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
3.4.23.39
-
RECOMMENDED NAME
GeneOntology No.
plasmepsin II
-
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
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
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
PATHWAY
KEGG Link
MetaCyc Link
hemoglobin degradation
-
SYNONYMS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
AH II
-
-
-
-
aspartic hemoglobinase II
-
-
-
-
malarial aspartic protease
-
-
PFAPD
-
-
-
-
plasmepsin 2
-
-
CAS REGISTRY NUMBER
COMMENTARY
159447-18-4
-
GENERAL INFORMATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
malfunction
-
multiple plasmepsin knockout mutants lacking plasmepsins I-III and I-IV, respectively show a significant increased parasite susceptibility to cyteine protease inhibitors. A ninefold increase in the potency of the calpain inhibitor N-acetyl-leucinyl-leucinyl-norleucinal (ALLN) against parasites lacking all four plasmepsins (I-IV) is observed. It is hypothesized that plasmepsins and some cysteine proteases play redundant or complementary roles in the digestive vacuole and that the absence of all plasmepsins (I-IV) renders these parasites highly susceptible to N-acetyl-leucinyl-leucinyl-norleucinal-mediated inhibition of falcipains
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
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
-
-
-
-
?
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid + H2O
?
show the reaction diagram
-
-
-
-
?
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
-
-
-
-
?
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
-
-
-
-
?
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
-
-
-
-
?
actin + H2O
?
show the reaction diagram
-
-
-
-
?
Ala-Leu-Glu-Arg-Thr-Phe-Leu-Ser-Phe-Pro-Thr + H2O
Ala-Leu-Glu-Arg-Thr-Phe + Leu-Ser-Phe-Pro-Thr
show the reaction diagram
-
-
-
-
?
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(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
-
-
-
-
?
Arg-Gln-Phe-Phe(p-NO2)-Ile-Thr + H2O
Arg-Gln-Phe + Phe(p-NO2)-Ile-Thr
show the reaction diagram
-
-
-
-
?
DABCYL-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-EDANS + H2O
?
show the reaction diagram
-
FRET substrate, substrate is designed to mimic the hemoglobin cleavage site. The substrate is conjugated with the fluorescent donor EDANS and the quencher DABCYL
-
-
?
DABCYL-L-Glu-L-Arg-L-Nle-L-Phe-L-Leu-L-Ser-L-Phe-L-Pro-EDANS + H2O
?
show the reaction diagram
-
FRET-based substrate
-
-
?
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH + H2O
?
show the reaction diagram
-
quenched fluorescent peptide substrate
-
-
?
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
-
-
-
-
?
EDANS-CO-CH2-CH2-COALERMFLSFP-diaminopimelate-(DABCYL)OH + H2O
?
show the reaction diagram
-
-
-
-
?
GST-SH3 peptide + H2O
?
show the reaction diagram
-
Y-/-V and L-/-L are major cleavage sites
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
-
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
-
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
enzyme is involved in initial steps of Plasmodium hemoglobin degradation
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
during the infection of erythrocytes by the human malaria parasite Plasmodium falciparum, up to 80% of the host cell hemoglobin is degraded to provide amino acids for parasite nutrition. Plasmepsin I and plasmepsin II are believed to be responsible for initiating the catabolic process
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
P46925
the enzyme initiates degradation of hemoglobin by cleavage at the alpha-chain between Phe33 and Leu34
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
the enzyme participates in the hemoglobin digestive pathway
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
the enzyme is involved in degradation of the host cell hemoglobin within the acidic food vacuole of the parasite
-
-
-
Hemoglobin + H2O
?
show the reaction diagram
-
pro-plasmepsin II is transported through the secretory system to cytostomal vacuoles and then is carried along with its substrate hemoglobin to the food vacuole where it is proteolytically processed to mature PMII
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
cleaves native hemoglobin and loosely folded alpha-chain
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
bovine and human hemoglobin are used
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
the enzyme participates in the hemoglobin digestive pathway
-
-
?
hemoglobin alpha-chain + H2O
?
show the reaction diagram
-
cleavage sites: Phe33-/-Leu34, Thr108-/-Leu109, Leu136-/-Thr137
-
-
?
hemoglobin beta-chain + H2O
?
show the reaction diagram
-
cleavage site: Leu32-/-Val33
-
-
?
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe + H2O
Leu-Glu-Arg-Ile-Phe + Phe(NO2)-Ser-Phe
show the reaction diagram
-
-
-
-
?
Leu-Ser-Phe(NO2)-Nle-Ala-Leu-OMe + H2O
?
show the reaction diagram
-
-
-
-
?
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Ala-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Asp-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys + H2O
Lys-Glu-Leu-Val-Phe + Phe(NO2)-Ala-Leu-Lys
show the reaction diagram
-
-
-
-
?
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
-
-
-
-
?
Lys-Glu-Phe-Val-Phe-4-nitrophenylalanine-Ala-Leu-Lys + H2O
?
show the reaction diagram
-
-
-
-
?
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
-
-
-
-
?
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
-
-
-
-
?
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Lys-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Phe-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ala-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Asp-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Ala-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Asp-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ala-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Ala-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Arg + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Arg
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Asp + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Asp
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ile + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Ile
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ser + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Ser
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Val + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Arg-Val
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Glu-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Glu-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Lys-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Lys-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ser-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Ser-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Val-Leu + H2O
Lys-Pro-Ile-Glu-Phe + Phe(NO2)-Val-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Leu-Phe-Nph-Arg-Leu + H2O
?
show the reaction diagram
-
chromogenic peptide substrate
-
-
?
Lys-Pro-Ile-Leu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Leu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Lys-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Nle-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Ser-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ile-Val-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ile-Val-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Lys-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Phe-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Pro-Ser-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
Myoglobin + H2O
?
show the reaction diagram
-
horse myoglobin is used
-
-
?
p47phox-PX + H2O
?
show the reaction diagram
-
PX domain of p47phox, a cytosolic factor of the neutrophil NADPH oxydase is digested
-
-
?
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
-
-
-
-
?
spectrin + H2O
?
show the reaction diagram
-
recombinant plasmepsin II hydrolyzes native spectrin at pH 6.8
-
-
?
spectrin + H2O
?
show the reaction diagram
-
the enzyme catalyzes the degradation of spectrin in the erythrocyte membrane cytoskeletron
-
-
?
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu + H2O
Lys-Ser-Ile-Glu-Phe + Phe(NO2)-Arg-Leu
show the reaction diagram
-
-
-
-
?
additional information
?
-
-
the enzyme has a preference for a small hydrophobic residue in the P3 position of the substrate. The S2 and S3 subsites of plasmepsin II are hydrophobic in nature and on this basis the hemoglobin-related substrate, with Arg and Thr in the P3 and P2 positions respectively may not represent the optimal substrate
-
-
-
additional information
?
-
-
multiple explicit-water molecular dynamics simulations of plasmepsin II, uncomplexed and with a hydroxypropylamine peptidomimetic inhibitor, indicate that protonation of Asp214 favours a stable active site structure
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Hemoglobin + H2O
?
show the reaction diagram
-
-
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
enzyme is involved in initial steps of Plasmodium hemoglobin degradation
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
during the infection of erythrocytes by the human malaria parasite Plasmodium falciparum, up to 80% of the host cell hemoglobin is degraded to provide amino acids for parasite nutrition. Plasmepsin I and plasmepsin II are believed to be responsible for initiating the catabolic process
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
P46925
the enzyme initiates degradation of hemoglobin by cleavage at the alpha-chain between Phe33 and Leu34
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
the enzyme participates in the hemoglobin digestive pathway
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
the enzyme is involved in degradation of the host cell hemoglobin within the acidic food vacuole of the parasite
-
-
-
Hemoglobin + H2O
?
show the reaction diagram
-
pro-plasmepsin II is transported through the secretory system to cytostomal vacuoles and then is carried along with its substrate hemoglobin to the food vacuole where it is proteolytically processed to mature PMII
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
the enzyme participates in the hemoglobin digestive pathway
-
-
?
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
-
-
-
-
?
spectrin + H2O
?
show the reaction diagram
-
the enzyme catalyzes the degradation of spectrin in the erythrocyte membrane cytoskeletron
-
-
?
INHIBITORS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
(1R,2R,3R,4R)-1,4-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-1,4-bis[5-(4-tert-butylphenyl)-1,3,4-oxadiazol-2-yl]butane-2,3-diol
-
-
(1RS) 3,3-difluoro-N-[2-(2-naphthyl)ethyl]-4-oxo-N-(4-pentylphenyl)cyclohexanecarboxamide
-
-
(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
-
-
(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
-
-
(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
-
-
(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
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-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
-
-
Iva-Val-Val-Sta-Ala-Sta
-
IC50: 0.1 nM
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
-
-
N',N'''-1,2-phenylenebis[N-(3-chlorophenyl)urea]
-
-
N'-[(4-methoxy-3-nitrobenzoyl)oxy]-2-(1-naphthyl)ethanimidamide
-
-
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
-
IC50: 143 nM
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 252 nM
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
-
most selective inhibitor
pepstatin A
-
inhibits autoactivation
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
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
additional information
-
none of the inhibitors analyzed to date have sufficient selectivity for plasmepsin I and II, compared to their human counterparts
-
additional information
-
single-digit nanomolar, low-molecular-weight inhibitors
-
additional information
-
plasmepsin is an important target for the development of antimalarial drugs, since its inhibition leads to the starvation of Plasmodium falciparum. A series of substrate-based dipeptide-type plasmepsin II inhibitors containing the hydroxymethylcarbonyl isostere as a transition-state mimic are synthesized
-
additional information
-
advances of computational approaches in inhibitor development
-
additional information
-
generation of an affinity matrix for purification of natural inhibitors by immobilization of the recombinant proenzyme to N-hydroxysuccinimide-activated Sepharose and the activation of the immobilized enzyme by incubation at pH 4.4 and 37C. The matrices are useful in the affinity purification of the inhibitory activity detected in marine invertebrates, such as Xestospongia muta, giant barrel sponge, and the gorgonian seafan coral Plexaura homomalla, with increases of 10.2- and 5.9fold in the specific inhibitory activity, respectively
-
KM VALUE [mM]
KM VALUE [mM] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.001
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
delF241 mutant enzyme expressed by a system that bypasses the need for autoactivation; mature enzyme expressed by a system that bypasses the need for autoactivation
0.00105
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
autoactivated enzyme
0.00127
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244A mutant enzyme expressed by a system that bypasses the need for autoactivation
0.00138
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244E mutant enzyme expressed by a system that bypasses the need for autoactivation
0.00233
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244K mutant enzyme expressed by a system that bypasses the need for autoactivation
0.00294
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
delF241 mutant enzyme expressed by a system that bypasses the need for autoactivation
0.00302
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244E mutant enzyme expressed by a system that bypasses the need for autoactivation
0.00305
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
autoactivated enzyme
0.00386
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
mature enzyme expressed by a system that bypasses the need for autoactivation
0.00433
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244A mutant enzyme expressed by a system that bypasses the need for autoactivation
0.00611
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244K mutant enzyme expressed by a system that bypasses the need for autoactivation
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
-
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
-
pH 4.4, 37C, mutant enzyme I287E
0.0146
-
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
-
pH 4.4, 37C, mutant enzyme M13E
0.0192
-
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
-
pH 4.4, 37C, mutant enzyme S77D
0.0334
-
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.06
-
Ala-Leu-Glu-Arg-Thr-Phe-Phe(NO2)-Ser-Phe-Pro-Thr
-
pH 4.7, 37C
0.11
-
Ala-Leu-Glu-Arg-Thr-Phe-Phe(NO2)-Ser-Phe-Pro-Thr
-
pH 4.7
0.00017
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
PMII without prosegment, pH 5, temperature not specified in the publication
0.0007
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
chimeric PMII (porcine pepsinogen prosegment fused to the mature region of PMII), pH 5, temperature not specified in the publication
0.0012
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
wild-type PMII, pH 5, temperature not specified in the publication
0.006
-
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37C, naturally occuring enzyme
0.01
-
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37C, recombinant enzyme
0.025
-
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4
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
