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Literature summary for 3.4.22.51 extracted from

  • Chen, Y.T.; Lira, R.; Hansell, E.; McKerrow, J.H.; Roush, W.R.
    Synthesis of macrocyclic trypanosomal cysteine protease inhibitors (2008), Bioorg. Med. Chem. Lett., 18, 5860-5863.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.51

Inhibitors

Inhibitors Comment Organism Structure
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
-
 Trypanosoma brucei rhodesiense
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
-
 Trypanosoma cruzi
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
-
 Trypanosoma brucei rhodesiense
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
-
 Trypanosoma cruzi
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-(morpholin-4-ylcarbonyl)-L-phenylalaninamide
-
 Trypanosoma cruzi
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
-
 Trypanosoma brucei rhodesiense
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
-
 Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei rhodesiense
-
-
-
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Phe-Arg-AMC
-
 Trypanosoma cruzi ?
-
 ?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Trypanosoma brucei rhodesiense ?
-
 ?

Synonyms

Synonyms Comment Organism
cruzain
-
 Trypanosoma cruzi
rhodesain
-
 Trypanosoma brucei rhodesiense

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000004
-
-
 Trypanosoma cruzi Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
0.0001
-
-
 Trypanosoma brucei rhodesiense Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
0.0002
-
-
 Trypanosoma cruzi (3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
0.006
-
-
 Trypanosoma brucei rhodesiense (3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
0.01
-
-
 Trypanosoma brucei rhodesiense (3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
0.01
-
 above 0.01 mM Trypanosoma cruzi (3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide