropyridine-2-carboxamide
-
-
N-[(1S)-1-([(1S,2S)-3-[(2-amino-2-oxoethyl)(benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl)-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-([[4-(1,3-benzodioxol-5-yl)benzyl]oxy]methyl)-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-benzyl-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-([(1S)-2-amino-1-[(4'-methylbiphenyl-4-yl)methyl]-2-oxoethyl]amino)-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-3-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl](benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-cyclo-hexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-3-cyclohexylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butyl-carbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
N-[(1S,2S)-3-[[2-(1,3-benzodioxol-5-yl)ethyl][3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoyl]amino]-1-benzyl-2-hydroxypropyl]-4-(benzyloxy)-3,5-dimethoxybenzamide
-
-
N-[(1SR,3RS)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-[(1SR,3SR)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
-
N-[(2'-chlorobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 191 nM
N-[(2S,3S)-2-hydroxy-3-[(phenoxyacetyl)amino]-4-phenylbutyl]-N-[2-(4-methoxyphenyl)ethyl]piperidine-4-carboxamide
-
inhibitor candidate, designed according to inhibitor modeling. Selectivity index Ki value Cathepsin D to Ki value PlmII is 15
N-[(2S,3S)-3-[[(3-chlorophenoxy)acetyl]amino]-2-hydroxy-4-phenylbutyl]-N-[2-(4-methoxyphenyl)ethyl]piperidine-4-carboxamide
-
-
N-[(2S,3S)-5-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-[(4-bromobenzyl)oxy]-3-hydroxy-5-oxopentan-2-yl]-2,4,6-trifluorobenzamide
-
inhibitor candidate, designed according to inhibitor modeling. Selectivity index Ki value Cathepsin D to Ki value PlmII is above 400
N-[(3S)-3-[(2S,5S,14S)-14-[(3,3-dimethylbutanoyl)amino]-2-(1-methylethyl)-3,11,15-trioxo-1,4,10-triazacyclopentadecan-5-yl]-3-hydroxypropanoyl]-L-valyl-L-leucylglycinamide
-
-
N-[(3S,4S)-3-hydroxy-6-phenyl-4-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]hexanoyl]-L-alanyl-L-leucinamide
-
-
N-[(4'-butylbiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 591 nM
N-[(4'-chlorobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 446 nM
N-[(4'-chlorobiphenyl-4-yl)methyl]-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
IC50: 407 nM
N-[(4'-cyanobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 160 nM
N-[(cyclopentylamino)carbonothioyl]-4-ethoxy-3-nitrobenzamide
-
-
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-(dibutylamino)ethyl]-4-pentyl-N-(3-phenoxybenzyl)benzamide
-
IC50: 469 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-piperidin-1-ylbenzyl)benzamide
-
IC50: 369 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-2-ylbenzyl)benzamide
-
IC50: 380 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-3-ylbenzyl)benzamide
-
IC50: 374 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-4-ylbenzyl)benzamide
-
IC50: 212 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyrimidin-5-ylbenzyl)benzamide
-
IC50: 531 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-thiomorpholin-4-ylbenzyl)benzamide
-
IC50: 188 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-([4'-(thiomorpholin-4-ylcarbonyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 56 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(1H-pyrrol-1-yl)benzyl]benzamide
-
IC50: 240 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(4-phenylpiperazin-1-yl)benzyl]benzamide
-
IC50: 200 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-phenylpyridin-2-yl)benzyl]benzamide
-
IC50: 2345 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-pyrimidin-5-ylpyridin-2-yl)benzyl]benzamide
-
IC50: 8530 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-phenylpyridin-3-yl)benzyl]benzamide
-
IC50: 589 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-pyrimidin-5-ylpyridin-3-yl)benzyl]benzamide
-
IC50: 2229 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(phenylamino)benzyl]benzamide
-
IC50: 224 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(pyridin-4-ylamino)benzyl]benzamide
-
IC50: 1816 nM
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 596 nM
N-[2-(dibutylamino)ethyl]-4-propyl-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 0.0396 mM
N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)-4-propylbenzamide
-
IC50: 0.0159 mM
N-[2-(dibutylamino)ethyl]-N-(4-pyridin-4-ylbenzyl)benzamide
-
IC50: 295 nM
N-[2-(dibutylamino)ethyl]-N-(4-pyrimidin-5-ylbenzyl)benzamide
-
IC50: 204 nM; IC50: 351 nM
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(phenyl)amino]benzyl)-4-pentylbenzamide
-
IC50: 574 nM
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(pyridin-4-yl)amino]benzyl)-4-pentylbenzamide
-
IC50: 3015 nM
N-[2-(dibutylamino)ethyl]-N-([3'-(trifluoromethyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 390 nM
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)-4-pentylbenzamide
-
IC50: 511 nM
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)benzamide
-
IC50: 104 nM
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 151 nM
N-[2-(dibutylamino)ethyl]-N-([4'-(2-morpholin-4-yl-2-oxoethyl)biphenyl-4-yl]methyl)-4-pentylbenzamide
-
IC50: 74 nM; IC50: 91 nM
N-[2-(dibutylamino)ethyl]-N-[(3',4'-dimethoxybiphenyl-4-yl)methyl]benzamide
-
IC50: 428 nM
N-[2-(dibutylamino)ethyl]-N-[(3'-methylbiphenyl-4-yl)methyl]benzamide
-
IC50: 293 nM
N-[2-(dibutylamino)ethyl]-N-[4-(1H-indol-1-yl)benzyl]-4-pentylbenzamide
-
IC50: 670 nM
N-[2-(dibutylamino)ethyl]-N-[4-(4-methylpiperazin-1-yl)benzyl]-4-pentylbenzamide
-
IC50: 2547 nM
N-[2-(dibutylamino)ethyl]-N-[4-(diethylamino)benzyl]-4-pentylbenzamide
-
IC50: 1491 nM
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-4-methyl-N-(4-methylpentyl)pentan-1-aminium
-
-
N-[2-hydroxy-2-(1,2,3,4-tetrahydrophenanthren-9-yl)ethyl]-N-pentylpentan-1-aminium
-
-
N-[3-(2,7-dichloro-9H-fluoren-4-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[3-(9H-fluoren-2-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[3-(dibutylamino)propyl]-4-pentyl-N-([4'-(2-pyrrolidin-1-ylethoxy)biphenyl-4-yl]methyl)benzamide
-
IC50: 221 nM
N-[3-(dibutylamino)propyl]-N-[(2'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 0.0011 mM; IC50: 322 nM
N-[3-(dibutylamino)propyl]-N-[(2'-methylbiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 597 nM
N-[3-(dibutylamino)propyl]-N-[(3',4'-dimethoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 468 nM
N-[3-(dibutylamino)propyl]-N-[(3'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 580 nM
N-[3-(dibutylamino)propyl]-N-[(4'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 246 nM
N-[3-[(2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionyl]-amino]-1-benzyl-2-hydroxy-propyl]-4-benzyloxy-3,5-dimethoxy-benzamide
-
-
N-[3-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
-
N-[4,4-difluoro-3-oxocyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)-acetamide
-
-
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]-2-methoxypyridine-4-carboxamide
-
IC50: 154 nM
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-3-carboxamide
-
IC50: 202 nM
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-4-carboxamide
-
IC50: 464 nM
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]pyrazine-2-carboxamide
-