-
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.058
-
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.069
-
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.055
-
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.073
-
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.109
-
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.006
-
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, recombinant enzyme
0.008
-
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, naturally occuring enzyme
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
-
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, naturally occuring enzyme or recombinant enzyme
0.02
-
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C
0.01
-
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
-
pH 4.4, 37C, recombinant enzyme
0.051
-
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.075
-
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.117
-
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.021
-
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.045
-
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.085
-
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.037
-
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.046
-
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.053
-
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.087
-
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.088
-
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.221
-
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.006
-
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.037
-
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.041
-
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.024
-
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.036
-
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.07
-
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.076
-
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
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
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.052
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme S77D
0.055
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.07
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E; pH 4.4, 37C, mutant enzyme M13E/I287E
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
-
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.04
-
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme S77D
0.05
-
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.022
-
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.017
-
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.031
-
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.039
-
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.006
-
Lys-Pro-Ile-Val-Phe-Phe(NO2)-Arg-Leu
-
pH 4.7, 37C
0.01
-
Lys-Pro-Ile-Val-Phe-Phe(NO2)-Arg-Leu
-
pH 4.7
0.035
-
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.037
-
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.25
-
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.024
-
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.064
-
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.07
-
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.056
-
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.071
-
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.092
-
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.049
-
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.1
-
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.11
-
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
additional information
-
additional information
-
-
-
TURNOVER NUMBER [1/s]
TURNOVER NUMBER MAXIMUM[1/s]
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.952
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244E mutant enzyme expressed by a system that bypasses the need for autoactivation
1.05
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
delF241 mutant enzyme expressed by a system that bypasses the need for autoactivation
1.51
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244K mutant enzyme expressed by a system that bypasses the need for autoactivation
2.33
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
mature enzyme expressed by a system that bypasses the need for autoactivation
2.51
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244A mutant enzyme expressed by a system that bypasses the need for autoactivation
2.52
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-CO-ALERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
autoactivated enzyme
0.431
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244E mutant enzyme expressed by a system that bypasses the need for autoactivation
0.596
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
delF241 mutant enzyme expressed by a system that bypasses the need for autoactivation
0.845
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244K mutant enzyme expressed by a system that bypasses the need for autoactivation
0.875
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
mature enzyme expressed by a system that bypasses the need for autoactivation
1.1
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
autoactivated enzyme
1.11
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
F244A mutant enzyme expressed by a system that bypasses the need for autoactivation
6.08
-
4-(4-dimethylaminophenylazo)benzoyl-CH2-CH2-CO-ERMFLSFP-diaminopimelate-5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid
-
delF241 mutant enzyme expressed by a system that bypasses the need for autoactivation; F244K mutant enzyme expressed by a system that bypasses the need for autoactivation
2.31
-
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
2.1
-
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
-
pH 4.4, 37C, mutant enzyme I287E
2.7
-
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
-
pH 4.4, 37C, mutant enzyme S77D
5.8
-
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
-
pH 4.4, 37C, mutant enzyme M13E
7.4
-
Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro
-
pH 4.4, 37C, mutant enzyme M13E/I287E
3.8
-
Ala-Leu-Glu-Arg-Thr-Phe-Phe(NO2)-Ser-Phe-Pro-Thr
-
pH 4.7
6
-
Ala-Leu-Glu-Arg-Thr-Phe-Phe(NO2)-Ser-Phe-Pro-Thr
-
pH 4.7, 37C
0.103
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
PMII without prosegment, pH 5, temperature not specified in the publication
1.11
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
chimeric PMII (porcine pepsinogen prosegment fused to the mature region of PMII), pH 5, temperature not specified in the publication
2.1
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
wild-type PMII, pH 5, temperature not specified in the publication
10
-
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37C, naturally occuring enzyme
13
-
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37C, recombinant enzyme
15
-
Leu-Glu-Arg-Ile-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4
9
-
Leu-Glu-Arg-Val-Phe-Phe(NO2)-Ser-Phe
-
pH 4.4, 37C
10.4
-
Leu-Ser-Phe(NO2)-Nle-Ala-Leu-Ome
-
pH 4.4, 37C
0.8
-
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.9
-
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
2
-
Lys-Ala-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.6
-
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.9
-
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
1.1
-
Lys-Asp-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
1.5
-
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, recombinant enzyme
