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Information on EC 3.4.22.51 - cruzipain
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3.4.22.51 cruzipainSpecify your search results
Word Map
- 3.4.22.51
- cathepsins
- brucei
-
protozoan
- trypomastigotes
- epimastigotes
-
trypanocidal
- trypanosomiasis
-
trypanosomal
- proteinases
- amastigote
- papain
- benznidazole
-
papain-like
-
anti-trypanosoma
-
vinyl
-
antiparasitic
- rhodesiense
- thiosemicarbazone
- cystatins
-
latin
- nifurtimox
-
nitril
- trypanothione
-
antichagasic
- chagasin
-
warhead
-
cruzi-infected
-
metacyclogenesis
-
tulahuen
- trans-sialidase
-
reservosomes
- falcipain-2
- bauhinia
- medicine
- kininogens
- congolense
-
metacyclic
- drug development
- pharmacology
- molecular biology
-
n-acylhydrazones
- z-phe-arg-amc
- semicarbazone
The enzyme appears in viruses and cellular organisms
Synonyms
brucipain, cathepsin L-like cysteine protease, cathepsin L-like protease, CatL-like protease, congopain, CP, cruzain, cruzipain, cruzipain 2, CTE-truncated recombinant protease, 
more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
brucipain
cathepsin L-like cysteine protease
CatL-like protease
congopain
CP
cruzain
cruzipain
CZP
evansain
-
-
-
-
GP57/51
-
-
-
-
major cysteine proteinase
proteinase, Trypanosoma congolese cysteine
-
-
-
-
proteinase, Trypanosoma cruzi cysteine
-
-
-
-
proteinase, Trypanosoma cysteine
-
-
-
-
trypanopain
-
-
-
-
Trypanosoma congolese cysteine protease
-
-
-
-
Trypanosoma cruzi cysteine protease
-
-
-
-
Trypanosoma cysteine protease
-
-
-
-
CatL-like protease
-
congopain
-
-
-
-
cruzain
-
-
-
-
cruzipain
-
-
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
broad endopeptidase specificity similar to that of cathepsin L
-
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
hydrolysis of peptide bond
-
-
-
-
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CAS REGISTRY NUMBER
COMMENTARY
102227-51-0
-
141588-22-9
-
84399-99-5
-
90371-53-2
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(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-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-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-Phe-Arg-4-methylcoumarin-7-amide + H2O
?
fluorogenic substrates based on the peptide benzoyl-Phe-Arg-4-methylcoumarin-7-amide
-
-
?
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
-
-
?
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-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-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
-
-
?
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
-
-
-
-
?
human IgG + H2O
?
-
specific cleavage sites on human IgG subclasses by cruzipain
-
-
?
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-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-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
-
-
?
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-amino-4-methylcoumarin
-
-
-
-
?
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
-
-
-
?
2-aminobenzoyl-LGMISLMKRPQ-N-(2,4-dinitrophenyl)ethylenediamine + H2O
?
Abz-LGMISLMKRPQ-EDDnp
-
-
?
benzoyl-FR-4-methylcoumarin 7-amide + H2O
?
fluorigenic substrates based on this peptide, substitution of Phe results in less susceptible substrates
-
-
?
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-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
Trypanosoma cruzi INC-5
-
-
-
?
Gelatin + H2O
?
-
-
-
?
Immunoglobulin G1 + H2O
?
cleaves specifically at the hinge region
-
-
?
Immunoglobulin G3 + H2O
?
cleaves specifically at the hinge region
-
-
?
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
-
-
?
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
?
-
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
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
Gelatin + H2O
?
-
-
-
?
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
?
-
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
?
-
-
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
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
NaCl
Km increases up to 400 mM, then decreases and remains constant at 50-60% up to 1 M, kcat maximum at 300 mM
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(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,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-(1,3-benzodioxol-5-yl)-3-(3-methoxy-4-phenoxyphenyl)prop-2-en-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-(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-(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-(4-bromophenyl)-1-(3a,7a-dihydro-1,3-benzodioxol-5-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'-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)-5-chloro-7-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
-
IC50: 0.0105 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
(methanethiolato)[2,2'-(thio-kappaS)bis[ethanethiolato-kappaS]] oxorhenium (V)
-
-
(p-methoxyphenylthiolato-S)[2,6-bis[(mercapto-kappaS)methyl]pyridine-kappaN] oxorhenium(V)
-
-
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-(5-bromo-2-hydroxybenzylidene)hydrazine
-
-
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 semicarbazone
-
0.1 mM, 36% of inhibition
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-[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
-
-
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
-
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
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
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 inhibtiion in trypomastigotes at 0.005 mM
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,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-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-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-[(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)
-
Triton X-100
-
non-specific inhibition in the presence of 0.02% (v/v) Triton X-100
[(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
(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
-
-
chagasin
computational protocol allows the identification and prediction of thermodynamics binding energy parameters for cruzipain/chagasin-like heterodimers
-
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
high molecular weight kininogen, inhibition decreases 10fold in presence of 0.1 mM heparan sulfate
-
L-trans-epoxysuccinylleucylamido(4-guanidino)butane
strong inhibitor
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
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
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.
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
guanidine hydrochloride
activates at low concentrations but inhibits above 2 M
Urea
maximal at 2 M with natural substrates, no activation with synthetic substrates
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
0.0036
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
0.0021
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
0.0003
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
-
0.0006
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
recombinant form without C-terminal extension
-
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
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
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
0.14
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
0.0683
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
0.055
benzoyl-Phe-Arg-7-amido-4-methylcoumarin
recombinant form without C-terminal extension
-
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
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.2
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
23
benzyloxycarbonyl-Arg-Ala-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
1.2
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
5.9
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
6
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
13
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
54
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
70
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
100
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
150
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
160
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
190
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
190
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
200
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
220
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 5.5, 25°C, wild-type enzyme
240
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
480
benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin
pH 9.9, 25°C, wild-type enzyme
250
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 3.5, 25°C, wild-type enzyme
560
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.4, 25°C, wild-type enzyme
680
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 4.1, 25°C, wild-type enzyme
1100
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.0, 25°C, wild-type enzyme
1500
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.0, 25°C, wild-type enzyme
1500
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.5, 25°C, wild-type enzyme
1600
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 5.6, 25°C, wild-type enzyme
1900
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 6.5, 25°C, wild-type enzyme
2100
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.0, 25°C, wild-type enzyme
2600
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.0, 25°C, wild-type enzyme
2600
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 9.0, 25°C, wild-type enzyme
2700
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, wild-type enzyme
2700
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 8.5, 25°C, wild-type enzyme
13000
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
pH 7.5, 25°C, mutant enzyme E208A
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.018
propeptide of cruzipain
-
at pH 6.5 the propeptide of cruzipain inactivates cruzipain competitively
-
additional information
additional information
Ki for cystatins and kininogens in the picomolar range