IC50: 243 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-piperidin-1-ylethyl)benzamide
-
IC50: 334 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-[4-(3-phenylpropyl)piperidin-1-yl]ethyl)benzamide
-
IC50: 165 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 831 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-([2-(diethylamino)ethyl](ethyl)amino)ethyl)-4-pentylbenzamide
-
IC50: 439 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-morpholin-4-ylethyl)-4-pentylbenzamide
-
IC50: 2897 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[benzyl(2-hydroxyethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 334 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 1501 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(3-butylheptyl)-4-pentylbenzamide
-
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(4-benzylpiperidin-1-yl)ethyl]-4-pentylbenzamide
-
IC50: 190 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 101 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 56 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
-
IC50: 1519 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dipropylamino)ethyl]-4-pentylbenzamide
-
IC50: 531 nM
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
IC50:195 nM
N-[4-(2,2'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 587 nM; IC50: 736 nM
N-[4-(2,4'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 642 nM
N-[4-(3,3'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 5266 nM
N-[4-(3,4'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 4553 nM
N-[4-(3,4-diethylisoxazol-5-yl)benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[4-(4-benzylpiperazin-1-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 646 nM
N-[4-(benzylamino)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 429 nM
N-[4-(benzyloxy)benzyl]-4-butoxy-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0034 mM
N-[4-(benzyloxy)benzyl]-4-butyl-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0013 mM
N-[4-(benzyloxy)benzyl]-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 845 nM
N-[4-(benzyloxy)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 112 nM
N-[4-(benzyloxy)benzyl]-N-[2-(dibutylamino)ethyl]-4-propylbenzamide
-
IC50: 0.0089 mM
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
-
-
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
N-[[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
pepstatin A
Piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
Piperidine-4-carboxylic acid {3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
pyridine-2-carboxylic acid ((R)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(3-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-(3-methoxyphenyl)ethylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-3-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcar-bamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcarbamoyl)-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-benzyloxymethyl-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-1-phenethylpropylcarbamoyl)-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-phenylaminoethyl-carbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-phenylpropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(4-cyanobenzylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(cyclohexylmethylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-butylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methylpropyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-butylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(3-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
pyridine-2-carboxylic acid((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
Ro17-7109
-
-
-
SC-50083
-
IC50: 0.0003467 mM
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
-
-
[4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-yl]acetic acid
-
IC50: 197 nM
[4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetic acid
-
IC50: 463 nM
[5-([[(4-bromophenyl)carbonyl]oxy]methyl)-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
-
Ki value for human cathepsin D 0.165 mM
[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl 7aH-indole-3-carboxylate
-
Ki value for human cathepsin D above 0.1 mM
[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
Ki value for human cathepsin D 0.262 mM
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
Ki value for human cathepsin D 0.051 mM
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.001 - 0.00233
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
0.00294 - 0.00611
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
0.000489
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, 37C
0.063
Abz-Thr-Ile-Nle-(4-nitro)Phe-Gln-Arg-NH2
-
pH 4.5, temperature not specified in the publication
0.0139 - 0.0334
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
0.06 - 0.11
Ala-Leu-Glu-Arg-Thr-Phe-Phe(NO2)-Ser-Phe-Pro-Thr
0.00017 - 0.0012
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
0.006 - 0.025
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
0.02
Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37C
0.0274
Leu-Ser-Phe(NO2)-Nle-Ala-Leu-Ome
-
pH 4.4, 37C
0.03 - 0.069
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
0.055 - 0.109
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
0.006 - 0.008
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
0.025
Lys-Glu-Phe-Ile-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C
0.046
Lys-Glu-Phe-Val-Lys-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, mutant enzyme S77D
0.007 - 0.02
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
0.01
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
-
pH 4.4, 37C, recombinant enzyme
0.051 - 0.117
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
0.021 - 0.085
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
0.037 - 0.053
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu
0.087 - 0.221
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu
0.006 - 0.041
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu
0.024 - 0.076
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
0.013
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ala-Leu
-
pH 4.4, 37C
0.171
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Arg
-
pH 4.4, 37C
0.101
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Asp
-
pH 4.4, 37C
0.013
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ile
-
pH 4.4, 37C
0.023 - 0.07
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
0.067
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ser
-
pH 4.4, 37C
0.017
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Val
-
pH 4.4, 37C
0.081
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Glu-Leu
-
pH 4.4, 37C
0.056
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Lys-Leu
-
pH 4.4, 37C
0.052
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ser-Leu
-
pH 4.4, 37C
0.016
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Val-Leu
-
pH 4.4, 37C
0.008
Lys-Pro-Ile-Leu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.004 - 0.05
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
0.022
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.017 - 0.039
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu
0.006 - 0.01
Lys-Pro-Ile-Val-Phe-Phe(NO2)-Arg-Leu
0.035 - 0.25
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu
0.024 - 0.07
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu
0.056 - 0.092
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu
0.049 - 0.11
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
additional information
additional information
-
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.952 - 2.52
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
0.431 - 6.08
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
2.31
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-(gamma-aminobutyryl)-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
Plasmodium falciparum
-
pH 5.0, 37C
2.1 - 7.4
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
3.8 - 6
Ala-Leu-Glu-Arg-Thr-Phe-Phe(NO2)-Ser-Phe-Pro-Thr
0.103 - 2.1
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
10 - 15
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
9
Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe
Plasmodium falciparum
-
pH 4.4, 37C
10.4
Leu-Ser-Phe(NO2)-Nle-Ala-Leu-Ome
Plasmodium falciparum
-
pH 4.4, 37C
0.8 - 2
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
0.6 - 1.1
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
1.5 - 6
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
7
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys
Plasmodium falciparum
-
pH 4.4, 37C, recombinant enzyme
15.2
Lys-Glu-Phe-Ile-Phe-Phe(NO2)-Ala-Leu-Lys
Plasmodium falciparum
-
pH 4.4, 37C
0.84
Lys-Glu-Phe-Val-Lys-Phe(NO2)-Ala-Leu-Lys
Plasmodium falciparum
-
pH 4.4, 37C, mutant enzyme S77D
9.05 - 19
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
11
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
Plasmodium falciparum
-
pH 4.4, 37C, recombinant enzyme
0.17 - 0.4
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
1 - 2.6
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
0.5 - 0.53
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu
0.3 - 0.4
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu
0.73 - 1.8
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu
0.25 - 0.86
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
5.7
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ala-Leu
Plasmodium falciparum
-
pH 4.4, 37C
0.53
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Arg
Plasmodium falciparum
-
pH 4.4, 37C
1.2
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Asp
Plasmodium falciparum
-
pH 4.4, 37C
0.9
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ile
Plasmodium falciparum
-
pH 4.4, 37C
1.7 - 3.5
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
0.44
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ser
Plasmodium falciparum
-
pH 4.4, 37C
0.7
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Val
Plasmodium falciparum
-
pH 4.4, 37C
6.3
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Glu-Leu
Plasmodium falciparum
-
pH 4.4, 37C
1.6
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Lys-Leu
Plasmodium falciparum
-
pH 4.4, 37C
1.7
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ser-Leu
Plasmodium falciparum
-
pH 4.4, 37C
2.6
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Val-Leu
Plasmodium falciparum
-
pH 4.4, 37C
1.7
Lys-Pro-Ile-Leu-Phe-Phe(NO2)-Arg-Leu
Plasmodium falciparum
-
pH 4.4, 37C
0.03 - 0.08
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
3.1
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu
Plasmodium falciparum
-
pH 4.4, 37C
0.73 - 1.1
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu
1.6 - 3.6
Lys-Pro-Ile-Val-Phe-Phe(NO2)-Arg-Leu
0.05 - 0.1
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu
2.4 - 3.1
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu
0.2 - 0.32
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu
1 - 1.3
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
additional information
additional information
Plasmodium falciparum
-
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
620 - 1660
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0014
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
-
0.00012
(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
-
-
0.00038
(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
-
-
0.000085
(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
-
-
0.000011
(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
-
-
0.000006
(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
-
-
0.000145
(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
-
-
0.000007
(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
-
-
0.000142
(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
-
-
0.0015
(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
-
-
0.0041
(2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S)-2-methyl-1-(methylcarbamoyl)propyl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
-
0.000096
(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
-
-
0.000013
(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
-
-
0.000181
(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
-
-
0.000014
(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
-
-
0.000015
(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
-
-
0.000006
(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
0.000059
(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
-
-
0.000129
(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
-
-
0.000047
(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
-
-
0.000029
(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
-
-
0.000041
(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
-
-
0.00013
(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
-
-
0.000032
(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
-
-
0.0000089
(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
-
-
0.000015
(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
-
-
0.0011
(2R,3R,4R,5R,14E)-5-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-1-oxa-7-azacyclohexadec-14-ene-2-carboxamide
-
-
0.003
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
-
0.0015
(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
-
-
0.00054
(2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000129
(2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.00093
(2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.00015
(2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000121
(2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.00143
(2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000379
(2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000579
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000117
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.00049
(3S,4S)-4-[([4-[4-amino-3-(4-chlorophenyl)butanoyl]-1-(biphenyl-4-ylmethyl)piperazin-2-yl]acetyl)amino]-N-butyl-3-hydroxy-5-phenylpentanamide
-
-
0.000007
(3S,4S)-4-[[(2S)-2-(benzylamino)-3-methylbutanoyl]amino]-N-[(1S)-1-(cyclohexylmethyl)-2-[[3-(1H-imidazol-1-yl)propyl]amino]-2-oxoethyl]-3-hydroxy-5-phenylpentanamide
-
-
0.348
(3S,4S)-5-(4-bromobenzyloxy)-3-hydroxy-4-(2-thiophen-2-ylacetylamino)pentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.284
(3S,4S)-5-(4-bromobenzyloxy)-4-(3,3-diphenylpropionylamino)-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.139
(3S,4S)-5-(4-bromobenzyloxy)-4-diphenylacetylamino-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.00005
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3R)-3-methyl-2-(2-(naphthalen-2-yl)acetamido)pentanamido)heptanamide