6
-
Lys-Glu-Leu-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, naturally occuring enzyme
7
-
Lys-Glu-Phe-Asn-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, recombinant enzyme
15.2
-
Lys-Glu-Phe-Ile-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C
0.84
-
Lys-Glu-Phe-Val-Lys-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, mutant enzyme S77D
9.05
-
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C
17
-
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, recombinant enzyme
19
-
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Ala-Leu-Lys
-
pH 4.4, 37C, naturally occuring enzyme
11
-
Lys-Glu-Phe-Val-Phe-Phe(NO2)-Arg-Leu-Lys
-
pH 4.4, 37C, recombinant enzyme
0.17
-
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.19
-
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.4
-
Lys-Lys-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
1
-
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
1.1
-
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
2.6
-
Lys-Phe-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.5
-
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C; pH 4.4, 37C, mutant enzyme M13E/I287E
0.53
-
Lys-Pro-Ala-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.3
-
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.32
-
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.4
-
Lys-Pro-Asp-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.73
-
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.89
-
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
1.8
-
Lys-Pro-Ile-Ala-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.25
-
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.44
-
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.86
-
Lys-Pro-Ile-Asp-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
5.7
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ala-Leu
-
pH 4.4, 37C
0.53
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Arg
-
pH 4.4, 37C
1.2
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Asp
-
pH 4.4, 37C
0.9
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ile
-
pH 4.4, 37C
1.7
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
2
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C; pH 4.4, 37C, mutant enzyme M13E; pH 4.4, 37C, mutant enzyme S77D
3.5
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.44
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Ser
-
pH 4.4, 37C
0.7
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Arg-Val
-
pH 4.4, 37C
6.3
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Glu-Leu
-
pH 4.4, 37C
1.6
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Lys-Leu
-
pH 4.4, 37C
1.7
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Ser-Leu
-
pH 4.4, 37C
2.6
-
Lys-Pro-Ile-Glu-Phe-Phe(NO2)-Val-Leu
-
pH 4.4, 37C
1.7
-
Lys-Pro-Ile-Leu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.03
-
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.04
-
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.7, 37C
0.06
-
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.08
-
Lys-Pro-Ile-Lys-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme S77D
3.1
-
Lys-Pro-Ile-Nle-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
0.73
-
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
0.91
-
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
1.1
-
Lys-Pro-Ile-Ser-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
1.6
-
Lys-Pro-Ile-Val-Phe-Phe(NO2)-Arg-Leu
-
pH 4.7
3.6
-
Lys-Pro-Ile-Val-Phe-Phe(NO2)-Arg-Leu
-
pH 4.7, 37C
0.05
-
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.08
-
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.1
-
Lys-Pro-Lys-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
2.4
-
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
2.9
-
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
3.1
-
Lys-Pro-Phe-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.2
-
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
0.27
-
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E
0.32
-
Lys-Pro-Ser-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
1
-
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme I287E
1.1
-
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C, mutant enzyme M13E/I287E
1.3
-
Lys-Ser-Ile-Glu-Phe-Phe(NO2)-Arg-Leu
-
pH 4.4, 37C
additional information
-
additional information
-
-
-
kcat/KM VALUE [1/mMs-1]
kcat/KM VALUE [1/mMs-1] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
620
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
PMII without prosegment, pH 5, temperature not specified in the publication
254276
1500
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
wild-type PMII, pH 5, temperature not specified in the publication
254276
1660
-
EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH
-
chimeric PMII (porcine pepsinogen prosegment fused to the mature region of PMII), pH 5, temperature not specified in the publication
254276
Ki VALUE [mM]
Ki VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
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
0.00043
-
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
-
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
-
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
-
Ro40-4388
-
pH 4.4, 37C
0.0007
-
Ro40-4388
-
-
0.0007
-
Ro40-4388
-
pH 4.4, 37C
0.00025
-
Ro40-5576
-
-
-
0.00025
-
Ro40-5576
-
pH 4.4, 37C
-
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
-
-
0.000034
-
methyl 4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-carboxylate
-
-
additional information
-
additional information
-
Ki-values for (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonylyxy)benzyl)-heptanoyl amide is above 2000 nM
-
additional information
-
additional information
-
Ki value for Iva-Val-Val-Sta-Ala-Sta is below 0.1 nM
-
additional information
-
additional information
-
the Ki-value for Ro17-7109 is above 0.015 mM
-
IC50 VALUE [mM]
IC50 VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.01
-
(1RS) 3,3-difluoro-N-[2-(2-naphthyl)ethyl]-4-oxo-N-(4-pentylphenyl)cyclohexanecarboxamide
-
pH 5.0, 37C
0.043
-
(1RS,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
-
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
-
-
0.00039
-
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-((2'-methoxybiphenyl-3-yl)methyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
0.00013
-
(1S,2S,3S,4R)-3-(4-hexylphenylsulfonyl)-N-(naphthalen-2-ylmethyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
0.00021
-
(1S,2S,3S,4R)-N-(3-bromobenzyl)-3-(4-hexylphenylsulfonyl)-7-azabicyclo[2.2.1]heptan-2-amine
-
-
0.038
-
(1SR,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
-
pH 5.0, 37C
0.0000043
-
(1Z)-N'-{[(4-chloro-3,5-dimethylphenoxy)acetyl]oxy}-2-(3,4-dimethoxyphenyl)ethanimidamide
-
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
-
-
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
-
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
-
pH 5.0, temperature not specified in the publication
0.0305
-
1-(4-nitrophenyl)-2-[2-(pyridin-2-yl)-1H-benzimidazol-1-yl]ethanone
-
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
-
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
-
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
-
-
0.0000961
-
2-(1,3-benzothiazol-2-ylamino)-N-(2-chlorophenyl)-6-oxo-1,4,5,6tetrahydro-4-pyrimidinecarboxamide
-
pH 4.5, 37C
0.0001452
-
2-(1-naphthyl)-N'-[(4-nitrobenzoyl)oxy]ethanimidamide
-
pH 4.5, 37C
0.019
-
