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(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(morpholin-4-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(morpholin-4-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(naphthalen-2-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(naphthalen-2-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(phenylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(phenylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1,3-benzothiazol-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1,3-benzothiazol-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1,3-benzothiazol-6-ylmethyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1,3-benzothiazol-6-ylmethyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1-benzofuran-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1-benzofuran-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1-benzothiophen-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1-benzothiophen-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1H-benzotriazol-5-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1H-benzotriazol-5-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1H-indol-5-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1H-indol-5-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(1H-indol-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(1H-indol-6-ylcarbonyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-(4-[(1S)-1-[(4-methoxybenzyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-(4-[(1S)-1-[(4-methoxybenzyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(1-methyl-1H-indol-6-yl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(1-methyl-1H-indol-6-yl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(2-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(2-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(3-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(3-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(4-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1,2-dimethyl-1-[[(4-methylphenyl)carbonyl]amino]propyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1-(benzylamino)-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1-(benzylamino)-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1-[[(2-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1-[[(2-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1-[[(3-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1-[[(3-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
(7-[[(2S)-2-[4-[(1S)-1-[[(4-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoyl]amino]-4-methyl-2-oxo-3,4-dihydro-2H-chromen-3-yl)acetic acid + H2O
(2S)-2-[4-[(1S)-1-[[(4-methoxyphenyl)carbonyl]amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl]hexanoic acid + 7-amino-4-methylcoumarin-3-acetic acid
-
-
-
ir
2-aminobenzoic acid-ALRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
?
2-aminobenzoic acid-KLGFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
?
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
and analogues
-
-
?
2-aminobenzoic acid-peptidyl-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
and derivatives, enzyme shows preference for benzyl-Cys or Arg at the P1 position and a hydrophobic non-aromatic residue at position P2
-
-
?
2-aminobenzoyl-ARF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2 + H2O
?
-
-
-
-
?
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-FRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Pro-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Trp-OH + H2O
?
-
-
-
-
?
2-aminobenzoyl-RRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH + H2O
?
-
-
-
-
?
Ac-Phe-Arg-7-amido-4-methylcoumarin + H2O
Ac-Phe-Arg + 7-amino-4-methylcoumarin
-
10 microM, 4 nanoM cruzain, 45 min, room temperature, pH 5.5
-
-
?
benzoyl-FR-4-methylcoumarin 7-amide + H2O
?
benzoyl-His-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-His-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzoyl-HR-4-methylcoumarin 7-amide + H2O
?
less susceptible substrate
-
-
?
benzoyl-PFR-4-nitroanilide + H2O
?
benzoyl-Phe-Arg-4-methylcoumarin-7-amide + H2O
?
fluorogenic substrates based on the peptide benzoyl-Phe-Arg-4-methylcoumarin-7-amide
-
-
?
benzoyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Arg + 7-amino-4-methylcoumarin
benzoyl-Phe-Val-Arg-p-nitroanilide + H2O
?
-
as active as with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzoyl-Pro-Phe-Arg-p-nitroanilide + H2O
?
-
41% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzoyl-RR-4-methylcoumarin 7-amide + H2O
?
less susceptible substrate
-
-
?
benzoyl-Tyr-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Tyr-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzoyl-Val-Gly-Arg-p-nitroanilide + H2O
?
-
52% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzoyl-YR-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
benzyloxycarbonyl-Ala-Arg-Arg-methoxy-beta-naphthylamide + H2O
?
-
36% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Arg-Ala + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Arg-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide + H2O
?
-
-
-
-
?
benzyloxycarbonyl-Gly-Pro-Arg-p-nitroanilide + H2O
?
-
66% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
benzyloxycarbonyl-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Phe-L-Arg + 7-amino-4-methylcoumarin
relatively low rates of substrate hydrolysis
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Phe-Arg-methoxy-beta-naphthylamide + H2O
?
-
30% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
Bovine serum albumin + H2O
?
-
-
-
?
Bz-Phe-Arg-4-methylcoumaryl-7-amide + H2O
Bz-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
Bz-Pro-Phe-Arg-4-nitroanilide + H2O
Bz-Pro-Phe-Arg + 4-nitroaniline
-
-
-
-
?
epsilon-NH2(capryl)-L-(SBzl)C-7-amido-4-methylcoumarin + H2O
?
-
-
-
-
?
human IgG + H2O
?
-
specific cleavage sites on human IgG subclasses by cruzipain
-
-
?
human NF-kappaB P65 + H2O
?
-
-
-
-
?
Immunoglobulin G1 + H2O
?
Immunoglobulin G3 + H2O
?
insulin A + H2O
?
-
-
-
?
insulin B + H2O
?
-
-
-
?
Lys-Arg-primaquine + H2O
Lys-Arg + primaquine
-
-
-
-
?
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine-(7-amido-4-methylcoumarin) + H2O
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine + 7-amino-4-methylcoumarin
-
-
-
-
?
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine-(7-amido-4-methylcoumarin) + H2O
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine + 7-amino-4-methylcoumarin
-
-
-
-
?
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine-(7-amido-4-methylcoumarin) + H2O
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine + 7-amino-4-methylcoumarin
-
-
-
-
?
N-carbobenzoxy-Arg-Arg-2-(4-methoxy)-naphthylamide + H2O
N-carbobenzoxy-Arg-Arg + 2-amino-4-methoxynaphthalene
-
-
-
?
N-carbobenzoxy-Val-Val-Arg-4-nitroanilide + H2O
?
N-carbobenzoxy-VVR-4-nitroanilide + H2O
N-carbobenzoxy-VVR + 4-nitroaniline
N-tert-butoxycarbonyl-O-benzyl-Ser-Gly-Arg-p-nitroanilide + H2O
?
-
39% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
N-tert-butoxycarbonyl-Val-Leu-Gly-Arg-p-nitroanilide + H2O
?
-
24% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
o-aminobenzoyl-ALRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-HLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-KARFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-KFRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-KLFFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLF + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLGFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLG + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLKFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLK + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFFKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FFKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFPKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FPKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFSFQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSFQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
no hydrolysis is detected
-
-
?
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFSPQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSPQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRFSRQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + FSRQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRLSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + LSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KLRRSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
o-aminobenzoyl-KLR + RSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
-
-
?
o-aminobenzoyl-KPRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-KRRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
o-aminobenzoyl-LLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
?
-
-
-
-
?
peptidyl-4-nitroanilide + H2O
?
derivatives of
-
-
?
peptidyl-beta-naphthylamide + H2O
?
peptidyl-methylcoumarin amide + H2O
?
and derivatives, enzyme shows preference for benzyl-Cys or Arg at the P1 position and a hydrophobic non-aromatic residue at position P2
-
-
?
Phe-Ala-primaquine + H2O
Phe-Ala + primaquine
-
-
-
-
?
Phe-Arg-primaquine + H2O
Phe-Arg + primaquine
-
-
-
-
?
tosyl-Gly-Pro-Arg-p-nitroanilide + H2O
tosyl-Gly-Pro-Arg + p-nitroaniline
-
25% of the activity with benzyloxycarbonyl-Arg-Arg-methoxy-beta-naphthylamide
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
additional information
?
-
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
?
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
Abz-LGMISLMKRPQ-EDDnp
-
-
?
azocasein + H2O
?
-
-
-
?
azocasein + H2O
?
-
-
-
-
?
azocasein + H2O
?
-
-
-
?
benzoyl-FR-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
benzoyl-FR-4-methylcoumarin 7-amide + H2O
?
-
-
-
-
?
benzoyl-FR-4-methylcoumarin 7-amide + H2O
?
fluorigenic substrates based on this peptide, substitution of Phe results in less susceptible substrates
-
-
?
benzoyl-PFR-4-nitroanilide + H2O
?
-
-
-
?
benzoyl-PFR-4-nitroanilide + H2O
?
-
-
-
-
?
benzoyl-PFR-4-nitroanilide + H2O
?
-
-
-
?
benzoyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzoyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzoyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
?
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
Gelatin + H2O
?
-
pH 5.5 or 10
-
-
?
Hemoglobin + H2O
?
-
-
-
-
?
Hemoglobin + H2O
?
-
-
-
?
Immunoglobulin G1 + H2O
?
-
-
-
?
Immunoglobulin G1 + H2O
?
cleaves specifically at the hinge region
-
-
?
Immunoglobulin G3 + H2O
?
-
-
-
?
Immunoglobulin G3 + H2O
?
cleaves specifically at the hinge region
-
-
?
KEEASSAVVGGPG + H2O
?
-
-
-
?
KEEASSAVVGGPG + H2O
?
-
-
-
-
?
KEEASSAVVRGPG + H2O
?
-
-
-
?
KEEASSAVVRGPG + H2O
?
-
-
-
-
?
N-carbobenzoxy-Val-Val-Arg-4-nitroanilide + H2O
?
-
-
-
?
N-carbobenzoxy-Val-Val-Arg-4-nitroanilide + H2O
?
excellent substrate
-
-
?
N-carbobenzoxy-VVR-4-nitroanilide + H2O
N-carbobenzoxy-VVR + 4-nitroaniline
-
-
-
?
N-carbobenzoxy-VVR-4-nitroanilide + H2O
N-carbobenzoxy-VVR + 4-nitroaniline
-
-
-
-
?
peptidyl-beta-naphthylamide + H2O
?
derivatives of
-
-
?
peptidyl-beta-naphthylamide + H2O
?
-
derivatives of
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
?
-
-
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
?
-
5 microM, pH 6.5, 28°C
-
-
?
additional information
?