-
-
0.0000589
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
0.0472
(3S,4S)-pyrrolidine-3,4-diyl bis(3,3-dimethylbutanoate)
-
pH 4.5, temperature not specified in the publication
0.0512
(3S,4S)-pyrrolidine-3,4-diyl bis(3-methylbutanoate)
-
pH 4.5, temperature not specified in the publication
0.0001
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-1-ylacetate)
-
pH 4.5, temperature not specified in the publication
0.001
(3S,4S)-pyrrolidine-3,4-diyl bis(naphthalen-2-ylacetate)
-
pH 4.5, temperature not specified in the publication
0.0114
(3S,4S)-pyrrolidine-3,4-diyl bis(phenylacetate)
-
pH 4.5, temperature not specified in the publication
0.019
(3S,4S)-pyrrolidine-3,4-diyl dibenzoate
-
pH 4.5, temperature not specified in the publication
0.163
(3S,4S)-pyrrolidine-3,4-diyl dicyclohexanecarboxylate
-
pH 4.5, temperature not specified in the publication
0.000014
(3S,6S,9S,12S,15S,18S)-15-(3-amino-3-oxopropyl)-18-sec-butyl-3,9-dibutyl-1-((S)-1-((S)-2,6-diaminohexanoyl)pyrrolidin-2-yl)-6-(hydroxymethyl)-12-isobutyl-1,4,7,13,16-pentaoxo-2,5,8,11,14,17-hexaazanonadecan-19-oic acid
-
-
0.0000005
(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
-
-
0.00007
(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
-
-
0.0000928
(5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
-
0.00000004
(5S,8S,12S,13S,16S,19S)-13-benzyl-12-hydroxy-8,23,23-trimethyl-16,19-bis(1-methylethyl)-5-(2-methylpropyl)-4,7,10,15,18,21-hexaoxo-3,6,9,14,17,20-hexaazatetracosan-1-amide
-
-
0.0000013
(6S,9S,12R,13S,17S,20R,21S)-13,21-dihydroxy-2,17-dimethyl-6,9-bis(1-methylethyl)-4,7,10,15,18-pentaoxo-12,20-bis(trifluoromethyl)-5,8,11,16,19-pentaazatricosan-23-oic acid
-
-
0.00001
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-(pyridine-2-ylmethyl)amino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
pH 4.0, 25C
0.000006
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-(pyridine-4-ylmethyl)amino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
pH 4.0, 25C
0.000007
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-ethylamino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
pH 4.0, 25C
0.000025
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(2,6-dimethyl-4-methylamino-phenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
pH 4.0, 25C
0.00001
(R)-N-[(1S,2R)-2-hydroxyindan-1-yl]-3-[(2S,3S)-3-(4-hydroxymethylphenoxyacetyl)amino-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
pH 4.0, 25C
0.144
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)amide
-
-
0.000011
(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
0.0000099
(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
-
-
0.000013
1-(3-methylbutyl)-N-(4-pentylbenzyl)-N-(4-pyridin-3-ylbenzyl)piperidin-4-amine
-
-
0.0000048
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-amide
-
-
0.000004
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
-
0.000003
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenylamino)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
-
0.000002
1-methyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-(3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl)-amide
-
-
0.0000041
1-Methyl-piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
0.000002
1-methyl-piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
0.0015
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
-
-
0.0008
2,3,4,7-tetrahydro-1H-azepine-3,5-diyldimethanediyl bis(4-aminobenzoate)
-
-
0.000096
2,5-Bis-allyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
0.000085
2,5-Bis-benzyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
4
2-([2-[4-([[3-(naphthalen-2-ylmethoxy)-7-azabicyclo[2.2.1]hept-2-yl]oxy]methyl)phenoxy]ethyl]sulfanyl)-1,3-benzothiazole
-
-
0.000018
3-amino-N-[(1S,3S,4S)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-1-(2-methylpropyl)-5-phenylpentyl]benzamide
-
-
0.000065
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
-
-
0.00003
4-(1-benzofuran-2-yl)-Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.02
4-(benzyloxy)-N-[(1S,2S)-3-[(1-benzylpiperidin-4-yl)amino]-1-(cyclohexylmethyl)-2-hydroxypropyl]-3,5-dimethoxybenzamide
-
-
0.0061
4-([[(4-phenoxyphenyl)amino]carbonyl]amino)benzenecarboximidamide
-
-
0.00003
4-amino-N-[(1S,3S,4S)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-1-(2-methylpropyl)-5-phenylpentyl]benzamide
-
-
0.00006
4-chloro-5-(4-chlorophenoxy)-2-[([[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl)amino]benzenesulfonate
-
-
0.002
6-[3-(1,3-benzothiazol-2-ylsulfanyl)propyl]-7-(2-naphthalen-1-ylethoxy)-1,2,3,4-tetrahydro-1,4-epiminonaphthalene
-
-
0.131
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
-
-
0.0004
benzyl 2-benzyl-2-[(2S,3R)-3-[(4-bromobenzyl)oxy]-2-hydroxy-4-oxo-4-[(2-piperidin-1-ylethyl)amino]butyl]hydrazinecarboxylate
-
-
0.0007
benzyl 3-benzyl-4-([2-[(1-formyl-3-methylbutyl)amino]-2-oxo-1-phenylethyl]amino)-4-oxobutanoate
-
-
0.00000025
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
-
-
0.0000019
extract from Plexaura homomalla
-
pH 4.4, 37C
-
0.0000464
extract from Xestospongia muta
-
pH 4.4, 37C
-
0.000044
L-lysyl-L-prolyl-L-phenylalanyl-N-[(1S)-1-benzyl-2-[[(1S)-1-benzyl-2-[[(1S)-2-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-1-(hydroxymethyl)-2-oxoethyl]amino]-2-oxoethyl]amino]ethyl]-L-norleucinamide
-
-
0.01
LCu(CH3COO)2
-
pH 4.7, 37C
0.013
LCuCl2
-
pH 4.7, 37C
0.000034
methyl 4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-carboxylate
-
-
0.004
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
-
pH 4.4, 37C
0.00043
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(N-benzyl-2-phenylacetamide)
-
pH 4.5, temperature not specified in the publication
0.000019
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
-
-
0.39
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
0.01
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
0.091
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
0.000308
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
0.000048
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.000693
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
0.00001
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
-
-
0.00000059
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-4-methyl-1-oxopentan-2-yl)-4-(4-((2S,3R)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.0000039
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
-
-
0.0000263
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
0.000103
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
-
-
0.0000121
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
0.000112
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
-
-
0.000035
N-((S)-1-(((2S,3S)-5-(((R)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-chloro-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
-
pH 5.0, 37C
0.000333
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-cyano-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)picolinamide
-
pH 5.0, 37C
0.0003
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(2,5-dimethyl-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
0.00022
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
-
0.00063
N-benzyl-2-bromo-N-[(4-[[2-(2,4-dichlorophenyl)ethyl](4-phenylbutanoyl)amino]pyrrolidin-3-yl)methyl]-4,5-dimethoxybenzamide
-