2-(2-naphthyl)-N-(4-pentylphenyl)-N-piperidin-4-ylacetamide hydrochloride
-
pH 5.0, 37C
0.000441
-
2-([4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-yl]oxy)ethanol
-
IC50: 441 nM
0.000189
-
2-anilino-3-chloro-N-phenyl-4-(phenylimino)-2-butenamide
-
pH 4.5, 37C
0.0001871
-
2-anilino-4-(3-furyl)-6-oxo-N-phenyl-1-cyclohexene-1-carboxamide
-
pH 4.5, 37C
0.00147
-
2-[4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-yl]ethanol
-
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
-
-
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
-
pH 5.0, temperature not specified in the publication
0.0002011
-
3-chloro-N-([2-(2-methoxybenzoyl)hydrazino]carbonothioyl)-1-benzothiophene-2-carboxamide
-
pH 4.5, 37C
0.062
-
3-[3-(4-chlorophenyl)-3-hydroxy-3-phenylpropyl]-3-azoniabicyclo[4.2.1]nonane
-
pH 5.0, temperature not specified in the publication
0.000713
-
4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-carbonitrile
-
IC50: 713 nM
0.000918
-
4'-(([2-(dibutylamino)ethyl](4-pentylbenzyl)amino)methyl)biphenyl-4-carbonitrile
-
IC50: 918 nM
0.000208
-
4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-3-carboxylic acid
-
IC50: 208 nM
0.000495
-
4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-carboxylic acid
-
IC50: 495 nM
0.000077
-
4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)-N,N-dimethylbiphenyl-4-carboxamide
-
IC50: 77 nM
0.0000064
-
4-amino-N'-(benzyloxy)-N-(2-methylphenyl)-1,2,5-oxadiazole-3carboximidamide
-
pH 4.5, 37C
0.000305
-
4-amino-N'-(benzyloxy)-N-(4-methylphenyl)-1,2,5-oxadiazole-3carboximidamide
-
pH 4.5, 37C
0.0000055
-
4-amino-N'-[(2,4-dichlorobenzyl)oxy]-N-(2-methylphenyl)-1,2,5oxadiazole-3-carboximidamide
-
pH 4.5, 37C
0.0000426
-
4-amino-N'-[(2-methyl-1-naphthyl)methoxy]-1,2,5-oxadiazole-3carboximidamide
-
pH 4.5, 37C
0.0059
-
4-butoxy-N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)benzamide
-
IC50: 0.0059 mM
0.0103
-
4-butoxy-N-[2-(dibutylamino)ethyl]-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 0.0103 mM
0.0023
-
4-butyl-N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)benzamide
-
IC50: 0.0023 mM
0.0039
-
4-butyl-N-[2-(dibutylamino)ethyl]-N-[4-(trifluoromethyl)benzyl]benzamide
-
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
-
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
-
pH 4.5, 37C
0.001831
-
6-bromo-2,3,4,9-tetrahydro-1H-carbazol-1-one Nphenylthiosemicarbazone
-
pH 4.5, 37C
0.0000006
-
Ac-Val-Val-Sta-Ala-Sta
-
IC50: 0.6 nM
0.00015
-
butyloxycarbonyl-His-Pro-Phe-His-Leu-PSI[CH(OH)-CH2]-Val-Ile-His
-
IC50: 150 nM
0.001
-
butyloxycarbonyl-His-Pro-Phe-His-Sta-Leu-Phe-NH2
-
IC50: 1000 nM
0.0000001
-
Iva-Val-Val-Sta-Ala-Sta
-
IC50: 0.1 nM
100
-
Lac-Val-Sta-Ala-Sta
-
IC50: 100 mM
0.014
-
LCu(CH3COO)2
-
pH 4.7, 37C
0.017
-
LCuCl2
-
pH 4.7, 37C
0.000124
-
methyl [4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-yl]acetate
-
IC50: 124 nM
0.000183
-
methyl [4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetate
-
IC50: 183 nM
0.000034
-
methyl [4'-([[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
0.000014
-
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylcyclohexyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
0.000011
-
methyl [4'-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)biphenyl-4-yl]acetate
-
-
0.0000076
-
N',N'''-1,2-phenylenebis[N-(3-chlorophenyl)urea]
-
pH 4.5, 37C
0.0002364
-
N'-[(4-methoxy-3-nitrobenzoyl)oxy]-2-(1-naphthyl)ethanimidamide
-
pH 4.5, 37C
0.0002374
-
N,N'-([(4,6-dimethyl-2-quinazolinyl)amino]methylylidene)dipropanamide
-
pH 4.5, 37C
0.095
-
N,N-dibutyl-3-(1,4-dihydronaphthalen-1-yl)-3-hydroxybutan-1-aminium
-
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
-
IC50: 0.0013 mM
0.001603
-
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyridin-4-ylbenzyl)ethane-1,2-diamine
-
IC50: 0.001603 mM
0.000000001631
-
N,N-dibutyl-N'-(4-pentylbenzyl)-N'-(4-pyrimidin-5-ylbenzyl)ethane-1,2-diamine
-
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
-
IC50: 0.002 mM
0.001022
-
N,N-dibutyl-N'-[(2'-fluorobiphenyl-4-yl)methyl]-N'-(4-pentylbenzyl)ethane-1,2-diamine
-
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
-
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
-
pH 4.5, 37C
0.000046
-
N-((4'-[2-(benzylamino)-2-oxoethyl]biphenyl-4-yl)methyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
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
-
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
-
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
-
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
0.0001464
-
N-(([2-(4-ethylphenyl)-6-methyl-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
-
pH 4.5, 37C
0.0001229
-
N-(([6-methyl-2-(4-methylphenyl)-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
-
pH 4.5, 37C
0.0000389
-
N-(2-([3-(1,3-benzodioxol-5-yl)-3-oxo-1-propen-1-yl]amino)phenyl)-4-nitrobenzenesulfonamide
-
pH 4.5, 37C
0.000000003329
-
N-(2-aminoethyl)-N-(biphenyl-4-ylmethyl)-4-pentylbenzamide
-
IC50: 0.003329 nM
0.0000875
-
N-(2-methoxyphenyl)-2-(5H-[1,2,4]triazino[5,6-b]indol-3ylthio)butanamide
-
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
-
pH 4.5, 37C
0.001088
-
N-(3,4-dimethylphenyl)-N'-(imino[(4,6,7-trimethyl-2-quinazolinyl)amino]methyl)thiourea
-
pH 4.5, 37C
0.013
-
N-(4-hexylphenyl)-2-(2-naphthyl)-N-piperidin-4-ylacetamide hydrochloride
-
pH 5.0, 37C
0.001912
-
N-(4-[5-(1,3-benzodioxol-5-yl)pyridin-2-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 1912 nM
0.000437
-
N-(4-[6-(1,3-benzodioxol-5-yl)pyridin-3-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 437 nM
0.000289
-
N-(4-[benzyl(methyl)amino]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 289 nM
0.0047
-
N-(biphenyl-4-ylmethyl)-4-butoxy-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0047 mM
0.0015
-
N-(biphenyl-4-ylmethyl)-4-butyl-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0015 mM
0.002067
-
N-(biphenyl-4-ylmethyl)-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 0.002067 mM
0.003943
-
N-(biphenyl-4-ylmethyl)-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 0.003943 mM
0.001161
-
N-(biphenyl-4-ylmethyl)-N-[2-(butylamino)ethyl]-4-pentylbenzamide
-
IC50: 0.001161 mM
0.000143
-
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 143 nM
0.000252
-
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 252 nM
0.0129
-
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-propylbenzamide
-
IC50: 0.0129 mM
0.002317
-
N-(biphenyl-4-ylmethyl)-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
-
IC50: 0.002317 mM
0.007
-
N-([(1RS)-3,3-difluoro-4-oxocyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
pH 5.0, 37C
0.1
-
N-([(1RS)-3,3-difluoro-4-oxocyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
value above, pH 5.0, 37C
0.019
-
N-([(1RS,4RS)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
pH 5.0, 37C
0.016
-
N-([(1RS,4SR)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
pH 5.0, 37C
0.1
-
N-([(1SR,4RS)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
value above, pH 5.0, 37C
0.1
-
N-([(1SR,4SR)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
value above, pH 5.0, 37C
0.0000088
-
N-([(2,4-dimethylphenyl)amino][(4-oxo-1,4,5,6,7,8-hexahydro-2-quinazolinyl)amino]methylene)benzamide
-
pH 4.5, 37C
0.0017
-
N-([3',5'-bis(trifluoromethyl)biphenyl-4-yl]methyl)-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0017 mM
0.00119
-
N-([3',5'-bis(trifluoromethyl)biphenyl-4-yl]methyl)-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
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