-
-
enzyme may be involved in facilitating parasite entry into the brain
-
-
?
additional information
?
-
-
enzyme may be involved in facilitating parasite entry into the brain
-
-
?
additional information
?
-
no substrate: benzyloxycarbonyl-Arg-Arg-aminomethyl coumarin
-
-
?
additional information
?
-
-
no substrate: benzyloxycarbonyl-Arg-Arg-aminomethyl coumarin
-
-
?
additional information
?
-
substrates are chromogenic peptides with a carboxyl Arg or Lys, enzyme requires at least one more amino acid, preferably Arg, Phe, Val or Leu between the terminal Arg or Lys and the amino-blocking group
-
-
?
additional information
?
-
substrates are chromogenic peptides with a carboxyl Arg or Lys, enzyme requires at least one more amino acid, preferably Arg, Phe, Val or Leu between the terminal Arg or Lys and the amino-blocking group
-
-
?
additional information
?
-
-
substrates are chromogenic peptides with a carboxyl Arg or Lys, enzyme requires at least one more amino acid, preferably Arg, Phe, Val or Leu between the terminal Arg or Lys and the amino-blocking group
-
-
?
additional information
?
-
synthetic chromogenic sustrates
-
-
?
additional information
?
-
-
synthetic chromogenic sustrates
-
-
?
additional information
?
-
antigenic character in natural human infections
-
-
?
additional information
?
-
-
antigenic character in natural human infections
-
-
?
additional information
?
-
stimulates potent humoral and cellular immune response during infection in both humans and mice
-
-
?
additional information
?
-
-
stimulates potent humoral and cellular immune response during infection in both humans and mice
-
-
?
additional information
?
-
enzyme plays a role in the production of antibodies against cardiac M2 muscarinic acetylcholine receptor
-
-
?
additional information
?
-
-
enzyme plays a role in the production of antibodies against cardiac M2 muscarinic acetylcholine receptor
-
-
?
additional information
?
-
-
cruzipain may act as a survival factor for cardiomyocytes because it rescues them from apoptosis and stimulates arginase-2
-
-
?
additional information
?
-
-
substrate specificity of cruzipain 2 isoform is analysed using internally quenched flurogenic substrates. It is found that cruzipain 2 compared to cruzipain differs substantially regarding the specificity in the S2, S1' and S2' pockets, suggesting that cruzipain 2 acts on distinct natural substrates
-
-
?
additional information
?
-
-
design of selective prodrugs of primaquine: Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine, cleaved by the enzyme in vivo and selectively inhibiting it, overview
-
-
?
additional information
?
-
-
design of selective prodrugs of primaquine: Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine, cleaved by the enzyme in vivo and selectively inhibiting it, overview. The molecular mechanism acts via nucleophilic attack of the catalytic Cys25 residue on the respective prodrug amide carbonyl carbon, releasing primaquine, docking study showing specific interactions between the prodrug and the S1 and S2 pockets of cruzipain with the dipeptides acting as distance holders
-
-
?
additional information
?
-
-
involvement of O-linked GlcNAc moiety present in the major cysteine protease both in cruzipain recognition and in the cross-reactivity between cruzipain and myosin molecules
-
-
?
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(1E)-1-(3,4-dichlorophenyl)-2-phenylethan-1-one thiosemicarbazone
-
IC50: 80 nM
(1E)-1-(3,4-dichlorophenyl)-3-phenylpropan-1-one thiosemicarbazone
-
IC50: 40 nM
(1E)-1-(3,4-dichlorophenyl)pentan-1-one thiosemicarbazone
-
IC50: 19 nM
(1E)-1-(3,4-dichlorophenyl)propan-1-one thiosemicarbazone
-
IC50: 30 nM
(1E)-1-(3-bromophenyl)propan-1-one thiosemicarbazone
-
IC50: 310 nM
(1E,2E)-1-(3,4-dichlorophenyl)-3-phenylprop-2-en-1-one thiosemicarbazone
-
IC50: 30 nM
(1Z)-1-(3,4-dichlorophenyl)-2-phenoxyethan-1-one thiosemicarbazone
-
IC50: 30 nM
(2(1H)-pyridinethionato-kappaS2)[2,6-bis[(mercapto-KappaS)methyl]pyridine-kappaN1] oxorhenium(V)
-
-
(2E)-1,3-bis(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-1,3-di(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(1-naphthyl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2,6-dichlorophenyl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2-chlorophenyl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(3-methoxy-4-phenoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(4-buthoxyphenyl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(5-methylfuran-2-yl)-2-propen-1-one
-
-
(2E)-1-(1,3-benzodioxol-5-yl)-3-(thiophen-2-yl)-2-propen-1-one
-
-
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
-
-
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(thiophen-2-yl)-2-propen-1-one
-
-
(2E)-1-(2'-hydroxy,3'-bromo,4',6'-dimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
-
-
(2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-buthoxyphenyl)-2-propen-1- one
-
-
(2E)-1-(2,4-dimethoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(2-naphthyl)-3-(2,6-dimethoxyphenyl)-2-propen-1-one
-
-
(2E)-1-(2-naphthyl)-3-(5-methylfuran-2-yl)-2-propen-1-one
-
-
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
-
-
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methylphenyl)prop-2-en-1-one
-
-
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-phenylprop-2-en-1-one
-
-
(2E)-1-(4-hydroxy-1,3-benzodioxol-5-yl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-2-[1-([1,1'-biphenyl]-4-yl)-2-(4-bromophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 11.8% inhibition, 23°C, pH 5.5; 0.05 mM, 88.9% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-bromophenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 67.5% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-chlorophenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 53.1% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-fluorophenyl)ethylidene]-N-methylhydrazine-1-carbothioamide
0.05 mM, 30.0% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-fluorophenyl)ethylidene]-N-phenylhydrazine-1-carbothioamide
0.05 mM, 35.0% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-fluorophenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 38.7% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-methoxyphenyl)ethylidene]-N-methylhydrazine-1-carbothioamide
0.05 mM, 29.8% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-methoxyphenyl)ethylidene]-N-phenylhydrazine-1-carbothioamide
0.05 mM, 42.8% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-methoxyphenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 70.9% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(4-methylphenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 67.6% inhibition, 23°C, pH 5.5
(2E)-2-[2-(4-bromophenoxy)-1-(naphthalen-1-yl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 73.6% inhibition, 23°C, pH 5.5
(2E)-2-{4-[(3-oxido-2,1,3-benzoxadiazol-5-yl)methoxy]benzylidene}hydrazinecarboximidamide
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-3-(3-methoxyphenyl)-1-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(4-bromophenyl)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)prop-2-en-1-one
-
-
(2E)-3-(4-fluorophenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-3-[4-(benzyloxy)-3-methoxyphenyl]-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-N'-(3'-bromo-4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
-
(2E)-N'-(4'-buthoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
-
(2E)-N'-(4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
-
(2S)-2-(1-[1-[(Z)-1-chloro-2-(phenylsulfonyl)ethenyl]pentyl]-1H-1,2,3-triazol-4-yl)-3-methyl-N-(quinolin-6-ylmethyl)butan-2-amine
10 microM
(2S)-3-methyl-2-(1-[1-[(E)-2-(phenylsulfonyl)ethenyl]pentyl]-1H-1,2,3-triazol-4-yl)-N-(quinolin-6-ylmethyl)butan-2-amine
10 microM
(2S)-N-(1-cyano-1-methylethyl)-3-phenyl-2-(phenylformamido)propanamide
i.e. Neq0410, inhibition is enthalpy driven with a clear detrimental contribution of the entropy difference to the free binding energy
(2S)-N-(1-cyanocyclopropyl)-3-phenyl-2-(phenylformamido)propanamide
i.e. Neq0570, inhibition is enthalpy driven with a clear detrimental contribution of the entropy difference to the free binding energy
(2S)-N-(cyanomethyl)-3-phenyl-2-(phenylformamido)-propanamide
i.e. Neq0409, inhibition is enthalpy driven with a clear detrimental contribution of the entropy difference to the free binding energy
(2Z)-2-(2-[([1,1'-biphenyl]-3-yl)oxy]-1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamide
0.05 mM, 65.4% inhibition, 23°C, pH 5.5
(2Z)-2-(2-[([1,1'-biphenyl]-4-yl)oxy]-1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamide
0.05 mM, 63.7% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(2,3-dichlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 81.8% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(2-chlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 58.9% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(3,4-dichlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 99.1% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(3-chloro-4-fluorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 93.7% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(3-chlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM,51.8 % inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(3-methoxyphenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 62.8% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-chlorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 76.3% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-ethylphenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 75.1% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-fluorophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 84.0% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-iodophenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 63.3% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-methoxyphenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 75.8% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-(4-tert-butylphenoxy)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 85.3% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-phenoxyethylidene]hydrazine-1-carbothioamide
0.05 mM, 61.8% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-[(naphthalen-1-yl)oxy]ethylidene]hydrazine-1-carbothioamide
-
(2Z)-2-[1-(4-bromophenyl)-2-[(naphthalen-2-yl)oxy]ethylidene]hydrazine-1-carbothioamide
0.05 mM, 72.1% inhibition, 23°C, pH 5.5
(2Z)-2-[1-(4-bromophenyl)-2-[4-(propan-2-yl)phenoxy]ethylidene]hydrazine-1-carbothioamide
0.05 mM, 49.7% inhibition, 23°C, pH 5.5