pH 4.5, temperature not specified in the publication
0.0005
N-benzyl-2-bromo-N-[(4-[[2-(2,4-dichlorophenyl)ethyl][3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoyl]amino]pyrrolidin-3-yl)methyl]-4,5-dimethoxybenzamide
-
pH 4.5, temperature not specified in the publication
0.000046
N-[(1S)-1-([(1S,2S)-3-[(2-amino-2-oxoethyl)(benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl)-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000011
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
-
-
0.00000056
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
-
-
0.0000022
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
-
-
0.000121
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
-
-
0.000579
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
-
-
0.00065
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
-
-
0.000117
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
-
-
0.23
N-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.000214
N-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-cyclo-hexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.00001
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
-
-
0.00026
N-[(1S,2S)-3-cyclohexylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.000055
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
-
-
0.0001
N-[(1S,2S)-3-[[2-(1,3-benzodioxol-5-yl)ethyl][3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoyl]amino]-1-benzyl-2-hydroxypropyl]-4-(benzyloxy)-3,5-dimethoxybenzamide
-
-
0.0000043
N-[(2S,3S)-3-[[(3-chlorophenoxy)acetyl]amino]-2-hydroxy-4-phenylbutyl]-N-[2-(4-methoxyphenyl)ethyl]piperidine-4-carboxamide
-
-
0.0000002
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
-
-
0.000046
N-[(3S,4S)-3-hydroxy-6-phenyl-4-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]hexanoyl]-L-alanyl-L-leucinamide
-
-
0.000011
N-[1-Benzyl-3-(2-biphenyl-4-yl-1-carbamoyl-ethylamino)-2-hydroxy-propyl]-2-(3-1H-indol-3-yl-propionylamino)-3-methyl-butyramide
-
-
0.0001
N-[3-[(2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionyl]-amino]-1-benzyl-2-hydroxy-propyl]-4-benzyloxy-3,5-dimethoxy-benzamide
-
-
0.000056
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(3-butylheptyl)-4-pentylbenzamide
-
-
0.0033
N2-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-leucinamide
-
-
0.0032
Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.000000037
Pepstatin
-
pH 5.0, 37C
0.000000024
pepstatin A
-
-
0.000009
Piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
0.000004 - 0.0000043
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
0.00005
PS-273800
-
-
0.015
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
-
-
0.0000057
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
-
-
0.0000011
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
-
-
0.029
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-(3-methoxyphenyl)ethylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
0.0022
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
-
-
0.0000044
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
-
-
0.0000009
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
-
-
0.011
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-benzyloxymethyl-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.046
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-1-phenethylpropylcarbamoyl)-2-methylpropyl)amide
-
-
0.000045
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
-
-
0.074
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-phenylaminoethyl-carbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.248
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.03
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-phenylpropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.256
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(4-cyanobenzylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.041
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(cyclohexylmethylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.068
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-butylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.025
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.000016
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methylpropyl)-amide
-
-
0.000013
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-butylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
0.0000019
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
-
-
0.0000011
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
-
-
0.0005 - 0.0007
Ro40-4388
0.00025
Ro40-5576
0.000403
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
-
-
0.0004
[5-([[(4-bromophenyl)carbonyl]oxy]methyl)-2,3,4,7-tetrahydro-1H-azepin-3-yl]methyl 4-aminobenzoate
-
-
0.0024
[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl 7aH-indole-3-carboxylate
-
-
0.001
[6-([[(4-aminophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
-
0.0013
[6-([[(4-nitrophenyl)carbonyl]oxy]methyl)-2,5,6,7-tetrahydro-1H-azepin-4-yl]methyl naphthalene-1-carboxylate
-
-
additional information
additional information
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.01
(1RS) 3,3-difluoro-N-[2-(2-naphthyl)ethyl]-4-oxo-N-(4-pentylphenyl)cyclohexanecarboxamide
Plasmodium falciparum
-
pH 5.0, 37C
0.043
(1RS,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
Plasmodium falciparum
-
pH 5.0, 37C
0.0148
(1S,2S,3S,4R)-3-(4-bromophenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00039
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00013
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.00021
(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
Plasmodium falciparum
-
-
0.038
(1SR,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
Plasmodium falciparum
-
pH 5.0, 37C
0.0000043
(1Z)-N'-{[(4-chloro-3,5-dimethylphenoxy)acetyl]oxy}-2-(3,4-dimethoxyphenyl)ethanimidamide
Plasmodium falciparum
-
pH 4.5, 37C
0.02158
(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
Plasmodium falciparum
-
-
0.000006
(2R,3R,4S,6R)-6-[[(E)-2-(4-acetylphenyl)ethenyl]oxy]-2-[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]heptanediamide
Plasmodium falciparum
-
predicted inhibition constant, temperature not specified in the publication, pH not specified in the publication
0.0212
1-(4-chlorophenyl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.0305
1-(4-nitrophenyl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.0147
1-(biphenyl-4-yl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.02
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
0.000039
2,3-difluoro-4-methyl-N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]benzamide
Plasmodium falciparum
-
-
0.0000961
2-(1,3-benzothiazol-2-ylamino)-N-(2-chlorophenyl)-6-oxo-1,4,5,6tetrahydro-4-pyrimidinecarboxamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0001452
2-(1-naphthyl)-N'-[(4-nitrobenzoyl)oxy]ethanimidamide
Plasmodium falciparum
-
pH 4.5, 37C
0.019
2-(2-naphthyl)-N-(4-pentylphenyl)-N-piperidin-4-ylacetamide hydrochloride
Plasmodium falciparum
-
pH 5.0, 37C
0.000441
2-([4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-yl]oxy)ethanol
Plasmodium falciparum
-
IC50: 441 nM
0.000189
2-anilino-3-chloro-N-phenyl-4-(phenylimino)-2-butenamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0001871
2-anilino-4-(3-furyl)-6-oxo-N-phenyl-1-cyclohexene-1-carboxamide
Plasmodium falciparum
-
pH 4.5, 37C
0.00147
2-[4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-yl]ethanol
Plasmodium falciparum
-
IC50: 0.00147 mM
0.0004
3'-(((1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-ylamino)methyl)biphenyl-2-ol
Plasmodium falciparum
-
-
0.018
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
0.0002011
3-chloro-N-([2-(2-methoxybenzoyl)hydrazino]carbonothioyl)-1-benzothiophene-2-carboxamide
Plasmodium falciparum
-
pH 4.5, 37C
0.062
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
0.000713 - 0.000918
4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-carbonitrile
0.000208
4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-3-carboxylic acid
Plasmodium falciparum
-
IC50: 208 nM
0.000495
4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-carboxylic acid
Plasmodium falciparum
-
IC50: 495 nM
0.000077
4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)-N,N-dimethylbiphenyl-4-carboxamide
Plasmodium falciparum
-
IC50: 77 nM
0.0000064
4-amino-N'-(benzyloxy)-N-(2-methylphenyl)-1,2,5-oxadiazole-3carboximidamide
Plasmodium falciparum
-
pH 4.5, 37C
0.000305
4-amino-N'-(benzyloxy)-N-(4-methylphenyl)-1,2,5-oxadiazole-3carboximidamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0000055
4-amino-N'-[(2,4-dichlorobenzyl)oxy]-N-(2-methylphenyl)-1,2,5oxadiazole-3-carboximidamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0000426
4-amino-N'-[(2-methyl-1-naphthyl)methoxy]-1,2,5-oxadiazole-3carboximidamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0059
4-butoxy-N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)benzamide
Plasmodium falciparum
-
IC50: 0.0059 mM
0.0103
4-butoxy-N-[2-(dibutylamino)ethyl]-N-[4-(trifluoromethyl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 0.0103 mM
0.0023
4-butyl-N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)benzamide
Plasmodium falciparum
-
IC50: 0.0023 mM
0.0039
4-butyl-N-[2-(dibutylamino)ethyl]-N-[4-(trifluoromethyl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 0.0039 mM
0.056
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
0.0000573
6-((2-[(5-chloro-2-methoxyphenyl)amino]-2-oxoethyl)thio)-5-cyano-N-(2-methoxyphenyl)-2-methyl-4-phenyl-1,4-dihydro-3-pyridinecarboxamide
Plasmodium falciparum
-
pH 4.5, 37C
0.001831
6-bromo-2,3,4,9-tetrahydro-1H-carbazol-1-one Nphenylthiosemicarbazone
Plasmodium falciparum
-
pH 4.5, 37C
0.0000006
Ac-Val-Val-Sta-Ala-Sta
Plasmodium falciparum
-
IC50: 0.6 nM
0.00015
butyloxycarbonyl-His-Pro-Phe-His-Leu-PSI[CH(OH)-CH2]-Val-Ile-His
Plasmodium falciparum
-
IC50: 150 nM
0.001
butyloxycarbonyl-His-Pro-Phe-His-Sta-Leu-Phe-NH2
Plasmodium falciparum
-
IC50: 1000 nM
0.0000001
Iva-Val-Val-Sta-Ala-Sta
Plasmodium falciparum
-
IC50: 0.1 nM
100
Lac-Val-Sta-Ala-Sta
Plasmodium falciparum
-
IC50: 100 mM
0.014
LCu(CH3COO)2
Plasmodium falciparum
-
pH 4.7, 37C
0.017
LCuCl2
Plasmodium falciparum
-
pH 4.7, 37C
0.000124
methyl [4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
IC50: 124 nM
0.000183
methyl [4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
IC50: 183 nM
0.000034
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.000014
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylcyclohexyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.000011
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
Plasmodium falciparum
-
-
0.0000076
N',N'''-1,2-phenylenebis[N-(3-chlorophenyl)urea]
Plasmodium falciparum
-
pH 4.5, 37C
0.0002364
N'-[(4-methoxy-3-nitrobenzoyl)oxy]-2-(1-naphthyl)ethanimidamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0002374
N,N'-([(4,6-dimethyl-2-quinazolinyl)amino]methylylidene)dipropanamide
Plasmodium falciparum
-
pH 4.5, 37C
0.095
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.0013
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyridin-2-ylbenzyl)ethane-1,2-diamine
Plasmodium falciparum
-
IC50: 0.0013 mM
0.001603
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyridin-4-ylbenzyl)ethane-1,2-diamine
Plasmodium falciparum
-
IC50: 0.001603 mM
0.000000001631
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyrimidin-5-ylbenzyl)ethane-1,2-diamine
Plasmodium falciparum
-
IC50: 0.001631 nM
0.002
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-([4'-(2-pyrrolidin-1-ylethoxy)biphenyl-4-yl]methyl)ethane-1,2-diamine
Plasmodium falciparum
-
IC50: 0.002 mM
0.001022
N,N-dibutyl-N'-[(2'-fluorobiphenyl-4-yl)methyl]-N'-(4-pentylbenzyl)ethane-1,2-diamine
Plasmodium falciparum
-
IC50: 0.001022 mM
0.0000621
N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-methyl-4-oxo-1,4-dihydro-2-pyrimidinyl)amino]methylene)benzamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0001181
N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-oxo-4-propyl-1,6-dihydro-2-pyrimidinyl)amino]methylene)-4-methoxybenzamide
Plasmodium falciparum
-
pH 4.5, 37C
0.000046
N-((4'-[2-(benzylamino)-2-oxoethyl]biphenyl-4-yl)methyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 46 nM
0.000022
N-((S)-1-(((2S,3S)-3-hydroxy-5-oxo-5-(((S)-1-oxo-3-phenyl-1-(prop-2-yn-1-ylamino)propan-2-yl)amino)-1-phenylpentan-2-yl)-amino)-3-methyl-1-oxobutan-2-yl)picolinamide
Plasmodium falciparum
-
pH 5.0, 37C
0.000028
N-((S)-1-(((2S,3S)-5-(((R)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-chloro-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
Plasmodium falciparum
-
pH 5.0, 37C
0.000141
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-1-oxopent-4-yn-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)-picolinamide
Plasmodium falciparum
-
pH 5.0, 37C
0.000333
N-((S)-1-(((2S,3S)-5-(((S)-1-(((S)-1-amino-4-methyl-1-oxopentan-2-yl)amino)-3-cyano-1-oxopropan-2-yl)amino)-3-hydroxy-5-oxo-1-phenylpentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)picolinamide
Plasmodium falciparum
-
pH 5.0, 37C
0.0001464
N-(([2-(4-ethylphenyl)-6-methyl-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0001229
N-(([6-methyl-2-(4-methylphenyl)-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0000389
N-(2-([3-(1,3-benzodioxol-5-yl)-3-oxo-1-propen-1-yl]amino)phenyl)-4-nitrobenzenesulfonamide
Plasmodium falciparum
-
pH 4.5, 37C
0.000000003329
N-(2-aminoethyl)-N-(biphenyl-4-ylmethyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 0.003329 nM
0.0000875
N-(2-methoxyphenyl)-2-(5H-[1,2,4]triazino[5,6-b]indol-3ylthio)butanamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0000095
N-(3,4-dichlorophenyl)-2-[(4,6-dimethyl-2-pyrimidinyl)amino]3a,4,5,6,7,7a-hexahydro-1H-benzimidazole-1-carboxamide
Plasmodium falciparum
-
pH 4.5, 37C
0.001088
N-(3,4-dimethylphenyl)-N'-(imino[(4,6,7-trimethyl-2-quinazolinyl)amino]methyl)thiourea
Plasmodium falciparum
-
pH 4.5, 37C
0.013
N-(4-hexylphenyl)-2-(2-naphthyl)-N-piperidin-4-ylacetamide hydrochloride
Plasmodium falciparum
-
pH 5.0, 37C
0.001912
N-(4-[5-(1,3-benzodioxol-5-yl)pyridin-2-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 1912 nM
0.000437
N-(4-[6-(1,3-benzodioxol-5-yl)pyridin-3-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 437 nM
0.000289
N-(4-[benzyl(methyl)amino]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 289 nM
0.0047
N-(biphenyl-4-ylmethyl)-4-butoxy-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 0.0047 mM
0.0015
N-(biphenyl-4-ylmethyl)-4-butyl-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 0.0015 mM
0.002067
N-(biphenyl-4-ylmethyl)-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
Plasmodium falciparum
-
IC50: 0.002067 mM