-
-
0.00003
-
N-benzyl-2-([3-(3-nitrophenyl)acryloyl]amino)benzamide
-
pH 4.5, 37C
0.000072
-
N-benzyl-4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-carboxamide
-
IC50: 72 nM
0.002
-
N-butyl-N-[2-[6-chloro-3-(3,4-dichlorophenyl)naphthalen-1-yl]-2-hydroxyethyl]butan-1-aminium
-
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
-
pH 5.0, temperature not specified in the publication
0.017
-
N-hexyl-N-[2-hydroxy-2-(phenanthren-9-yl)ethyl]hexan-1-aminium
-
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
-
pH 5.0, 37C
0.02
-
N-[(1SR,3SR)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
pH 5.0, 37C
0.000191
-
N-[(2'-chlorobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 191 nM
0.0000043
-
N-[(2S,3S)-2-hydroxy-3-[(phenoxyacetyl)amino]-4-phenylbutyl]-N-[2-(4-methoxyphenyl)ethyl]piperidine-4-carboxamide
-
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
-
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
-
IC50: 591 nM
0.000446
-
N-[(4'-chlorobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 446 nM
0.000407
-
N-[(4'-chlorobiphenyl-4-yl)methyl]-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
IC50: 407 nM
0.00016
-
N-[(4'-cyanobiphenyl-4-yl)methyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 160 nM
0.0000045
-
N-[(cyclopentylamino)carbonothioyl]-4-ethoxy-3-nitrobenzamide
-
pH 4.5, 37C
0.000146
-
N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentyl-N-[4-[(pyridin-3-ylmethyl)carbamoyl]benzyl]benzamide
-
-
0.000054
-
N-[1-(3-methylbutyl)piperidin-4-yl]-5-pentyl-N-[[4'-(piperidin-1-ylcarbonyl)biphenyl-4-yl]methyl]pyridine-2-carboxamide
-
-
0.000145
-
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)amino]benzyl]-4-pentylbenzamide
-
-
0.000113
-
N-[1-(3-methylbutyl)piperidin-4-yl]-N-[4-[methyl(pyridin-4-yl)amino]benzyl]-4-pentylbenzamide
-
-
0.000469
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(3-phenoxybenzyl)benzamide
-
IC50: 469 nM
0.000369
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-piperidin-1-ylbenzyl)benzamide
-
IC50: 369 nM
0.00038
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-2-ylbenzyl)benzamide
-
IC50: 380 nM
0.000374
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-3-ylbenzyl)benzamide
-
IC50: 374 nM
0.000212
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-4-ylbenzyl)benzamide
-
IC50: 212 nM
0.000531
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyrimidin-5-ylbenzyl)benzamide
-
IC50: 531 nM
0.000188
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-thiomorpholin-4-ylbenzyl)benzamide
-
IC50: 188 nM
0.000056
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-([4'-(thiomorpholin-4-ylcarbonyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 56 nM
0.00024
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(1H-pyrrol-1-yl)benzyl]benzamide
-
IC50: 240 nM
0.0002
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(4-phenylpiperazin-1-yl)benzyl]benzamide
-
IC50: 200 nM
0.002345
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-phenylpyridin-2-yl)benzyl]benzamide
-
IC50: 2345 nM
0.00853
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-pyrimidin-5-ylpyridin-2-yl)benzyl]benzamide
-
IC50: 8530 nM
0.000589
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-phenylpyridin-3-yl)benzyl]benzamide
-
IC50: 589 nM
0.002229
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-pyrimidin-5-ylpyridin-3-yl)benzyl]benzamide
-
IC50: 2229 nM
0.000224
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(phenylamino)benzyl]benzamide
-
IC50: 224 nM
0.001816
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(pyridin-4-ylamino)benzyl]benzamide
-
IC50: 1816 nM
0.000596
-
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 596 nM
0.0396
-
N-[2-(dibutylamino)ethyl]-4-propyl-N-[4-(trifluoromethyl)benzyl]benzamide
-
IC50: 0.0396 mM
0.0159
-
N-[2-(dibutylamino)ethyl]-N-(3-phenoxybenzyl)-4-propylbenzamide
-
IC50: 0.0159 mM
0.000295
-
N-[2-(dibutylamino)ethyl]-N-(4-pyridin-4-ylbenzyl)benzamide
-
IC50: 295 nM
0.000204
-
N-[2-(dibutylamino)ethyl]-N-(4-pyrimidin-5-ylbenzyl)benzamide
-
IC50: 204 nM
0.000351
-
N-[2-(dibutylamino)ethyl]-N-(4-pyrimidin-5-ylbenzyl)benzamide
-
IC50: 351 nM
0.000574
-
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(phenyl)amino]benzyl)-4-pentylbenzamide
-
IC50: 574 nM
0.003015
-
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(pyridin-4-yl)amino]benzyl)-4-pentylbenzamide
-
IC50: 3015 nM
0.00039
-
N-[2-(dibutylamino)ethyl]-N-([3'-(trifluoromethyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 390 nM
0.000511
-
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)-4-pentylbenzamide
-
IC50: 511 nM
0.000104
-
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)benzamide
-
IC50: 104 nM
0.000151
-
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethyl)biphenyl-4-yl]methyl)benzamide
-
IC50: 151 nM
0.000074
-
N-[2-(dibutylamino)ethyl]-N-([4'-(2-morpholin-4-yl-2-oxoethyl)biphenyl-4-yl]methyl)-4-pentylbenzamide
-
IC50: 74 nM
0.000091
-
N-[2-(dibutylamino)ethyl]-N-([4'-(2-morpholin-4-yl-2-oxoethyl)biphenyl-4-yl]methyl)-4-pentylbenzamide
-
IC50: 91 nM
0.000428
-
N-[2-(dibutylamino)ethyl]-N-[(3',4'-dimethoxybiphenyl-4-yl)methyl]benzamide
-
IC50: 428 nM
0.000293
-
N-[2-(dibutylamino)ethyl]-N-[(3'-methylbiphenyl-4-yl)methyl]benzamide
-
IC50: 293 nM
0.00067
-
N-[2-(dibutylamino)ethyl]-N-[4-(1H-indol-1-yl)benzyl]-4-pentylbenzamide
-
IC50: 670 nM
0.002547
-
N-[2-(dibutylamino)ethyl]-N-[4-(4-methylpiperazin-1-yl)benzyl]-4-pentylbenzamide
-
IC50: 2547 nM
0.001491
-
N-[2-(dibutylamino)ethyl]-N-[4-(diethylamino)benzyl]-4-pentylbenzamide
-
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
-
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
-
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
-
pH 5.0, temperature not specified in the publication
0.032
-
N-[3-(9H-fluoren-2-yl)-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
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
-
IC50: 221 nM
0.000322
-
N-[3-(dibutylamino)propyl]-N-[(2'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 322 nM
0.0011
-
N-[3-(dibutylamino)propyl]-N-[(2'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 0.0011 mM
0.000597
-
N-[3-(dibutylamino)propyl]-N-[(2'-methylbiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 597 nM
0.000468
-
N-[3-(dibutylamino)propyl]-N-[(3',4'-dimethoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 468 nM
0.00058
-
N-[3-(dibutylamino)propyl]-N-[(3'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 580 nM
0.000246
-
N-[3-(dibutylamino)propyl]-N-[(4'-methoxybiphenyl-4-yl)methyl]-4-pentylbenzamide
-
IC50: 246 nM
0.002
-
N-[3-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]-3-hydroxypropyl]-N-pentylpentan-1-aminium
-
pH 5.0, temperature not specified in the publication
0.024
-
N-[4,4-difluoro-3-oxocyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)-acetamide
-
pH 5.0, 37C
0.000154
-
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]-2-methoxypyridine-4-carboxamide
-
IC50: 154 nM
0.000202
-
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-3-carboxamide
-
IC50: 202 nM
0.000464
-
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-4-carboxamide
-
IC50: 464 nM
0.000243
-
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]pyrazine-2-carboxamide
-
IC50: 243 nM
0.000334
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-piperidin-1-ylethyl)benzamide
-
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
-
IC50: 165 nM
0.000831
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 831 nM
0.000439
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-([2-(diethylamino)ethyl](ethyl)amino)ethyl)-4-pentylbenzamide
-
IC50: 439 nM
0.002897
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-morpholin-4-ylethyl)-4-pentylbenzamide
-
IC50: 2897 nM
0.000334
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[benzyl(2-hydroxyethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 334 nM
0.001501
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
-
IC50: 1501 nM
0.00019
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(4-benzylpiperidin-1-yl)ethyl]-4-pentylbenzamide
-
IC50: 190 nM
0.000101
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 101 nM
0.000056
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 56 nM
0.001519
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
-
IC50: 1519 nM
0.000531
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dipropylamino)ethyl]-4-pentylbenzamide
-
IC50: 531 nM
0.000195
-
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[3-(dibutylamino)propyl]-4-pentylbenzamide
-
IC50:195 nM
0.000587
-
N-[4-(2,2'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 587 nM
0.000736
-
N-[4-(2,2'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 736 nM
0.000642
-
N-[4-(2,4'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 642 nM
0.005266
-
N-[4-(3,3'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 5266 nM
0.004553
-
N-[4-(3,4'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 4553 nM
0.000018
-
N-[4-(3,4-diethylisoxazol-5-yl)benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
0.000646
-
N-[4-(4-benzylpiperazin-1-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 646 nM
0.000429
-
N-[4-(benzylamino)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 429 nM
0.0034
-
N-[4-(benzyloxy)benzyl]-4-butoxy-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0034 mM
0.0013
-
N-[4-(benzyloxy)benzyl]-4-butyl-N-[2-(dibutylamino)ethyl]benzamide
-
IC50: 0.0013 mM
0.000845
-
N-[4-(benzyloxy)benzyl]-N',N'-dibutyl-N-(4-pentylbenzyl)ethane-1,2-diamine
-
IC50: 845 nM
0.000112
-
N-[4-(benzyloxy)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
-
IC50: 112 nM
0.0089
-
N-[4-(benzyloxy)benzyl]-N-[2-(dibutylamino)ethyl]-4-propylbenzamide
-
IC50: 0.0089 mM
0.000031
-
N-[4-([[1-(3-methylbutyl)piperidin-4-yl][(4-pentylphenyl)carbonyl]amino]methyl)phenyl]-1-benzothiophene-2-carboxamide
-
-
0.000032
-
N-[4-[5-(3,4-dimethoxybenzyl)-1,2,4-oxadiazol-3-yl]benzyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
0.000067
-
N-[[5-(2,5-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
0.000047
-
N-[[5-(3,4-dichlorophenyl)furan-2-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
0.000236
-
N-[[5-(4-chlorophenyl)isoxazol-3-yl]methyl]-N-[1-(3-methylbutyl)piperidin-4-yl]-4-pentylbenzamide
-
-
0.0000002
-
Pepstatin
-
pH 5.0, temperature not specified in the publication
0.0000875
-
pepstatin A
-
pH 4.5, 37C
0.0003467
-
SC-50083
-
IC50: 0.0003467 mM
0.000197
-
[4'-(([2-(dibutylamino)ethyl](phenylcarbonyl)amino)methyl)biphenyl-4-yl]acetic acid
-
IC50: 197 nM
0.000463
-
[4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetic acid
-
IC50: 463 nM
pH OPTIMUM
pH MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
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
4.5
-
-
assay at, at pH 4.5 the number of cleavage sites is lower at 0C than at room temperature. PSM2 produces more cleavage sites at pH 4.5 than at pH 2.2
4.7
-
-
assay at
5
-
-
optimal pH of wild-type PMII, chimeric PMII and PMII without prosegment
pH RANGE
pH RANGE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
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
TEMPERATURE OPTIMUM MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
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 ACCESSION NO.
COMMENTARY
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 ACCESSION NO.
COMMENTARY
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
-
pro-plasmepsin II is transported through the secretory system to cytostomal vacuoles and then is carried along with its substrate hemoglobin to the food vacuole where it is proteolytically processed to mature PMII
Manually annotated by BRENDA team
-
the plasmepsins, although not essential, contribute significantly to the fitness of the parasite and are required for efficient degradation of endosomal vesicles delivered to the digestive vacuole
Manually annotated by BRENDA team
-
digestive vacuole
-
Manually annotated by BRENDA team
MOLECULAR WEIGHT
MOLECULAR WEIGHT MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
38000
-
-
activated form
43000
-
-
precursor form
SUBUNITS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
?
-
x * 36924, calculation from nucleotide sequence
?
-
x * 36924, calculation from nucleotide sequence
-
monomer
-
PM II exists mainly as a monomer in solution and that the monomer is fully functional for catalysis
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
proteolytic modification
-
the proenzyme has an unusually long propart of 125 amino acid residues that mediates type II membrane anchoring of the proenzyme, activation occurs by removal of the propart, proplasmepsin II can autoactivate at acidic pH
proteolytic modification
-
proplasmepsin maturation appears to require acidic conditions, proplasmepsin maturation may not be autocatalytic in vivo
proteolytic modification
-
recombinant proplasmepsin II autoactivates at acidic pH, but the location of the cleavage site varies dependening on the conditions used
proteolytic modification
-
plasmepsin II is produced as a precursor. The propart region, about 120 residues, is more than twice as long as those of archetypal zymogens
proteolytic modification
-
the processing of PM II and IV occurs via an intra- and inter-molecular autocatalytic event as well as via a transcatalytic event between them
proteolytic modification
-
pro-plasmepsin II is transported through the secretory system to cytostomal vacuoles and then is carried along with its substrate hemoglobin to the food vacuole where it is proteolytically processed to mature PMII
proteolytic modification
-
the large N-terminal displacement and the interdomain shift from the proenzyme structure to active plasmepsin are promoted by essential dynamics sampling. An intermediate, stabilized by electrostatic interactions between the catalytic dyad and the N-terminus of mature plasmepsin, is observed along all activation trajectories. The stabilizing interactions in the activation intermediate of plasmepsin are similar to those in the X-ray structure of pepsinogen. The catalytic aspartates act as hydrogen bond acceptors for the N-terminal amino group and the Ser2 hydroxyl in plasmepsin, and the side chains of Lys36pro and Tyr9 in pepsinogen
proteolytic modification
-
PSM2 is less active after maturation. At pH 2.2 PSM2 activity is observed only without maturation
proteolytic modification
-
protein is expressed as an inactive zymogen with a large prosegment
proteolytic modification
-
the PMII zymogen utilizes a prosegment-catalyzed folding mechanism
Crystallization/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
crystal structure of Met205Ser mutant enzyme in complex with the two inhibitors rs367 and rs370, crystals are grown at 293 K by vapor diffusion in hanging drops
-
crystal structure of uncomplexed plasmepsin II as well as the complex with the potent inhibitor EH58, crystals are grown at 20C by vapor diffusion in hanging drops
-
crystal structures of Plm II, uncomplexed and in complex with different inhibitors, reveal considerable conformational flexibility