(2Z)-2-[2-(3-bromophenoxy)-1-(4-bromophenyl)ethylidene]hydrazine-1-carbothioamide
0.05 mM, 81.3% inhibition, 23°C, pH 5.5
(3-oxido-2,1,3-benzoxadiazol-5-yl)methyl (2E)-2-(4-hydroxybenzylidene)hydrazinecarbimidothioate
-
-
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
(3Z)-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.008 mM
(3Z)-5,7-dimethyl-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.016 mM
(3Z)-5-bromo-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.02 mM
(3Z)-5-chloro-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.021 mM
(3Z)-5-chloro-7-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.0105 mM
(3Z)-5-iodo-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.009 mM
(3Z)-5-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.02-0.05 mM
(3Z)-5-nitro-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.03 mM
(5R)-5-(3,4-difluorophenyl)-3-[2-[(5S)-5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]-5-methylimidazolidine-2,4-dione
in the epimastigote form, the inhibitor does not show trypanocidal effects, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM
(E)-(3,4-dichlorophenyl)(2-phenylcyclopropyl)methanone thiosemicarbazone
-
IC50: 30 nM
(E)-(3,4-dichlorophenyl)(4-methylphenyl)methanone thiosemicarbazone
-
IC50: 40 nM
(E)-cyclohexyl(3,4-dichlorophenyl)methanone thiosemicarbazone
-
IC50: 3000 nM
(E/Z)-N'-(2-chlorobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(2-hhenylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(2-hydroxybenzylidene)-3-methylquinoxaline-2-hydrazide
-
25 microM
(E/Z)-N'-(2-hydroxybenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM
(E/Z)-N'-(3-chlorobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-bromobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-chlorobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-dimethylaminobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-fluorobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-hydroxybenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-isopropylbenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(4-nitrobenzylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(furfurylidene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(pyridin-2-ylmethylene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-(pyridin-4-ylmethylene)-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(E/Z)-N'-benzylidene-3-phenylquinoxaline-2-hydrazide
-
25 microM, inhibition of parasite growth
(m-bromophenyl)ethylketone thiosemicarbazone
-
-
(methanethiolato)[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium (V)
-
-
(p-methoxyphenylthiolato-S)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN] oxorhenium(V)
-
-
1-(2,5-dimethylbenzyl)-5-methyl-1H-indole-2,3-dione
-
IC50: 0.08 mM
1-(3-methoxybenzyl)-5-methyl-1H-indole-2,3-dione
-
IC50: 0.002 mM
1-(biphenyl-2-ylmethyl)-5-methyl-1H-indole-2,3-dione
-
IC50: 0.0028 mM
1-benzyl-5-chloro-1H-indole-2,3-dione
-
IC50: 0.09 mM
1-benzyl-5-iodo-1H-indole-2,3-dione
-
IC50: 0.09 mM
1-[(5R)-3,5-di(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-2-([5-[(5S)-5-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)ethanone
in the epimastigote form, the inhibitor does not show trypanocidal effects, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM
2,2-dimethyl-5-[4-(N-phenyl-N'-phenylethyl)amidinopiperazin-1-ylmethyl]-2H-benzimidazole 1,3-di-N-oxide
-
-
2-(N-1-phenyl-ethylidenehydrazino)-4-trifluoromethylpyrimidine
-
100 microM
2-(N-1-phenyl-ethylidenehydrazino)-5-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-1-phenyl-ethylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-2-hydroxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-hydroxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-hydroxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-methoxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM, 20% inhibitory effect
2-(N-2-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM, 45% inhibitory effect
2-(N-2-methyl-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-2-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM, 45% inhibitory effect
2-(N-4-chloro-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM, 80% inhibitory effect
2-(N-4-chloro-benzylidenehydrazino)-5-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-4-chloro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM, 60% inhibitory effect
2-(N-4-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM, 40% inhibitory effect
2-(N-4-methoxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-4-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-4-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
-
100 microM, 40% inhibitory effect
2-(N-4-methyl-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-4-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-4-nitro-benzylidenehydrazino)-4-trifluoromethylpyrimidine
-
100 microM, 50% inhibitory effect
2-(N-4-nitro-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-4-nitro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
-
100 microM
2-(N-benzylidenehydrazino)-4-trifluoromethylpyrimidine
-
100 microM, 30% inhibitory effect
2-(N-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-(N-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
-
100 microM
2-[(2Z)-2-[(2Z)-(3-bromobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
17% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
7% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-(4-fluorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
3% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
22% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-benzylidenehydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
3% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(2Z)-2-[(2Z)-[1-(3-bromophenyl)ethylidene]hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide
-
22% inhibition at 0.1 mM inhibitor and 140 nM enzyme
2-[(benzofuroxan-5-yl)methylene]-1-(2-hydroxybenzylidene)hydrazine
-
-
2-[(benzofuroxan-5-yl)methylene]-1-(4-hydroxybenzylidene)hydrazine
-
-
2-[(benzofuroxan-5-yl)methylene]-1-(5-bromo-2-hydroxybenzylidene)hydrazine
-
-
3,4,5-trimethoxy-N'-[(E)-(4-nitrophenyl)methylidene]benzohydrazide
-
-
3,4,5-trimethoxy-N'-[(E)-naphthalen-1-ylmethylidene]benzohydrazide
-
-
3-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
10 microM
3-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)-2-oxoheptyl 2,6-bis(trifluoromethyl)benzoate
10 microM
3-(4-[(1S)-1,2-dimethyl-1-[(quinolin-6-ylmethyl)amino]propyl]-1H-1,2,3-triazol-1-yl)-2-oxoheptyl 2,6-dimethylbenzoate
10 microM
3-(4-[(1S)-1-[(1,3-benzothiazol-6-ylmethyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)-1-(2,3,5,6-tetrafluorophenoxy)heptan-2-one
10 microM
3-(4-[(1S)-1-[(1,3-benzothiazol-6-ylmethyl)amino]-1,2-dimethylpropyl]-1H-1,2,3-triazol-1-yl)-2-oxoheptyl 2,6-bis(trifluoromethyl)benzoate
10 microM
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde amidinohydrazone
-
-
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde semicarbazone
-
0.1 mM, 36% of inhibition
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde thiosemicarbazone
-
-
4-amino-6-methyl-3-([2-[(5R)-3-(naphthalen-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]sulfanyl)-1,2,4-triazin-5(4H)-one
shows trypanocidal activity, promising structure in the search for new agents to treat Chagas disease
5-chloro-1-(4-chlorobenzyl)-1H-indole-2,3-dione
-
IC50: 0.006 mM
5-fluoro-1H-indole-2,3-dione
-
IC50: 0.03 mM
5-[4-(N,N'-diphenyl)amidinopiperazin-1-ylmethyl]benzo[1,2-c]1,2,5-oxadiazole N-oxide
-
-
5-[4-(N-benzyl-N'-phenyl)amidinopiperazin-1-ylmethyl]-2,2-dimethyl-2H-benzimidazole 1,3-di-N-oxide
-
-
5-[4-(N-benzyl-N'-phenyl)amidinopiperazin-1-ylmethyl]benzo[1,2-c]1,2,5-oxadiazole N-oxide
-
-
5-[4-(N-furyl-N'-phenyl)amidinopiperazin-1-ylmethyl]-2,2-dimethyl-2H-benzimidazole 1,3-di-N-oxide
-
-
5-[4-(N-furyl-N'-phenyl)amidinopiperazin-1-ylmethyl]benzo[1,2-c]1,2,5-oxadiazole N-oxide
-
-
5-[4-(N-phenyl-N'-phenylethyl)amidinopiperazin-1-yl methyl]benzo[1,2-c]1,2,5-oxadiazole N-oxide
-
-
6-[(E)-2-(phenylsulfonyl)ethenyl]-2,1,3-benzoxadiazole 1-oxide
-
-
aceto[2,6-bis[(butylthio-jS)methyl]phenyl-kappaC]-,(SP-4-3)-palladium(II)
-
-
alpha2-Macroglobulin
40% inhibition at a 1:1 ratio of cruzipain and alpha2-macroglobulin
-
azocasein
substrate inhibition
-
benznidazole
-
presents 80% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to parasite recrudescence in trypomastigotes on the 15th day at 0.01 mM
benzofuroxan-5-carboxaldehyde thiosemicarbazone
-
0.1 mM, 7% of inhibition
benzoyl-Tyr-Ala-chloromethyl ketone
first quantum mechanics/molecular mechanics studies show that benzoyl-Tyr-Ala-chloromethyl ketone is a good candidate for the development of a proper inhibitor of cruzain, which in turn can be used in the treatment of Chagas desease
benzoyl-Tyr-Ala-fluoromethyl ketone
-
benzyl 5-chloro-2,3-dioxoindoline-1-carboxylate
-
IC50: 0.08 mM
benzyloxycarbonyl-Phe-Ala-fluoromethylketone
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
substrate inhibition
biotin-Phe-Ala-fluoromethylketone
-
chagasin mutant delta T31-T32
-
-
-
chagasin mutant P30A
-
-
-
chagasin mutant T31A
-
-
-
chagasin mutant T31A/T32A
-
-
-
chagasin mutant T31S
-
-
-
chagasin mutant T31V
-
-
-
chagasin mutant T31Y
-
-
-
chagasin mutant T32A
-
-
-
chagasin mutant T32E
-
-
-
chagasin mutant T32S
-
-
-
chagasin mutant T32V
-
-
-
chagasin mutant T32Y
-
-
-
chagasin mutant W93A
-
-
-
chagasin mutant Y89F
-
-
-
chagasin mutant Y89S
-
-
-
chloro[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium(V)
-
-
diaceto[2-[(2-pyridinyl-kappaN)methyl]-phenyl-kappaC]Au(III)-,(SP-4-3)
-
-
guanidine hydrochloride
activates at low concentrations but inhibits above 2 M
hydroxymethylnitrofurazone
-
presents 100% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to complete inhibition in trypomastigotes at 0.005 mM
KSCN
activates at low concentrations but inhibits above 1 M
L-trans-epoxysuccinylleucylamido(4-guanidino)butane
methyl (2E)-[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate
-
75% inhibition at 0.1 mM inhibitor and 140 nM enzyme
methyl (2E)-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate
-
71% inhibition at 0.1 mM inhibitor and 140 nM enzyme
methyl (2E)-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate
-
7% inhibition at 0.1 mM inhibitor and 140 nM enzyme
methyl (2E)-[(2Z)-3-methyl-4-oxo-2-[(2Z)-[4-(trifluoromethyl)benzylidene]hydrazinylidene]-1,3-thiazolidin-5-ylidene]ethanoate
-
65% inhibition at 0.1 mM inhibitor and 140 nM enzyme
N'-(furan-2-ylmethyl)-N-phenylpiperazine-1-carboximidamide
-
10% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
N'-benzyl-N-phenylpiperazine-1-carboximidamide
-
5.4% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
N'-[(E)-(2,6-dichlorophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
-
-
N'-[(E)-(4-bromophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
-
-
N,N'-diphenylpiperazine-1-carboximidamide
-
6.3% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
N-(1-cyanocyclopropyl)-Nalpha-(phenylacetyl)-L-phenylalaninamide
pKi: 6.4 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(4-fluorophenyl)acetyl]-L-phenylalaninamide
pKi: 6.3 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(4-hydroxyphenyl)acetyl]-L-phenylalaninamide
pKi: 7.0 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(4-iodophenyl)acetyl]-L-phenylalaninamide
pKi: 7.2 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(4-methylphenyl)acetyl]-L-phenylalaninamide
pKi: 6.6 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[(pyridin-4-yl)acetyl]-L-phenylalaninamide
pKi: 5.9 (-log(Ki/M))
N-(1-cyanocyclopropyl)-Nalpha-[[4-(trifluoromethyl)phenyl]acetyl]-L-phenylalaninamide
pKi: 6.6 (-log(Ki/M))
N-(4-([(2Z)-2-(4-bromophenyl)-2-(2-carbamothioylhydrazinylidene)ethyl]oxy)phenyl)acetamide
0.05 mM, 80.7% inhibition, 23°C, pH 5.5
N-carbobenzoxy-FA-diazomethylketone
inhibition in vivo
N-carbobenzoxy-FF-diazomethylketone
inhibition in vivo
N-carbobenzoxy-FK-acyloxymethylketone
inhibition in vivo
N-carbobenzoxy-VVR-4-nitroanilide
strong substrate inhibition
N-methyl-2-[(2Z)-3-methyl-4-oxo-2-[(2Z)-[4-(trifluoromethyl)benzylidene]hydrazinylidene]-1,3-thiazolidin-5-yl]acetamide
-
27% inhibition at 0.1 mM inhibitor and 140 nM enzyme
N-methyl-2-[(2Z)-4-oxo-2-[(2Z)-(2-sulfanylbenzylidene)hydrazinylidene]-1,3-thiazolidin-5-yl]acetamide
-
27% inhibition at 0.1 mM inhibitor and 140 nM enzyme
N-phenyl benzofuroxan-5-carboxaldehyde thiosemicarbazone
-
-
N-phenyl-N'-(2-phenylethyl)piperazine-1-carboximidamide
-
3.2% inhibition at 0.1 mM, at pH 5.3, temperature not specified in the publication
N-[4-methyl-3-(piperidin-1-ylsulfonyl)phenyl]-4-oxo-4-(3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)butanamide
weak inhibitor shows trypanocidal activity, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM
N4-allyl benzofuroxan-5-carboxaldehyde thiosemicarbazone
-
0.1 mM, 36% of inhibition
Nalpha-benzoyl-N-(1-cyanocyclopropyl)-L-phenylalaninamide
-
Nalpha-benzoyl-N-(2-cyanopropan-2-yl)-L-phenylalaninamide
-
Nalpha-benzoyl-N-(cyanomethyl)-L-phenylalaninamide
-
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-(morpholin-4-ylcarbonyl)-L-phenylalaninamide
-
-
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
Nalpha-[(3-chlorophenyl)acetyl]-N-(1-cyanocyclopropyl)-L-phenylalaninamide
pKi: 6,4 (-log(Ki/M)); pKi: 6.6 (-log(Ki/M))
Nalpha-[(4-bromophenyl)acetyl]-N-(1-cyanocyclopropyl)-L-phenylalaninamide
pKi: 6.9 (-log(Ki/M))
Nalpha-[(4-chlorophenyl)acetyl]-N-(1-cyanocyclopropyl)-L-phenylalaninamide
pKi: 7.2 (-log(Ki/M))
nitrofurazone
-
a 5-nitro-2-furfurylidenesemicarbazone, presents 90% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to parasite recrudescence in trypomastigotes on the 15th day at 0.005 mM
pregnancy zone protein
50% inhibition at a 1:1 ratio of cruzipain and pregnancy zone protein
-
primaquine
-
active against cruzipain, design of selective prodrugs Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine to be cleaved by the enzyme in vivo and selectively inhibiting it, overview
propeptide of cruzipain
-
PCZ, is also a good inhibitor of brucipain from Trypanosoma brucei. The propeptide of cruzipain does not inhibit human cathepsins S, K or B or papain at the tested concentrations, and moderately inhibits human cathepsin V. Human cathepsin F is very efficiently inhibited (Ki of 32 picomol/L)
-
S-methyl thiomethanesulfonate
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
Triton X-100
-
non-specific inhibition in the presence of 0.02% (v/v) Triton X-100
Urea
70% inhibition at 5 M
[(2Z)-2-[(2Z)-(2-fluorobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid
-
6% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid
-
11% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid
-
38% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(2Z)-2-[(2Z)-(4-nitrobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid
-
4% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(2Z)-4-oxo-2-[(2Z)-(thiophen-2-ylmethylidene)hydrazinylidene]-1,3-thiazolidin-5-yl]acetic acid
-
34% inhibition at 0.1 mM inhibitor and 140 nM enzyme
[(S)-1-carboxy-2-phenylethyl]-carbamoyl-L-Arg-L-Val-arginal
-
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
-
-
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
-
-
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
-
-
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
-
-
benzyloxycarbonyl-Phe-Ala-fluoromethylketone
-
benzyloxycarbonyl-Phe-Ala-fluoromethylketone
-
-
chagasin
-
-
-
chagasin
computational protocol allows the identification and prediction of thermodynamics binding energy parameters for cruzipain/chagasin-like heterodimers
-
E-64
-
-
E-64
-
complete inhibition at 0.1 mM inhibitor and 140 nM enzyme
K11777
-
the chemotherapeutical drug targets the major cysteine protease cruzain and disrupts amastigote intracellular development. The mechanism of drug resistance, in primary epimastigotes, is due to secretion of inactive, unprocessed cruzain
L-kininogen
-
-
L-kininogen
high molecular weight kininogen, inhibition decreases 10fold in presence of 0.1 mM heparan sulfate
-
L-trans-epoxysuccinylleucylamido(4-guanidino)butane
-
L-trans-epoxysuccinylleucylamido(4-guanidino)butane
strong inhibitor
leupeptin
-
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
-
-
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
irreversible inhibitor
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
1 microM
additional information
pro-region of the trypanosomal enzyme inhibits the enzyme function, cystatins and kininogens are inhibitors, overview: inhibitors
-
additional information
-
pro-region of the trypanosomal enzyme inhibits the enzyme function, cystatins and kininogens are inhibitors, overview: inhibitors
-
additional information
-
in general immunoglobulin G fractions isolated from rabbits immunised with rabbit apha2-macroglobulin-recombinant catalytic domain of congopain-complexes are the most inhibitory towards the proteolytic activity of congopain. Antibodies produced by rabbits immunised with recombinant catalytic domain of congopain in Freund's adjuvant are generally found to weakly inhibit congopain with a maximum of 40%
-
additional information
-
synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma cruzi, inhibitory potencies and cytotoxic effects, molecular modeling and QSAR studies, overview. No inhibition by (RS)-2-(2-(2-bromobenzylidene)hydrazono)-3-methyl-4-oxo-5-thiazolidine-N-methylacetamide and (Z)-((2-(4-fluorobenzylidene)hydrazono)-3-methyl-5-methoxycarbonylmethylene)thiazolidin-4-one at 0.1 mM
-
additional information
-
synthesis and inhibitory effects against cruzipaon of a series of thirty-three chalcone and seven hydrazide derivatives, overview
-
additional information
-
AM1 semi-empirical molecular modeling studies analysing cruzain inhibitory activity, overview
-
additional information
-
0.01% (v/v) of Triton X-100 does not interfere with enzyme activity
-
additional information
-
not inhibited by CA-074-OMe
-
additional information
the AS2 site as a target for the design of cruzain inhibitors is limited
-
additional information
apolar substituents or halogen atom substitution at the aryl position improved cruzain inhibition and antiparasitic activity in comparison to unsubstituted thiosemicarbazone
-
additional information
-
apolar substituents or halogen atom substitution at the aryl position improved cruzain inhibition and antiparasitic activity in comparison to unsubstituted thiosemicarbazone
-
additional information
nitrile-based inhibitors are efficient inhibitors of cruzain that bind by forming a covalent bond with this enzyme
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.0003 - 0.001
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
0.019
2-aminobenzoyl-ARF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.0013
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
-
37°C, pH 5.5
0.0035
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.0039
2-aminobenzoyl-FRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.000065 - 0.00012
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
0.0036
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Pro-OH
-
37°C, pH 5.5
0.0023
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Trp-OH
-
37°C, pH 5.5
0.00095
2-aminobenzoyl-RRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.001
Ac-Phe-Arg-7-amido-4-methylcoumarin
-
-
0.028 - 0.029
azocasein
-
0.043
benzoyl-His-Arg-7-amido-4-methylcoumarin
pH 6.3, 37°C
-
0.066
benzoyl-PFR-4-nitroanilide
0.0006 - 0.015
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
-
0.0119
benzoyl-RR-aminomethyl coumarin
pH 6.3, 37°C
0.001
benzoyl-Tyr-Arg-7-amido-4-methylcoumarin
-
-
0.038 - 0.163
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
0.0029 - 0.078
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
0.0011
benzyloxycarbonyl-FR-aminomethyl coumarin
pH 6.3, 37°C
0.00054 - 0.0052
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
0.0008 - 0.0032
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
0.0058
epsilon-NH2(capryl)-L-(SBzl)C-7-amido-4-methylcoumarin
-
-
0.0021
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.0025
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.0021
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.011
N-carbobenzoxy-Arg-Arg-2-(4-methoxy)-naphthylamide
-
0.033
N-carbobenzoxy-VVR-4-nitroanilide
0.0044
o-aminobenzoyl-ALRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0021
o-aminobenzoyl-HLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.006
o-aminobenzoyl-KARFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0051
o-aminobenzoyl-KFRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0028
o-aminobenzoyl-KLFFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0114
o-aminobenzoyl-KLGFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0079
o-aminobenzoyl-KLKFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.004 - 0.0051
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
0.0046
o-aminobenzoyl-KLRFFKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0079
o-aminobenzoyl-KLRFPKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0022 - 0.0073
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
0.0078
o-aminobenzoyl-KLRFSPQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0046