0.003943
N-(biphenyl-4-ylmethyl)-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 0.003943 mM
0.001161
N-(biphenyl-4-ylmethyl)-N-[2-(butylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 0.001161 mM
0.000143 - 0.000252
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.0129
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-propylbenzamide
Plasmodium falciparum
-
IC50: 0.0129 mM
0.002317
N-(biphenyl-4-ylmethyl)-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 0.002317 mM
0.007
N-([(1RS)-3,3-difluoro-4-oxocyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
Plasmodium falciparum
-
pH 5.0, 37C
0.1
N-([(1RS)-3,3-difluoro-4-oxocyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
Plasmodium falciparum
-
value above, pH 5.0, 37C
0.019
N-([(1RS,4RS)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
Plasmodium falciparum
-
pH 5.0, 37C
0.016
N-([(1RS,4SR)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
Plasmodium falciparum
-
pH 5.0, 37C
0.1
N-([(1SR,4RS)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
0.0000088
N-([(2,4-dimethylphenyl)amino][(4-oxo-1,4,5,6,7,8-hexahydro-2-quinazolinyl)amino]methylene)benzamide
Plasmodium falciparum
-
pH 4.5, 37C
0.0017
N-([3',5'-bis(trifluoromethyl)biphenyl-4-yl]methyl)-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 0.0017 mM
0.00119
N-([3',5'-bis(trifluoromethyl)biphenyl-4-yl]methyl)-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 0.00119 mM
0.000019
N-([5-[3,5-bis(trifluoromethyl)phenyl]furan-2-yl]methyl)-N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentylpyridine-2-carboxamide
Plasmodium falciparum
-
-
0.00003
N-benzyl-2-([3-(3-nitrophenyl)acryloyl]amino)benzamide
Plasmodium falciparum
-
pH 4.5, 37C
0.000072
N-benzyl-4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-carboxamide
Plasmodium falciparum
-
IC50: 72 nM
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
0.005
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
0.017
N-hexyl-N-[2-hydroxy-2-(phenanthren-9-yl)ethyl]hexan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.024
N-[(1SR,3RS)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
Plasmodium falciparum
-
pH 5.0, 37C
0.02
N-[(1SR,3SR)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
Plasmodium falciparum
-
pH 5.0, 37C
0.000191
N-[(2'-chlorobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 191 nM
0.0000043
N-[(2S,3S)-2-hydroxy-3-[(phenoxyacetyl)amino]-4-phenylbutyl]-N-[2-(4-methoxyphenyl)ethyl]piperidine-4-carboxamide
Plasmodium falciparum
-
predicted inhibition constant, temperature not specified in the publication, pH not specified in the publication
0.00001
N-[(2S,3S)-5-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-[(4-bromobenzyl)oxy]-3-hydroxy-5-oxopentan-2-yl]-2,4,6-trifluorobenzamide
Plasmodium falciparum
-
predicted inhibition constant, temperature not specified in the publication, pH not specified in the publication
0.000591
N-[(4'-butylbiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 591 nM
0.000446
N-[(4'-chlorobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 446 nM
0.000407
N-[(4'-chlorobiphenyl-4-yl)methyl]-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 407 nM
0.00016
N-[(4'-cyanobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 160 nM
0.0000045
N-[(cyclopentylamino)carbonothioyl]-4-ethoxy-3-nitrobenzamide
Plasmodium falciparum
-
pH 4.5, 37C
0.000146
N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentyl-N-[4-[(pyridin-3-ylmethyl)carbamoyl]benzyl]benzamide
Plasmodium falciparum
-
-
0.000054
N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentyl-N-[[4'-(piperidin-1-ylcarbonyl)biphenyl-4-yl]methyl]pyridine-2-carboxamide
Plasmodium falciparum
-
-
0.000145
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)amino]benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000113
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[methyl(pyridin-4-yl)amino]benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000469
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(3-phenoxybenzyl)benzamide
Plasmodium falciparum
-
IC50: 469 nM
0.000369
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-piperidin-1-ylbenzyl)benzamide
Plasmodium falciparum
-
IC50: 369 nM
0.00038
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-2-ylbenzyl)benzamide
Plasmodium falciparum
-
IC50: 380 nM
0.000374
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-3-ylbenzyl)benzamide
Plasmodium falciparum
-
IC50: 374 nM
0.000212
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-4-ylbenzyl)benzamide
Plasmodium falciparum
-
IC50: 212 nM
0.000531
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyrimidin-5-ylbenzyl)benzamide
Plasmodium falciparum
-
IC50: 531 nM
0.000188
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-thiomorpholin-4-ylbenzyl)benzamide
Plasmodium falciparum
-
IC50: 188 nM
0.000056
N-[2-(dibutylamino)ethyl]-4-pentyl-N-([4'-(thiomorpholin-4-ylcarbonyl)biphenyl-4-yl]methyl)benzamide
Plasmodium falciparum
-
IC50: 56 nM
0.00024
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(1H-pyrrol-1-yl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 240 nM
0.0002
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(4-phenylpiperazin-1-yl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 200 nM
0.002345
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-phenylpyridin-2-yl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 2345 nM
0.00853
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-pyrimidin-5-ylpyridin-2-yl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 8530 nM
0.000589
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-phenylpyridin-3-yl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 589 nM
0.002229
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-pyrimidin-5-ylpyridin-3-yl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 2229 nM
0.000224
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(phenylamino)benzyl]benzamide
Plasmodium falciparum
-
IC50: 224 nM
0.001816
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(pyridin-4-ylamino)benzyl]benzamide
Plasmodium falciparum
-
IC50: 1816 nM
0.000596
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(trifluoromethyl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 596 nM
0.0396
N-[2-(dibutylamino)ethyl]-4-propyl-N-[4-(trifluoromethyl)benzyl]benzamide
Plasmodium falciparum
-
IC50: 0.0396 mM
0.0159
N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)-4-propylbenzamide
Plasmodium falciparum
-
IC50: 0.0159 mM
0.000295
N-[2-(dibutylamino)ethyl]-N-(4-pyridin-4-ylbenzyl)benzamide
Plasmodium falciparum
-
IC50: 295 nM
0.000204 - 0.000351
N-[2-(dibutylamino)ethyl]-N-(4-pyrimidin-5-ylbenzyl)benzamide
0.000574
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(phenyl)amino]benzyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 574 nM
0.003015
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(pyridin-4-yl)amino]benzyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 3015 nM
0.00039
N-[2-(dibutylamino)ethyl]-N-([3'-(trifluoromethyl)biphenyl-4-yl]methyl)benzamide
Plasmodium falciparum
-
IC50: 390 nM
0.000511
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 511 nM
0.000104
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)benzamide
Plasmodium falciparum
-
IC50: 104 nM
0.000151
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethyl)biphenyl-4-yl]methyl)benzamide