-
crystallization of proplasmepsin II by sitting drops
-
generation of 3D-QSAR pharmacophore models for binding of PlmII inhibitors. A series of 26 inhibitors were modeled in the binding clefts of the PlmII and human cathepsin D to establish QSAR models of the proteases inhibition. The contributions of the P2 and P3' residues to the inhibitors binding affinity are responsible for the target selectivity
-
hanging drop method, X-ray structure of plasmepsin II complexed with the potent non-peptidomimetic achiral inhibitor at 1.6 A
-
ligand docking studies with plasmepsin II predict binding of benzimidazole compounds at the center of the extended substrate-binding cleft. According to the plausible mode of binding,the pyridine ring of benzimidazole compounds interact with S1' subsite residues whereas the acetophenone moiety is in contact with S1-S3 subsites of plasmepsin II active center
-
molecular dynamics simulation using inhibitor (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
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plasmepsin II in complex with inhibitor 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
-
plasmepsin II in complex with isovaleryl pepstatin
-
plasmepsin II in complex with pepstatin A
-
sequence and structural analysis combined with molecular dynamics simulations to predict the functional residues. Residues Y17, V105, T108, L191, L242, Q275, and T298 are important for plasmepsin function. Residues V105 and T108 are localized in a flap of an interior pocket. There is a rapid conformational change in the L3 region of plasmepsins that closes the active site
-
the aspartic acid residues in structure PDB 1lfA is noncoplanar. The catalytic water molecule is present, but the plane of the carboxylate group of Asp214 is rotated by 66 from its original position
-
Purification/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
proplasmepsin
-
protein is autoactivated at pH 4.7
-
using a Q-Sepharose fast flow column
-
using nickel affinity chromatography and gel filtration
-
Cloned/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
DNA encoding the last 48 residues of the pro-part and the whole mature sequence of Plasmodium falciparum plasmepsin II is cloned into the T7-dependent vector pET3a for expression in Escherichia coli BL21
-
DNA encoding the last 48 residues of the propart and the whole mature sequence of plasmepsin II is inserted into the T7 dependent vector pET 3a for high level expression in Escherichia coli
-
engineering a plasmepsin II with the active site surface of plasmepsin I and expression in Escherichia coli
-
expressed in Escherichia coli
-
expressed in Escherichia coli as a recombinant protein
-
expression as a glutathione-S-transferase-proteinase fusion construct in Escherichia coli
-
expression in Escherichia coli
-
PSM2 (residues 78-453) are recombinantly expressed
-
recombinantly expressed in Escherichia coli
-
recombinantly expressed in Escherichia coli BL21
-
wild-type and mutant enzymes
-
ENGINEERING
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
D158A
-
active-site mutant of both plasmepsin II and IV shows neither autocatalytic processing nor proteolytic activities
D338A
-
active-site mutant of both plasmepsin II and IV shows neither autocatalytic processing nor proteolytic activities
I287E
-
changes in substrate specificity compared to wild-type enzyme, the turnover-number for Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro is 42% of that of the wild-type enzyme, the Km-value is 51% of that of the wild-type enzyme
M13E
-
the turnover-number for Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro is 1.16fold higher than the turnover-number of the wild-type enzyme, the Km-value is 54% of that of the wild-type enzyme
M13E/I287E
-
changes in substrate specificity compared to wild-type enzyme, the turnover-number for Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-Pro is 1.48fold higher than the turnover-number of the wild-type enzyme, the Km-value is 1.23fold higher than that of the wild-type enzyme
proteolytic modification
-
prodomain processing of plasmepsin II and plasmepsin IV occurs via an intra- and inter-molecular autocatalytic event as well as via a transcatalytic event between them
S77D
-
changes in substrate specificity compared to wild-type enzyme, cleavage of Lys-Glu-Phe-Val-Lys-Phe(NO2)-Ala-Leu-Lys that is not cleaved by the wild-type enzyme, the turnover-number for Ala-Leu-Glu-Arg-Nle-Phe-Phe(NO2)-Ser-Phe-is 54% of the turnover-number of the wild-type enzyme, the Km-value is 71% of that of the wild-type enzyme
D214A
-
mutation abolishes proteolytic activity
D34A
-
mutation abolishes proteolytic activity
D34S
-
mutation abolishes proteolytic activity
D34S/D214S
-
mutation abolishes proteolytic activity
M205S
-
mutant enzyme with reduced chances of autolysis during purification
additional information
-
engineering a plasmepsin II with the active site surface of plasmepsin I largely maintains the plasmepsin II substrate and inhibitor specificity
additional information
-
active-site mutants of both plasmepsin II and IV showed neither autocatalytic processing nor proteolytic activities. The mutants of both plasmepsins are efficiently processed upon incubation with their respective wild type proteins
additional information
-
the role of the prosegment in aspartic proteinase structure and function is investigated by generating a chimeric protein consisting of the porcine pepsinogen prosegment fused to the mature region of PMII (pepproPMII): Chimeric protein pepproPMII is capable of both autoactivation and hydrolysis of a synthetic substrate. CD measurements indicate that pepproPMII has reduced thermal stability when compared with zymogen PMII. Prosegment is not critical to obtain a functional enzyme but likely plays a role in protein stabilization; the role of the prosegment in aspartic proteinase structure and function is investigated by generating a chimeric protein consisting of the prosegment of PMII fused to pepsin (PMIIpropep). Chimeric protein is expressed in Escherichia coli but extremely unstable suggesting protein misfolding
Renatured/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
differential scanning calorimetry reveals that the native state of PMII is irreversibly unfolded, and in the pH range of 6.5-8.0, PMII refolds to a denatured state with higher thermal stability than native state. The denatured state can also be formed upon partially unfolding PMII at pH 11.0 and 37C for 2 h, followed by adjustment to a pH in the range of 6.5-8.0. While the denatured state can be folded/unfolded reversibly, the native state exists as a kinetically trapped state. The native state is kinetically trapped by an unfolding barrier of 25.5 kcal/mol, and yet once unfolded, is prevented from folding by a comparable folding barrier
-
APPLICATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
analysis
-
cheap and high-throughput heterogeneous enzymatic assay for measuring plasmepsin II activity in order to use it as a tool in the discovery of new inhibitors of this enzyme
medicine
-
inhibitors of plasmepsin II are potential antimalarial agents
medicine
-
plasmepsin is an important target for the development of antimalarial drugs, since its inhibition leads to the starvation of Plasmodium falciparum
molecular biology
-
plasmepsin 2 but not plasmepsin 4 is a pential tool for hydrogen/deuterium exchange coupled to mass spectroscopy (DXMS) studies