o-aminobenzoyl-KLRFSRQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0038
o-aminobenzoyl-KLRLSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0132
o-aminobenzoyl-KLRRSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0117
o-aminobenzoyl-KPRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0032
o-aminobenzoyl-KRRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0036
o-aminobenzoyl-LLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0003
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
recombinant form without C-terminal extension
0.001
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
-
0.000065
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
with 0.06 mM heparan sulfate
0.00012
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
-
0.028
azocasein
pH 4.5, 25°C
-
0.029
azocasein
pH 8.5, 40°C
-
0.066
benzoyl-PFR-4-nitroanilide
-
0.066
benzoyl-PFR-4-nitroanilide
-
-
0.0006
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
recombinant form without C-terminal extension
-
0.0012
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.3, 37°C
-
0.0017
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
-
-
0.01 - 0.015
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
-
-
0.038
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
0.163
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.0029
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
0.0036
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
0.0037
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
0.0041
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
0.0043
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
0.0046
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
0.0066
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
0.011
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
0.012
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.9, 25°C, wild-type enzyme
0.017
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.5, 25°C, wild-type enzyme
0.028
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
0.045
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.056
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
0.068
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
0.078
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
0.00054
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
0.00056
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
0.00061
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
0.00062
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
0.00068
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
0.0007
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
0.00077
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
0.00087
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.6, 25°C, wild-type enzyme
0.00088
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
0.0013
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
0.0016
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.0019
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
0.0025
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
0.0052
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
0.0008
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
truncated enzyme
0.00096
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
-
0.003
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
pH 4.5, 25°C
0.0032
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
pH 8.5, 40°C
0.033
N-carbobenzoxy-VVR-4-nitroanilide
pH 9
0.033
N-carbobenzoxy-VVR-4-nitroanilide
-
pH 9
0.004
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0051
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0022
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.0073
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.0683 - 0.08
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
0.1
2-aminobenzoyl-ARF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
4.2
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
-
37°C, pH 5.5
5.5
2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
2.9
2-aminobenzoyl-FRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.025 - 0.0583
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
1.4
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Pro-OH
-
37°C, pH 5.5
3.4
2-aminobenzoyl-Phe-Arg-(2,4-dinitrophenyl)-epsilon-NH2-lysine-Trp-OH
-
37°C, pH 5.5
0.13
2-aminobenzoyl-RRF-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
-
37°C, pH 5.5
0.172
benzoyl-His-Arg-7-amido-4-methylcoumarin
-
-
0.0433 - 0.193
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
-
0.0783
benzoyl-RR-aminomethyl coumarin
-
0.017 - 0.89
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
0.1 - 8
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
0.158
benzyloxycarbonyl-FR-aminomethyl coumarin
-
13 - 21
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
2.16 - 4.49
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
10.8
epsilon-NH2(capryl)-L-(SBzl)C-7-amido-4-methylcoumarin
-
-
0.14
N-alpha-benzyloxy-carbonyl-L-phenylalanyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.15
N-alpha-benzyloxycarbonyl-L-arginyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.13
N-alpha-benzyloxycarbonyl-L-tyrosyl-L-alanine-(7-amido-4-methylcoumarin)
-
37°C, pH 6.5
0.0805
N-carbobenzoxy-Arg-Arg-2-(4-methoxy)-naphthylamide
-
4.5
o-aminobenzoyl-ALRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
5.6
o-aminobenzoyl-HLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
1.3
o-aminobenzoyl-KARFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
1.9
o-aminobenzoyl-KFRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
2.5
o-aminobenzoyl-KLFFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
5.6
o-aminobenzoyl-KLGFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
14.2
o-aminobenzoyl-KLKFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
8.2 - 15.2
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
9.7
o-aminobenzoyl-KLRFFKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
2.8
o-aminobenzoyl-KLRFPKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
4.3 - 6.9
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
13.9
o-aminobenzoyl-KLRFSPQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
12.5
o-aminobenzoyl-KLRFSRQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
9.1
o-aminobenzoyl-KLRLSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
1.9
o-aminobenzoyl-KLRRSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
0.5
o-aminobenzoyl-KPRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
7.7
o-aminobenzoyl-KRRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
6.7
o-aminobenzoyl-LLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
additional information
additional information
-
0.0683
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
recombinant form without C-terminal extension
0.08
2-aminobenzoic acid-KLRFSKQ-N-(2,4-dinitrophenyl)ethylenediamine
-
0.025
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
-
0.0583
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine
with 0.06 mM heparan sulfate
0.0433
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
-
-
0.055
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
recombinant form without C-terminal extension
-
0.193
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
-
-
0.017
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.89
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
0.1
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
0.27
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
0.4
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
0.7
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
1.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
3.7
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.5, 25°C, wild-type enzyme
5.8
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
5.8
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.9, 25°C, wild-type enzyme
5.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
6.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
6.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
7.1
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
7.2
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
7.4
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
8
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
13
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
13
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
13
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
13.5
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
13.5
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
13.6
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.6, 25°C, wild-type enzyme
14
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
14
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
14
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
14.1
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
15
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
16
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
17
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
21
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
2.16
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
truncated enzyme
4.49
benzyloxycarbonyl-Phe-Arg-aminomethyl coumarin
-
8.2
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
15.2
o-aminobenzoyl-KLRFAKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
4.3
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
6.9
o-aminobenzoyl-KLRFSKQ-N-(2,4-dinitrophenyl)-ethylenediamine
-
-
additional information
additional information
-
-
additional information
additional information
-
-
-
additional information
additional information
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.00008
(1E)-1-(3,4-dichlorophenyl)-2-phenylethan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 80 nM
0.00004
(1E)-1-(3,4-dichlorophenyl)-3-phenylpropan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 40 nM
0.000019
(1E)-1-(3,4-dichlorophenyl)pentan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 19 nM
0.00003
(1E)-1-(3,4-dichlorophenyl)propan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 30 nM
0.00031
(1E)-1-(3-bromophenyl)propan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 310 nM
0.00003
(1E,2E)-1-(3,4-dichlorophenyl)-3-phenylprop-2-en-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 30 nM
0.00003
(1Z)-1-(3,4-dichlorophenyl)-2-phenoxyethan-1-one thiosemicarbazone
Trypanosoma cruzi
-
IC50: 30 nM
0.000015
(2(1H)-pyridinethionato-kappaS2)[2,6-bis[(mercapto-KappaS)methyl]pyridine-kappaN1] oxorhenium(V)
Trypanosoma cruzi
-
-
0.1
(2E)-1,3-bis(2,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1,3-di(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(1,3-benzodioxol-5-yl)-3-(1-naphthyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.02
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2,6-dichlorophenyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2-chlorophenyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-1-(1,3-benzodioxol-5-yl)-3-(3-methoxy-4-phenoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.046
(2E)-1-(1,3-benzodioxol-5-yl)-3-(4-buthoxyphenyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.023
(2E)-1-(1,3-benzodioxol-5-yl)-3-(5-methylfuran-2-yl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.022
(2E)-1-(1,3-benzodioxol-5-yl)-3-(thiophen-2-yl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.048
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.1
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(thiophen-2-yl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.037
(2E)-1-(2'-hydroxy,3'-bromo,4',6'-dimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.082
(2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-buthoxyphenyl)-2-propen-1- one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.1
(2E)-1-(2,4-dimethoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(2-naphthyl)-3-(2,6-dimethoxyphenyl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(2-naphthyl)-3-(5-methylfuran-2-yl)-2-propen-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.045
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.02
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3-methoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.035
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.03
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methylphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-phenylprop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.025
(2E)-1-(4-hydroxy-1,3-benzodioxol-5-yl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.0006
(2E)-2-[1-([1,1'-biphenyl]-4-yl)-2-(4-bromophenoxy)ethylidene]hydrazine-1-carbothioamide
Trypanosoma cruzi
23°C, pH 5.5
0.1
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.02
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-3-(1,3-benzodioxol-5-yl)-1-(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.1
(2E)-3-(3-methoxyphenyl)-1-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.03
(2E)-3-(4-bromophenyl)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-3-(4-fluorophenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05 - 0.06
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
0.037
(2E)-3-[4-(benzyloxy)-3-methoxyphenyl]-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-N'-(3'-bromo-4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.047
(2E)-N'-(4'-buthoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.05
(2E)-N'-(4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.000008
(2Z)-2-[1-(4-bromophenyl)-2-(3,4-dichlorophenoxy)ethylidene]hydrazine-1-carbothioamide
Trypanosoma cruzi
23°C, pH 5.5
0.00007
(2Z)-2-[1-(4-bromophenyl)-2-(3-chloro-4-fluorophenoxy)ethylidene]hydrazine-1-carbothioamide
Trypanosoma cruzi
23°C, pH 5.5
0.0004
(2Z)-2-[1-(4-bromophenyl)-2-(4-fluorophenoxy)ethylidene]hydrazine-1-carbothioamide
Trypanosoma cruzi
23°C, pH 5.5
0.01
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
0.0002 - 0.006
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
0.008
(3Z)-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.008 mM
0.016
(3Z)-5,7-dimethyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.016 mM
0.02
(3Z)-5-bromo-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.02 mM
0.021
(3Z)-5-chloro-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.021 mM
0.0105
(3Z)-5-chloro-7-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.0105 mM
0.009
(3Z)-5-iodo-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.009 mM
0.02 - 0.05
(3Z)-5-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.02-0.05 mM
0.03
(3Z)-5-nitro-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.03 mM
0.05035
(5R)-5-(3,4-difluorophenyl)-3-[2-[(5S)-5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]-5-methylimidazolidine-2,4-dione
Trypanosoma cruzi
23°C, pH 6.8
0.00003
(E)-(3,4-dichlorophenyl)(2-phenylcyclopropyl)methanone thiosemicarbazone
Trypanosoma cruzi
-
IC50: 30 nM
0.00004
(E)-(3,4-dichlorophenyl)(4-methylphenyl)methanone thiosemicarbazone
Trypanosoma cruzi
-
IC50: 40 nM
0.003
(E)-cyclohexyl(3,4-dichlorophenyl)methanone thiosemicarbazone
Trypanosoma cruzi
-
IC50: 3000 nM
0.02
(E/Z)-N'-(2-hydroxybenzylidene)-3-methylquinoxaline-2-hydrazide
Trypanosoma cruzi
-
-
0.0159
(E/Z)-N'-(2-hydroxybenzylidene)-3-phenylquinoxaline-2-hydrazide
Trypanosoma cruzi
-
-
0.005
(methanethiolato)[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium (V)
Trypanosoma cruzi
-
-
0.00035
(p-methoxyphenylthiolato-S)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN] oxorhenium(V)
Trypanosoma cruzi
-
-
0.08
1-(2,5-dimethylbenzyl)-5-methyl-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.08 mM
0.002
1-(3-methoxybenzyl)-5-methyl-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.002 mM
0.0028
1-(biphenyl-2-ylmethyl)-5-methyl-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.0028 mM
0.09
1-benzyl-5-chloro-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.09 mM
0.09
1-benzyl-5-iodo-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.09 mM
0.08437
1-[(5R)-3,5-di(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-2-([5-[(5S)-5-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)ethanone
Trypanosoma cruzi
23°C, pH 6.6
0.15
2-(N-2-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.15 mM
0.1
2-(N-2-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.1 mM
0.1
2-(N-2-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.1 mM
0.085
2-(N-4-chloro-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
-
0.1
2-(N-4-chloro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
Trypanosoma cruzi
-
about 0.1 mM
0.1
2-(N-4-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.1 mM
0.1
2-(N-4-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
Trypanosoma cruzi
-
above 0.1 mM
0.1
2-(N-4-nitro-benzylidenehydrazino)-4-trifluoromethylpyrimidine
Trypanosoma cruzi
-
about 0.1 mM
0.15
2-(N-benzylidenehydrazino)-4-trifluoromethylpyrimidine
Trypanosoma cruzi
-
above 0.15 mM
0.068
2-[(benzofuroxan-5-yl)methylene]-1-(2-hydroxybenzylidene)hydrazine
Trypanosoma cruzi
-
-
0.1
2-[(benzofuroxan-5-yl)methylene]-1-(4-hydroxybenzylidene)hydrazine
Trypanosoma cruzi
-
-
0.073
2-[(benzofuroxan-5-yl)methylene]-1-(5-bromo-2-hydroxybenzylidene)hydrazine
Trypanosoma cruzi
-
-
0.06
3,4,5-trimethoxy-N'-[(E)-(4-nitrophenyl)methylidene]benzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.04
3,4,5-trimethoxy-N'-[(E)-naphthalen-1-ylmethylidene]benzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.032
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde amidinohydrazone
Trypanosoma cruzi
-
-
0.1
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde semicarbazone
Trypanosoma cruzi
-
above 0.1 mM
0.043
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde thiosemicarbazone
Trypanosoma cruzi
-
-
0.05623
4-amino-6-methyl-3-([2-[(5R)-3-(naphthalen-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]sulfanyl)-1,2,4-triazin-5(4H)-one
Trypanosoma cruzi
23°C, pH 6.7
0.006
5-chloro-1-(4-chlorobenzyl)-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.006 mM
0.03
5-fluoro-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.03 mM
0.00007
aceto[2,6-bis[(butylthio-jS)methyl]phenyl-kappaC]-,(SP-4-3)-palladium(II)
Trypanosoma cruzi
-
-
0.1
benzofuroxan-5-carboxaldehyde thiosemicarbazone
Trypanosoma cruzi
-
above 0.1 mM
0.08
benzyl 5-chloro-2,3-dioxoindoline-1-carboxylate
Trypanosoma cruzi
-
IC50: 0.08 mM
0.00004
chloro[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium(V)
Trypanosoma cruzi
-
-
0.0007
diaceto[2-[(2-pyridinyl-kappaN)methyl]-phenyl-kappaC]Au(III)-,(SP-4-3)
Trypanosoma cruzi
-
-
0.0106
hydroxymethylnitrofurazone
Trypanosoma cruzi
-
pH 6.5, 37°C
0.05
N'-[(E)-(2,6-dichlorophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.055
N'-[(E)-(4-bromophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
Trypanosoma cruzi
-
pH 6.5, 22°C
0.078
N-phenyl benzofuroxan-5-carboxaldehyde thiosemicarbazone
Trypanosoma cruzi
-
-
1.41
N-[4-methyl-3-(piperidin-1-ylsulfonyl)phenyl]-4-oxo-4-(3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)butanamide
Trypanosoma cruzi
23°C, pH 6.5
0.1
N4-allyl benzofuroxan-5-carboxaldehyde thiosemicarbazone
Trypanosoma cruzi
-
above 0.1 mM
0.000004 - 0.0001
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
0.0077
nifurtimox
Trypanosoma cruzi
-
-
0.0228
nitrofurazone
Trypanosoma cruzi
-
pH 6.5, 37°C
0.05
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.06
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
Trypanosoma cruzi
-
pH 6.5, 22°C
0.01
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
Trypanosoma brucei rhodesiense
-
-
0.01
(3S,5R,10R)-N-benzyl-3-(2-methylpropyl)-2-oxo-10-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazecane-5-carboxamide
Trypanosoma cruzi
-
above 0.01 mM
0.0002
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
Trypanosoma cruzi
-
-
0.006
(3S,5R,11R)-N-benzyl-3-(2-methylpropyl)-2-oxo-11-[(E)-2-(phenylsulfonyl)ethenyl]-1,4-diazacycloundecane-5-carboxamide
Trypanosoma brucei rhodesiense
-
-
0.000004
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
Trypanosoma cruzi
-
-
0.0001
Nalpha-[(2R,3E)-2-benzyl-4-(phenylsulfonyl)but-3-enoyl]-N-[(4-methylpiperazin-1-yl)carbonyl]-L-phenylalaninamide
Trypanosoma brucei rhodesiense
-
-
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Alvarez, V.; Parussini, F.; Aslund, L.; Cazzulo, J.J.
Expression in insect cells of active mature cruzipain from Trypanosoma cruzi, containing its C-terminal domain
Protein Expr. Purif.
26
467-475
2002
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
Alves, L.C.; Melo, R.L.; Cezari, M.H.S.; Sanderson, S.J.; Mottram, J.C.; Coombs, G.H.; Juliano, L.; Juliano, M.A.
Analysis of the S2 subsite specificities of the recombinant cysteine proteinases CPB of Leishmania mexicana, and cruzain of Trypanosoma cruzi, using fluorescent substrates containing non-natural basic amino acids
Mol. Biochem. Parasitol.
117
137-143
2001
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
Cazzulo, J.J.; Bravo, M.; Raimond, A.; Engstroem, U.; Lindeberg, G.; Hellman, U.
Hydrolysis of synthetic peptides by cruzipain, the major cysteine proteinase from Trypanosoma cruzi, provides evidence for self-processing and the possibility of more specific substrates for the enzyme
Cell. Mol. Biol.
