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Literature summary extracted from

  • Noteberg, D.; Hamelink, E.; Hulten, J.; Wahlgren, M.; Vrang, L.; Samuelsson, B.; Hallberg, A.
    Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes (2003), J. Med. Chem., 46, 734-746.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.23.38 (2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 (5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
 Plasmodium falciparum
3.4.23.38 (5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 (5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
 Plasmodium falciparum
3.4.23.39 (5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
 Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
3.4.23.38 Plasmodium falciparum
-
-
-
3.4.23.39 Plasmodium falciparum
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.23.38 additional information Plasmodium falciparum-infected cultured human erythrocytes Plasmodium falciparum
-
3.4.23.39 additional information Plasmodium falciparum-infected cultured human erythrocytes Plasmodium falciparum
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.23.38 4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid + H2O
-
 Plasmodium falciparum 4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Nle-Phe + Leu-Ser-Phe-Pro-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
-
 ?
3.4.23.39 4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid + H2O
-
 Plasmodium falciparum ?
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.23.38 0.000063
-
 (2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.000068
-
 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.000098
-
 (2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.000115
-
 (2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.000438
-
 (2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.000469
-
 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.00053
-
 (2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.001
-
 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.0011
-
 (2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.0013
-
 (2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.38 0.0019
-
 (5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
 Plasmodium falciparum
3.4.23.38 0.002046
-
 (5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
 Plasmodium falciparum
3.4.23.39 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 Plasmodium falciparum
3.4.23.39 0.0000928
-
 (5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
 Plasmodium falciparum
3.4.23.39 0.000117
-
 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 0.000121
-
 (2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 0.000129
-
 (2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 0.00015
-
 (2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 0.000379
-
 (2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 0.00054
-
 (2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 0.000579
-
 (2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 0.00093
-
 (2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum
3.4.23.39 0.00143
-
 (2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
 Plasmodium falciparum