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Literature summary for 3.4.23.B19 extracted from

  • Gazdik, M.; Jarman, K.E.; ONeill, M.T.; Hodder, A.N.; Lowes, K.N.; Jousset Sabroux, H.; Cowman, A.F.; Boddey, J.A.; Sleebs, B.E.
    Exploration of the P3 region of PEXEL peptidomimetics leads to a potent inhibitor of the Plasmodium protease, plasmepsin V (2016), Bioorg. Med. Chem., 24, 1993-2010 .
    View publication on PubMed
Search for more literature for 3.4.23.B19

Inhibitors

Inhibitors Comment Organism Structure
3-amino-N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
4-amino-N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N-[(benzyloxy)carbonyl]-3-carbamimidamido-L-phenylalanyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N-[(benzyloxy)carbonyl]-4-carbamimidamido-L-phenylalanyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N-[(benzyloxy)carbonyl]-O-carbamimidamido-L-homoseryl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-L-arginyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N-carbamimidoyl-L-glutaminyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-(methylsulfonyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-(N-cyanocarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-(N-hydroxycarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-(N-methoxycarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-(N-methylcarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-(N-nitrocarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-(propan-2-yl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-carbamimidoyl-N5-methyl-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-carbamoyl-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N2-[(benzyloxy)carbonyl]-N5-ethanimidoyl-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
N5-acetyl-N2-[(benzyloxy)carbonyl]-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
-
 Plasmodium falciparum
WEHI-842 potent inhibitor Plasmodium falciparum
WEHI-916 potent inhibitor Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q8I6Z5 isolate 3D7
-

Synonyms

Synonyms Comment Organism
PMV
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
 pH and temperature not specified in the publication Plasmodium falciparum WEHI-842
0.000121
-
 pH and temperature not specified in the publication Plasmodium falciparum WEHI-916
0.000128
-
 at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-L-arginyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.00274
-
 at pH 6.4 and 37°C Plasmodium falciparum N-[(benzyloxy)carbonyl]-O-carbamimidamido-L-homoseryl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.00388
-
 at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-(N-hydroxycarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.0377
-
 at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-(N-methylcarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.0403
-
 at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-ethanimidoyl-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.0416
-
 at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N-carbamimidoyl-L-glutaminyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-carbamoyl-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum 3-amino-N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum 4-amino-N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum N-[(benzyloxy)carbonyl]-3-carbamimidamido-L-phenylalanyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum N-[(benzyloxy)carbonyl]-4-carbamimidamido-L-phenylalanyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-(methylsulfonyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-(N-cyanocarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-(N-nitrocarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-(propan-2-yl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-carbamimidoyl-N5-methyl-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.05
-
 IC50 above 0.05 mM, at pH 6.4 and 37°C Plasmodium falciparum N5-acetyl-N2-[(benzyloxy)carbonyl]-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide
0.18
-
 at pH 6.4 and 37°C Plasmodium falciparum N2-[(benzyloxy)carbonyl]-N5-(N-methoxycarbamimidoyl)-L-ornithyl-N-[(3S,4S)-3-hydroxy-6-methyl-1-oxo-1-[(2-phenylethyl)amino]heptan-4-yl]-L-valinamide