42
691-696
1996
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
Cazzulo, J.J.; Cazzulo Franke, M.C.; Martinez, J.; Franke de Cazzulo, B.M.
Some kinetic properties of a cysteine proteinase (cruzipain) from Trypanosoma cruzi
Biochim. Biophys. Acta
1037
186-191
1990
Trypanosoma cruzi (Q598P5)
brenda
Cazzulo, J.J.; Stoka, V.; Turk, V.
Cruzipain, the major cysteine proteinase from the protozoan parasite Trypanosoma cruzi
Biol. Chem.
378
1-10
1997
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
Del Nery, E.; Juliano, M.A.; Meldal, M.; Svendsen, I.; Scharfstein, J.; Walmsley, A.; Juliano, L.
Characterization of the substrate specificity of the major cysteine protease (cruzipain) from Trypanosoma cruzi using a portion-mixing combinatorial library and fluorogenic peptides
Biochem. J.
323
427-433
1997
Trypanosoma cruzi (Q598P5)
-
brenda
Eakin, A.E.; McGrath, M.E.; McKerrow, J.H.; Fletterick, R.J.; Craik, C.S.
Production of crystallizable cruzain, the major cysteine protease from Trypanosoma cruzi
J. Biol. Chem.
268
6115-6118
1993
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
Gillmor, S.A.; Craik, C.S.; Fletterick, R.J.
Structural determinants of specificity in the cysteine protease cruzain
Protein Sci.
6
1603-1611
1997
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
Judice, W.A.; Cezari, M.H.; Lima, A.P.; Scharfstein, J.; Chagas, J.R.; Tersariol, I.L.; Juliano, M.A.; Juliano, L.
Comparison of the specificity, stability and individual rate constants with respective activation parameters for the peptidase activity of cruzipain and its recombinant form, cruzain, from Trypanosoma cruzi
Eur. J. Biochem.
268
6578-6586
2001
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
Lalmanach, G.; Boulange, A.; Serveau, C.; Lecaille, F.; Scharfstein, J.; Gauthier, F.; Authie, E.
Congopain from Trypanosoma congolense: drug target and vaccine candidate
Biol. Chem.
383
739-749
2002
Trypanosoma congolense (Q26909), Trypanosoma congolense
brenda
Lima, A.P.C.A.; Almeida, P.C.; Tersariol, I.L.S.; Schmitz, V.; Schmaier, A.H.; Juliano, L.; Hirata, I.Y.; Muller-Esterl, W.; Chagas, J.R.; Scharfstein, J.
Heparan sulfate modulates kinin release by Trypanosoma cruzi through the activity of cruzipain
J. Biol. Chem.
277
5875-5881
2002
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
McGrath, M.E.; Eakin, A.E.; Engel, J.C.; McKerrow, J.H.; Craik, C.C.; Fletterick, R.J.
The crystal structure of cruzain: a therapeutic target for Chagas' disease
J. Mol. Biol.
247
251-259
1995
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
brenda
Ramos, A.M.; Duschak, V.G.; Gerez de Burgos, N.M.; Barboza, M.; Remedi, M.S.; Vides, M.A.; Chiabrando, G.A.
Trypanosoma cruzi: cruzipain and membrane-bound cysteine proteinase isoform(s) interacts with human alpha2-macroglobulin and pregnancy zone protein
Exp. Parasitol.
100
121-130
2002
Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
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Salvati, L.; Mattu, M.; Polticelli, F.; Tiberi, F.; Gradoni, L.; Venturini, G.; Bolognesi, M.; Ascenzi, P.
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
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Trypanosoma cruzi (Q598P5), Trypanosoma cruzi
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Aoki, M.P.; Guinazu, N.L.; Pellegrini, A.V.; Gotoh, T.; Masih, D.T.; Gea, S.
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Trypanosoma cruzi
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Chiyanzu, I.; Hansell, E.; Gut, J.; Rosenthal, P.J.; McKerrow, J.H.; Chibale, K.
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Fujii, N.; Mallari, J.P.; Hansell, E.J.; Mackey, Z.; Doyle, P.; Zhou, Y.M.; Gut, J.; Rosenthal, P.J.; McKerrow, J.H.; Guy, R.K.
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Judice, W.A.; Puzer, L.; Cotrin, S.S.; Carmona, A.K.; Coombs, G.H.; Juliano, L.; Juliano, M.A.
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Duschak, V.G.; Barboza, M.; Couto, A.S.
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Barboza, M.; Duschak, V.G.; Fukuyama, Y.; Nonami, H.; Erra-Balsells, R.; Cazzulo, J.J.; Couto, A.S.
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Barboza, M.; Duschak, V.G.; Cazzulo, J.J.; de Lederkremer, R.M.; Couto, A.S.
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Berasain, P.; Carmona, C.; Frangione, B.; Cazzulo, J.J.; Goni, F.
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Stempin, C.C.; Garrido, V.V.; Dulgerian, L.R.; Cerban, F.M.
Cruzipain and SP600125 induce p38 activation, alter NO/arginase balance and favor the survival of Trypanosoma cruzi in macrophages
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Trypanosoma cruzi
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Reis, F.C.; Costa, T.F.; Sulea, T.; Mezzetti, A.; Scharfstein, J.; Broemme, D.; Menard, R.; Lima, A.P.
The propeptide of cruzipain--a potent selective inhibitor of the trypanosomal enzymes cruzipain and brucipain, and of the human enzyme cathepsin F
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dos Reis, F.C.; Judice, W.A.; Juliano, M.A.; Juliano, L.; Scharfstein, J.; Lima, A.P.
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Trypanosoma cruzi
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Scharfstein, J.; Monteiro, A.C.; Schmitz, V.; Svensjoe, E.
Angiotensin-converting enzyme limits inflammation elicited by Trypanosoma cruzi cysteine proteases: a peripheral mechanism regulating adaptive immunity via the innate kinin pathway
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Trypanosoma cruzi
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Chen, Y.T.; Lira, R.; Hansell, E.; McKerrow, J.H.; Roush, W.R.
Synthesis of macrocyclic trypanosomal cysteine protease inhibitors
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Trypanosoma brucei rhodesiense, Trypanosoma cruzi
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Zanatta, N.; Amaral, S.S.; Dos Santos, J.M.; de Mello, D.L.; Fernandes, L.d.a..S.; Bonacorso, H.G.; Martins, M.A.; Andricopulo, A.D.; Borchhardt, D.M.
Convergent synthesis and cruzain inhibitory activity of novel 2-(N-benzylidenehydrazino)-4-trifluoromethyl-pyrimidines
Bioorg. Med. Chem.
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Trypanosoma cruzi
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Porcal, W.; Hernandez, P.; Boiani, L.; Boiani, M.; Ferreira, A.; Chidichimo, A.; Cazzulo, J.J.; Olea-Azar, C.; Gonzalez, M.; Cerecetto, H.
New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle
Bioorg. Med. Chem.
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Trypanosoma cruzi, Trypanosoma cruzi Tulahuen 2
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Romeiro, N.C.; Aguirre, G.; Hernandez, P.; Gonzalez, M.; Cerecetto, H.; Aldana, I.; Perez-Silanes, S.; Monge, A.; Barreiro, E.J.; Lima, L.M.
Synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones, designed as cruzain inhibitors candidates
Bioorg. Med. Chem.
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Trypanosoma cruzi, Trypanosoma cruzi Tulahuen 2
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Elias, C.G.; Pereira, F.M.; Dias, F.A.; Silva, T.L.; Lopes, A.H.; dAvila-Levy, C.M.; Branquinha, M.H.; Santos, A.L.
Cysteine peptidases in the tomato trypanosomatid Phytomonas serpens: influence of growth conditions, similarities with cruzipain and secretion to the extracellular environment
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Trypanosoma cruzi, Trypanosoma cruzi Dm28c
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dos Reis, F.C.; Smith, B.O.; Santos, C.C.; Costa, T.F.; Scharfstein, J.; Coombs, G.H.; Mottram, J.C.; Lima, A.P.
The role of conserved residues of chagasin in the inhibition of cysteine peptidases
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Trypanosoma cruzi
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SantAnna, C.; Parussini, F.; Lourenco, D.; de Souza, W.; Cazzulo, J.J.; Cunha-e-Silva, N.L.
All Trypanosoma cruzi developmental forms present lysosome-related organelles
Histochem. Cell Biol.
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Trypanosoma cruzi, Trypanosoma cruzi Y
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Acosta, D.M.; Arnaiz, M.R.; Esteva, M.I.; Barboza, M.; Stivale, D.; Orlando, U.D.; Torres, S.; Laucella, S.A.; Couto, A.S.; Duschak, V.G.
Sulfates are main targets of immune responses to cruzipain and are involved in heart damage in BALB/c immunized mice
Int. Immunol.
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Trypanosoma cruzi, Trypanosoma cruzi Tulahuen 2
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Brak, K.; Doyle, P.S.; McKerrow, J.H.; Ellman, J.A.
Identification of a new class of nonpeptidic inhibitors of cruzain
J. Am. Chem. Soc.
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Trypanosoma cruzi (P25779), Trypanosoma cruzi
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Fricker, S.P.; Mosi, R.M.; Cameron, B.R.; Baird, I.; Zhu, Y.; Anastassov, V.; Cox, J.; Doyle, P.S.; Hansell, E.; Lau, G.; Langille, J.; Olsen, M.; Qin, L.; Skerlj, R.; Wong, R.S.; Santucci, Z.; McKerrow, J.H.
