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Literature summary for 3.4.23.39 extracted from

  • Degliesposti, G.; Kasam, V.; Da Costa, A.; Kang, H.K.; Kim, N.; Kim, D.W.; Breton, V.; Kim, D.; Rastelli, G.
    Design and discovery of plasmepsin II inhibitors using an automated workflow on large-scale grids (2009), ChemMedChem, 4, 1164-1173.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinantly expressed in Escherichia coli BL21 Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
(1Z)-N'-{[(4-chloro-3,5-dimethylphenoxy)acetyl]oxy}-2-(3,4-dimethoxyphenyl)ethanimidamide
-
Plasmodium falciparum
2-(1,3-benzothiazol-2-ylamino)-N-(2-chlorophenyl)-6-oxo-1,4,5,6­tetrahydro-4-pyrimidinecarboxamide
-
Plasmodium falciparum
2-(1-naphthyl)-N'-[(4-nitrobenzoyl)oxy]ethanimidamide
-
Plasmodium falciparum
2-([N-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-(methylsulfonyl)glycyl]amino)-N-isobutylbenzamide
-
Plasmodium falciparum
2-anilino-3-chloro-N-phenyl-4-(phenylimino)-2-butenamide
-
Plasmodium falciparum
2-anilino-4-(3-furyl)-6-oxo-N-phenyl-1-cyclohexene-1-carboxamide
-
Plasmodium falciparum
3-chloro-N-([2-(2-methoxybenzoyl)hydrazino]carbonothioyl)-1-benzothiophene-2-carboxamide
-
Plasmodium falciparum
4-amino-N'-(benzyloxy)-N-(2-methylphenyl)-1,2,5-oxadiazole-3­carboximidamide
-
Plasmodium falciparum
4-amino-N'-(benzyloxy)-N-(4-methylphenyl)-1,2,5-oxadiazole-3­carboximidamide
-
Plasmodium falciparum
4-amino-N'-[(2,4-dichlorobenzyl)oxy]-N-(2-methylphenyl)-1,2,5­oxadiazole-3-carboximidamide
-
Plasmodium falciparum
4-amino-N'-[(2-methyl-1-naphthyl)methoxy]-1,2,5-oxadiazole-3­carboximidamide
-
Plasmodium falciparum
4-methoxy-N-(2-[5-(2-nitrophenyl)-2-furyl]-1-([(4-pyridinylmethyl)amino]carbonyl)vinyl)benzamide
-
Plasmodium falciparum
6-((2-[(5-chloro-2-methoxyphenyl)amino]-2-oxoethyl)thio)-5-cyano-N-(2-methoxyphenyl)-2-methyl-4-phenyl-1,4-dihydro-3-pyridinecarboxamide
-
Plasmodium falciparum
6-bromo-2,3,4,9-tetrahydro-1H-carbazol-1-one N­phenylthiosemicarbazone
-
Plasmodium falciparum
N',N'''-1,2-phenylenebis[N-(3-chlorophenyl)urea]
-
Plasmodium falciparum
N'-[(4-methoxy-3-nitrobenzoyl)oxy]-2-(1-naphthyl)ethanimidamide
-
Plasmodium falciparum
N,N'-([(4,6-dimethyl-2-quinazolinyl)amino]methylylidene)dipropanamide
-
Plasmodium falciparum
N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-methyl-4-oxo-1,4-dihydro-2-pyrimidinyl)amino]methylene)benzamide
-
Plasmodium falciparum
N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-oxo-4-propyl-1,6-dihydro-2-pyrimidinyl)amino]methylene)-4-methoxybenzamide
-
Plasmodium falciparum
N-(([2-(4-ethylphenyl)-6-methyl-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
-
Plasmodium falciparum
N-(([6-methyl-2-(4-methylphenyl)-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
-
Plasmodium falciparum
N-(1,3-benzodioxol-5-ylmethyl)-N'-[4-(2-oxo-2H-chromen-3-yl)-1,3­thiazol-2-yl]succinamide
-
Plasmodium falciparum
N-(2-([3-(1,3-benzodioxol-5-yl)-3-oxo-1-propen-1-yl]amino)phenyl)-4-nitrobenzenesulfonamide
-
Plasmodium falciparum
N-(2-methoxyphenyl)-2-(5H-[1,2,4]triazino[5,6-b]indol-3­ylthio)butanamide
-
Plasmodium falciparum
N-(3,4-dichlorophenyl)-2-[(4,6-dimethyl-2-pyrimidinyl)amino]­3a,4,5,6,7,7a-hexahydro-1H-benzimidazole-1-carboxamide
-
Plasmodium falciparum
N-(3,4-dimethylphenyl)-N'-(imino[(4,6,7-trimethyl-2-quinazolinyl)amino]methyl)thiourea
-
Plasmodium falciparum
N-(amino[(4,6-dimethyl-2-quinazolinyl)amino]methylene)-2-(4-chlorophenyl)acetamide
-
Plasmodium falciparum
N-([(2,4-dimethylphenyl)amino][(4-oxo-1,4,5,6,7,8-hexahydro-2-quinazolinyl)amino]methylene)benzamide
-
Plasmodium falciparum
N-benzyl-2-([3-(3-nitrophenyl)acryloyl]amino)benzamide
-
Plasmodium falciparum
N-[(cyclopentylamino)carbonothioyl]-4-ethoxy-3-nitrobenzamide
-
Plasmodium falciparum
pepstatin A
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
using a Q-Sepharose fast flow column Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DABCYL-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-EDANS + H2O FRET substrate, substrate is designed to mimic the hemoglobin cleavage site. The substrate is conjugated with the fluorescent donor EDANS and the quencher DABCYL Plasmodium falciparum ?
-
?

Synonyms

Synonyms Comment Organism
plasmepsin II
-
Plasmodium falciparum

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
4.5
-
assay at Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000043
-
pH 4.5, 37°C Plasmodium falciparum (1Z)-N'-{[(4-chloro-3,5-dimethylphenoxy)acetyl]oxy}-2-(3,4-dimethoxyphenyl)ethanimidamide
0.0000045
-
pH 4.5, 37°C Plasmodium falciparum N-[(cyclopentylamino)carbonothioyl]-4-ethoxy-3-nitrobenzamide
0.0000055
-
pH 4.5, 37°C Plasmodium falciparum 4-amino-N'-[(2,4-dichlorobenzyl)oxy]-N-(2-methylphenyl)-1,2,5­oxadiazole-3-carboximidamide
0.0000064
-
pH 4.5, 37°C Plasmodium falciparum 4-amino-N'-(benzyloxy)-N-(2-methylphenyl)-1,2,5-oxadiazole-3­carboximidamide
0.0000076
-
pH 4.5, 37°C Plasmodium falciparum N',N'''-1,2-phenylenebis[N-(3-chlorophenyl)urea]
0.0000088
-
pH 4.5, 37°C Plasmodium falciparum N-([(2,4-dimethylphenyl)amino][(4-oxo-1,4,5,6,7,8-hexahydro-2-quinazolinyl)amino]methylene)benzamide
0.0000095
-
pH 4.5, 37°C Plasmodium falciparum N-(3,4-dichlorophenyl)-2-[(4,6-dimethyl-2-pyrimidinyl)amino]­3a,4,5,6,7,7a-hexahydro-1H-benzimidazole-1-carboxamide
0.00003
-
pH 4.5, 37°C Plasmodium falciparum N-benzyl-2-([3-(3-nitrophenyl)acryloyl]amino)benzamide
0.0000389
-
pH 4.5, 37°C Plasmodium falciparum N-(2-([3-(1,3-benzodioxol-5-yl)-3-oxo-1-propen-1-yl]amino)phenyl)-4-nitrobenzenesulfonamide
0.0000426
-
pH 4.5, 37°C Plasmodium falciparum 4-amino-N'-[(2-methyl-1-naphthyl)methoxy]-1,2,5-oxadiazole-3­carboximidamide
0.0000573
-
pH 4.5, 37°C Plasmodium falciparum 6-((2-[(5-chloro-2-methoxyphenyl)amino]-2-oxoethyl)thio)-5-cyano-N-(2-methoxyphenyl)-2-methyl-4-phenyl-1,4-dihydro-3-pyridinecarboxamide
0.0000621
-
pH 4.5, 37°C Plasmodium falciparum N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-methyl-4-oxo-1,4-dihydro-2-pyrimidinyl)amino]methylene)benzamide
0.0000875
-
pH 4.5, 37°C Plasmodium falciparum pepstatin A
0.0000875
-
pH 4.5, 37°C Plasmodium falciparum N-(2-methoxyphenyl)-2-(5H-[1,2,4]triazino[5,6-b]indol-3­ylthio)butanamide
0.0000961
-
pH 4.5, 37°C Plasmodium falciparum 2-(1,3-benzothiazol-2-ylamino)-N-(2-chlorophenyl)-6-oxo-1,4,5,6­tetrahydro-4-pyrimidinecarboxamide
0.0001181
-
pH 4.5, 37°C Plasmodium falciparum N-((2,3-dihydro-1,4-benzodioxin-6-ylamino)[(6-oxo-4-propyl-1,6-dihydro-2-pyrimidinyl)amino]methylene)-4-methoxybenzamide
0.0001229
-
pH 4.5, 37°C Plasmodium falciparum N-(([6-methyl-2-(4-methylphenyl)-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
0.0001452
-
pH 4.5, 37°C Plasmodium falciparum 2-(1-naphthyl)-N'-[(4-nitrobenzoyl)oxy]ethanimidamide
0.0001464
-
pH 4.5, 37°C Plasmodium falciparum N-(([2-(4-ethylphenyl)-6-methyl-2H-1,2,3-benzotriazol-5-yl]amino)carbonothioyl)-2-nitrobenzamide
0.0001871
-
pH 4.5, 37°C Plasmodium falciparum 2-anilino-4-(3-furyl)-6-oxo-N-phenyl-1-cyclohexene-1-carboxamide
0.000189
-
pH 4.5, 37°C Plasmodium falciparum 2-anilino-3-chloro-N-phenyl-4-(phenylimino)-2-butenamide
0.0002011
-
pH 4.5, 37°C Plasmodium falciparum 3-chloro-N-([2-(2-methoxybenzoyl)hydrazino]carbonothioyl)-1-benzothiophene-2-carboxamide
0.0002364
-
pH 4.5, 37°C Plasmodium falciparum N'-[(4-methoxy-3-nitrobenzoyl)oxy]-2-(1-naphthyl)ethanimidamide
0.0002374
-
pH 4.5, 37°C Plasmodium falciparum N,N'-([(4,6-dimethyl-2-quinazolinyl)amino]methylylidene)dipropanamide
0.000305
-
pH 4.5, 37°C Plasmodium falciparum 4-amino-N'-(benzyloxy)-N-(4-methylphenyl)-1,2,5-oxadiazole-3­carboximidamide
0.001088
-
pH 4.5, 37°C Plasmodium falciparum N-(3,4-dimethylphenyl)-N'-(imino[(4,6,7-trimethyl-2-quinazolinyl)amino]methyl)thiourea
0.001831
-
pH 4.5, 37°C Plasmodium falciparum 6-bromo-2,3,4,9-tetrahydro-1H-carbazol-1-one N­phenylthiosemicarbazone