Plasmodium falciparum
-
IC50: 151 nM
0.000074 - 0.000091
N-[2-(dibutylamino)ethyl]-N-([4'-(2-morpholin-4-yl-2-oxoethyl)biphenyl-4-yl]methyl)-4-pentylbenzamide
0.000428
N-[2-(dibutylamino)ethyl]-N-[(3',4'-dimethoxybiphenyl-4-yl)methyl]benzamide
Plasmodium falciparum
-
IC50: 428 nM
0.000293
N-[2-(dibutylamino)ethyl]-N-[(3'-methylbiphenyl-4-yl)methyl]benzamide
Plasmodium falciparum
-
IC50: 293 nM
0.00067
N-[2-(dibutylamino)ethyl]-N-[4-(1H-indol-1-yl)benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 670 nM
0.002547
N-[2-(dibutylamino)ethyl]-N-[4-(4-methylpiperazin-1-yl)benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 2547 nM
0.001491
N-[2-(dibutylamino)ethyl]-N-[4-(diethylamino)benzyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 1491 nM
0.005
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
0.019
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
0.024
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
0.032
N-[3-(9H-fluoren-2-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.000221
N-[3-(dibutylamino)propyl]-4-pentyl-N-([4'-(2-pyrrolidin-1-ylethoxy)biphenyl-4-yl]methyl)benzamide
Plasmodium falciparum
-
IC50: 221 nM
0.000322 - 0.0011
N-[3-(dibutylamino)propyl]-N-[(2'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
0.000597
N-[3-(dibutylamino)propyl]-N-[(2'-methylbiphenyl-4-yl)methyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 597 nM
0.000468
N-[3-(dibutylamino)propyl]-N-[(3',4'-dimethoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 468 nM
0.00058
N-[3-(dibutylamino)propyl]-N-[(3'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 580 nM
0.000246
N-[3-(dibutylamino)propyl]-N-[(4'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 246 nM
0.002
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
0.024
N-[4,4-difluoro-3-oxocyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)-acetamide
Plasmodium falciparum
-
pH 5.0, 37C
0.000154
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]-2-methoxypyridine-4-carboxamide
Plasmodium falciparum
-
IC50: 154 nM
0.000202
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-3-carboxamide
Plasmodium falciparum
-
IC50: 202 nM
0.000464
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-4-carboxamide
Plasmodium falciparum
-
IC50: 464 nM
0.000243
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]pyrazine-2-carboxamide
Plasmodium falciparum
-
IC50: 243 nM
0.000334
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-piperidin-1-ylethyl)benzamide
Plasmodium falciparum
-
IC50: 334 nM
0.000165
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-[4-(3-phenylpropyl)piperidin-1-yl]ethyl)benzamide
Plasmodium falciparum
-
IC50: 165 nM
0.000831
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
Plasmodium falciparum
-
IC50: 831 nM
0.000439
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-([2-(diethylamino)ethyl](ethyl)amino)ethyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 439 nM
0.002897
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-morpholin-4-ylethyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 2897 nM
0.000334
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[benzyl(2-hydroxyethyl)amino]ethyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 334 nM
0.001501
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 1501 nM
0.00019
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(4-benzylpiperidin-1-yl)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 190 nM
0.000101
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 101 nM
0.000056
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 56 nM
0.001519
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 1519 nM
0.000531
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dipropylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 531 nM
0.000195
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50:195 nM
0.000587 - 0.000736
N-[4-(2,2'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000642
N-[4-(2,4'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 642 nM
0.005266
N-[4-(3,3'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 5266 nM
0.004553
N-[4-(3,4'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 4553 nM
0.000018
N-[4-(3,4-diethylisoxazol-5-yl)benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000646
N-[4-(4-benzylpiperazin-1-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 646 nM
0.000429
N-[4-(benzylamino)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 429 nM
0.0034
N-[4-(benzyloxy)benzyl]-4-butoxy-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 0.0034 mM
0.0013
N-[4-(benzyloxy)benzyl]-4-butyl-N-[2-(dibutylamino)ethyl]benzamide
Plasmodium falciparum
-
IC50: 0.0013 mM
0.000845
N-[4-(benzyloxy)benzyl]-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
Plasmodium falciparum
-
IC50: 845 nM
0.000112
N-[4-(benzyloxy)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
Plasmodium falciparum
-
IC50: 112 nM
0.0089
N-[4-(benzyloxy)benzyl]-N-[2-(dibutylamino)ethyl]-4-propylbenzamide
Plasmodium falciparum
-
IC50: 0.0089 mM
0.000031
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
Plasmodium falciparum
-
-
0.000032
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000067
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000047
N-[[5-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.000236
N-[[5-(4-chlorophenyl)isoxazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
Plasmodium falciparum
-
-
0.0000002
Pepstatin
Plasmodium falciparum
-
pH 5.0, temperature not specified in the publication
0.0000875
pepstatin A
Plasmodium falciparum
-
pH 4.5, 37C
0.0003467
SC-50083
Plasmodium falciparum
-
IC50: 0.0003467 mM
0.000197
[4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-yl]acetic acid
Plasmodium falciparum
-
IC50: 197 nM
0.000463
[4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetic acid
Plasmodium falciparum
-
IC50: 463 nM
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
2.2
-
assay at, PSM2 produces more cleavage sites at pH 4.5 than at pH 2.2. At pH 2.2 PSM2 activity is observed only without maturation
4.7
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
3 - 5
-
the zpepproPMII chimeric protein (porcine pepsinogen prosegment fused to the mature region of PMII) activates at pH 3-5. Activation at these pH values is consistent with the pH-dependent autoactivation observed for wildtype zymogen PMII
3.5 - 6
-
pH 3.5: about 65% of maximal activity, pH 6.0: about 30% of maximal activity, hydrolysis of Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
3.5 - 6.5
-
active over the range
4 - 5.5
-
pH 4.0: about 40% of maximal activity, pH 5.5: about 10% of maximal activity
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0
-
assay at, at pH 4.5 the number of cleavage sites is lower at 0C than at room temperature
additional information
-
assay at room temperature. At pH 4.5 the number of cleavage sites is lower at 0C than at room temperature
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
the proplasmepsin II gene is not transcribed until the later trophozoite stage of parasite growth
Manually annotated by BRENDA team
additional information
-
Plasmodium falciparum-infected cultured human erythrocytes
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
proplasmepsin II 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