Metal compounds for the treatment of parasitic diseases
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Fampa, P.; Lisboa, C.V.; Jansen, A.M.; Santos, A.L.; Ramirez, M.I.
Protease expression analysis in recently field-isolated strains of Trypanosoma cruzi: a heterogeneous profile of cysteine protease activities between TC I and TC II major phylogenetic groups
Parasitology
135
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2008
Trypanosoma cruzi
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Pereira, F.M.; Elias, C.G.; dAvila-Levy, C.M.; Branquinha, M.H.; Santos, A.L.
Cysteine peptidases in Herpetomonas samuelpessoai are modulated by temperature and dimethylsulfoxide-triggered differentiation
Parasitology
136
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2009
Trypanosoma cruzi, Trypanosoma cruzi Dm28c
brenda
Abdulla, M.H.; OBrien, T.; Mackey, Z.B.; Sajid, M.; Grab, D.J.; McKerrow, J.H.
RNA interference of Trypanosoma brucei cathepsin B and L affects disease progression in a mouse model
PLoS Negl. Trop. Dis.
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2008
Trypanosoma brucei
brenda
Cazorla, S.I.; Frank, F.M.; Becker, P.D.; Corral, R.S.; Guzman, C.A.; Malchiodi, E.L.
Prime-boost immunization with cruzipain co-administered with MALP-2 triggers a protective immune response able to decrease parasite burden and tissue injury in an experimental Trypanosoma cruzi infection model
Vaccine
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2008
Trypanosoma cruzi, Trypanosoma cruzi RA
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Huson, L.E.; Authie, E.; Boulange, A.F.; Goldring, J.P.; Coetzer, T.H.
Modulation of the immunogenicity of the Trypanosoma congolense cysteine protease, congopain, through complexation with alpha2-macroglobulin
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Trypanosoma congolense
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Ortiz, P.A.; Maia da Silva, F.; Cortez, A.P.; Lima, L.; Campaner, M.; Pral, E.M.; Alfieri, S.C.; Teixeira, M.M.
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Trypanosoma rangeli (D0QZL7), Trypanosoma rangeli (D0QZL8), Trypanosoma rangeli (D0QZM0), Trypanosoma rangeli (D0QZM2), Trypanosoma rangeli (D0QZM5), Trypanosoma rangeli (D0QZM6), Trypanosoma rangeli (D0QZM9)
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Cortez, A.; Rodrigues, A.; Garcia, H.; Neves, L.; Batista, J.; Bengaly, Z.; Paiva, F.; Teixeira, M.
Cathepsin L-like genes of Trypanosoma vivax from Africa and South America - characterization, relationships and diagnostic implications
Mol. Cell. Probes
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Trypanosoma vivax (C0J3Y8), Trypanosoma vivax (C0J3Z1)
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Pizzo, C.; Saiz, C.; Talevi, A.; Gavernet, L.; Palestro, P.; Bellera, C.; Blanch, L.B.; Benitez, D.; Cazzulo, J.J.; Chidichimo, A.; Wipf, P.; Mahler, S.G.
Synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma cruzi
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2011
Trypanosoma cruzi
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Borchhardt, D.; Mascarello, A.; Chiaradia, L.; Nunes, R.; Oliva, G.; Yunes, R.; Andricopulo, A.
Biochemical evaluation of a series of synthetic chalcone and hydrazide derivatives as novel inhibitors of cruzain from Trypanosoma cruzi
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Trypanosoma cruzi
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Trossini, G.; Malvezzi, A.; Amaral, A.; Rangel-Yagui, C.; Izidoro, M.; Cezari, M.; Juliano, L.; Chin, C.; Menezes, C.; Ferreira, E.
Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: Investigation of a new target in Trypanosoma cruzi
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Trypanosoma cruzi
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Trossini, G.; Chin, C.; de Souza Menezes, C.; Ferreira, E.
Molecular modeling suggests cruzain specificity for peptide primaquine prodrugs
Lett. Drug Des. Discov.
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528-533
2010
Trypanosoma cruzi
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Acosta, D.M.; Soprano, L.L.; Ferrero, M.; Landoni, M.; Esteva, M.I.; Couto, A.S.; Duschak, V.G.
A striking common O-linked N-acetylglucosaminyl moiety between cruzipain and myosin
Parasite Immunol.
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Trypanosoma cruzi
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Doyle, P.S.; Zhou, Y.M.; Hsieh, I.; Greenbaum, D.C.; McKerrow, J.H.; Engel, J.C.
The Trypanosoma cruzi protease cruzain mediates immune evasion
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Trypanosoma cruzi
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Merlino, A.; Benitez, D.; Campillo, N.; Pez, J.; Tinoco, L.; Gonzlez, M.; Cerecetto, H.
Amidines bearing benzofuroxan or benzimidazole 1,3-dioxide core scaffolds as Trypanosoma cruzi-inhibitors: Structural basis for their interactions with cruzipain
MedChemComm
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90-101
2012
Trypanosoma cruzi
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Uehara, L.A.; Moreira, O.C.; Oliveira, A.C.; Azambuja, P.; Lima, A.P.; Britto, C.; dos Santos, A.L.; Branquinha, M.H.; dAvila-Levy, C.M.
Cruzipain promotes Trypanosoma cruzi adhesion to Rhodnius prolixus midgut
PLoS Negl. Trop. Dis.
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2012
Trypanosoma cruzi, Trypanosoma cruzi Dm28c
brenda
Barbosa da Silva, E.; Dall, E.; Briza, P.; Brandstetter, H.; Ferreira, R.S.
Cruzain structures apocruzain and cruzain bound to S-methyl thiomethanesulfonate and implications for drug design
Acta Crystallogr. Sect. F
75
419-427
2019
Trypanosoma cruzi (P25779), Trypanosoma cruzi
brenda
Arafet, K.; Ferrer, S.; Moliner, V.
First quantum mechanics/molecular mechanics studies of the inhibition mechanism of cruzain by peptidyl halomethyl ketones
Biochemistry
54
3381-3391
2015
Trypanosoma cruzi (P25779), Trypanosoma cruzi
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Zhai, X.; Meek, T.D.
Catalytic mechanism of cruzain from Trypanosoma cruzi as determined from solvent kinetic isotope effects of steady-state and pre-steady-state kinetics
Biochemistry
57
3176-3190
2018
Trypanosoma cruzi (P25779), Trypanosoma cruzi
brenda
Cianni, L.; Sartori, G.; Rosini, F.; De Vita, D.; Pires, G.; Lopes, B.R.; Leitao, A.; Burtoloso, A.C.B.; Montanari, C.A.
Leveraging the cruzain S3 subsite to increase affinity for reversible covalent inhibitors
Bioorg. Chem.
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Trypanosoma cruzi (P25779), Trypanosoma cruzi
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Fabian, L.; Martini, M.F.; Sarduy, E.S.; Estrin, D.A.; Moglioni, A.G.
Evaluation of quinoxaline compounds as ligands of a site adjacent to S2 (AS2) of cruzain
Bioorg. Med. Chem. Lett.
29
2197-2202
2019
Trypanosoma cruzi (P25779)
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Espindola, J.W.; Cardoso, M.V.; Filho, G.B.; Oliveira E Silva, D.A.; Moreira, D.R.; Bastos, T.M.; Simone, C.A.; Soares, M.B.; Villela, F.S.; Ferreira, R.S.; Castro, M.C.; Pereira, V.R.; Murta, S.M.; Sales Junior, P.A.; Romanha, A.J.; Leite, A.C.
Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain
Eur. J. Med. Chem.
101
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2015
Trypanosoma cruzi (P25779), Trypanosoma cruzi
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Reyes-Espinosa, F.; Juarez-Saldivar, A.; Palos, I.; Herrera-Mayorga, V.; Garcia-Perez, C.; Rivera, G.
In silico analysis of homologous heterodimers of cruzipain-chagasin from structural models built by homology
Int. J. Mol. Sci.
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2019
Trypanosoma cruzi (P25779)
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Herrera-Mayorga, V.; Lara-Ramirez, E.E.; Chacon-Vargas, K.F.; Aguirre-Alvarado, C.; Rodriguez-Paez, L.; Alcantara-Farfan, V.; Cordero-Martinez, J.; Nogueda-Torres, B.; Reyes-Espinosa, F.; Bocanegra-Garcia, V.; Rivera, G.
Structure-based virtual screening and in vitro evaluation of new Trypanosoma cruzi cruzain inhibitors
Int. J. Mol. Sci.
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2019
Trypanosoma cruzi (P25779), Trypanosoma cruzi, Trypanosoma cruzi INC-5 (P25779)
brenda
Dos Santos, A.M.; Cianni, L.; De Vita, D.; Rosini, F.; Leitao, A.; Laughton, C.A.; Lameira, J.; Montanari, C.A.
Experimental study and computational modelling of cruzain cysteine protease inhibition by dipeptidyl nitriles
Phys. Chem. Chem. Phys.
20
24317-24328
2018
Trypanosoma cruzi (P25779)
brenda
Ferrao, P.M.; dAvila-Levy, C.M.; Araujo-Jorge, T.C.; Degrave, W.M.; Goncalves, A.d.a. .S.; Garzoni, L.R.; Lima, A.P.; Feige, J.J.; Bailly, S.; Mendonca-Lima, L.; Waghabi, M.C.
Cruzipain activates latent TGF-beta from host cells during T. cruzi invasion
PLoS ONE
10
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2015
Trypanosoma cruzi (P25779), Trypanosoma cruzi
brenda