-
additional information
additional information
-
Ki for cystatins and kininogens in the picomolar range
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
-
-
0.025
(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
0.037
(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
0.016
(3Z)-5,7-dimethyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.016 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
0.02 - 0.05
(3Z)-5-methyl-1H-indole-2,3-dione 3-thiosemicarbazone
Trypanosoma cruzi
-
IC50: 0.02-0.05 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
0.005
(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
-
-
0.0028
1-(biphenyl-2-ylmethyl)-5-methyl-1H-indole-2,3-dione
Trypanosoma cruzi
-
IC50: 0.0028 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
0.1
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
-
-
0.073
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
0.1
4-(benzofuroxan-5-ylmethyloxy)benzaldehyde semicarbazone
Trypanosoma cruzi
-
above 0.1 mM
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
0.00007
aceto[2,6-bis[(butylthio-jS)methyl]phenyl-kappaC]-,(SP-4-3)-palladium(II)
Trypanosoma cruzi
-
-
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
-
-
0.05
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
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
0.05
(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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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
4.5
-
hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
6 - 7
-
hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
6.5
6.8
7.6
additional information
6.5
-
assay at room temperature, 5 min, 0.64 nM cruzain, 50 mM sodium phosphate, 100 mM sodium chloride, 5 mM EDTA
8
-
30 min, 50 mM Tris-acetate buffer, 0.3 mM Bz-Pro-Phe-Arg-pNA, 10 mM beta-mercaptoethanol
additional information
substrates placing hydrophobic residues in the specificity pocket are cleaved at a broader pH range than hydrophilic substrates
additional information
-
substrates placing hydrophobic residues in the specificity pocket are cleaved at a broader pH range than hydrophilic substrates
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
3.5 - 9
-
pH 3.5: about 65% of maximal activity, pH 6.5-9.0: about 55% of maximal activity, hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-OH
4.5 - 7.4
hydrophobic substrates reach 50% activity at pH 4.5 and maintain full activity above pH 7.5, more hydrophilic side chains only reach 50% activity at pH 5.5-6
4.5 - 9
-
pH 4.5: about 45% of maximal activity, pH 9.0: about 45% of maximal activity, hydrolysis of 2-aminobenzoyl-FRA-(2,4-dinitrophenyl)-epsilon-NH2-lysine-NH2
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
additional information
additional information
-
assay at room temperature, pH 6.5, 5 min, 0.64 nM cruzain, 50 mM sodium phosphate, 100 mM sodium chloride, 5 mM EDTA
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
638875, 638876, 638877, 638878, 638879, 638880, 638881, 638882, 638883, 638885, 638886, 638887, 638888, 638890, 638891, 638892
SwissProt
brenda
-
667144, 667653, 667936, 667951, 668522, 668551, 670178, 670179, 677418, 679761, 679892, 696523, 696645, 696710, 696760, 697814, 697939, 698164, 698293
-
-
brenda
-
-
-
brenda
-
UniProt
brenda
recombinantly expressed in Escherichia coli as a C-terminally truncated protein
-
-
brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
studies are carried out using murine macrophage cell line J774 as well as bone marrow-derived macrophages from BALB/c mice
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
the signaling factor NF-kB P65 colocalizes with cruzain on the cell surface of intracellular wild-type parasites
brenda
-
membrane bound compartments between nucleus and kinetoplast
-
brenda
-
membrane bound compartments between nucleus and kinetoplast
-
-
brenda
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
-
the O-GlcNAc moieties constitute a common epitope between cruzipain and either myosin or other cardiac O-GlcNAc-containing proteins
malfunction
-
cruzain-deficient Trypanosoma cruzi rapidly activates host macrophages via NF-kB P65 and is unable to survive intracellularly within macrophages. No significant IL-12 expression occurs in macrophages infected with wild-type Trypanosoma cruzi and treated with lipopolysacchrides and brefeldin A, confirming impairment of macrophage activation pathways
metabolism
the enzyme is expressed by the protozoan parasite Trypanosoma cruzi during Chagas disease infection
physiological function
physiological function
-
infection with wild-type parasites appears to induce cruzain-mediated proteolysis of NF-kappaB P65 leading to unresponsiveness of the host macrophage during early 60 min of infection. This immune evasion mechanism may be critical for Trypaosoma cruzi survival during early natural infection with a low number of trypmastigotes. The signaling factor NF-kappaB P65 colocalizes with cruzain on the cell surface of intracellular wild-type parasites, and is proteolytically cleaved. Transcription factor NF-kappaB P65 is translocated to the nucleus and activated only in macrophages infected with cruzain-deficient parasites
physiological function
-
cruzipain promotes Trypanosoma cruzi adhesion to Rhodnius prolixus midgut
physiological function
cruzain is the major cysteine protease involved in the survival of the parasite Trypanosoma cruzi
physiological function
key enzyme for the survival and propagation of this parasite lifecycle
physiological function
the enzyme is the etiological agent of Chagas disease
physiological function
-
cruzipain promotes Trypanosoma cruzi adhesion to Rhodnius prolixus midgut
-
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UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). CYSP_TRYCR
467
1
49836
Swiss-Prot
Secretory Pathway (Reliability: 1)
Q4E0J6_TRYCC
Trypanosoma cruzi (strain CL Brener)
174
1
18857
TrEMBL
Secretory Pathway (Reliability: 1)
Q4CTX9_TRYCC
Trypanosoma cruzi (strain CL Brener)
181
0
19299
TrEMBL
other Location (Reliability: 1)
Q4CQ35_TRYCC
Trypanosoma cruzi (strain CL Brener)
247
2
27163
TrEMBL
other Location (Reliability: 3)
Q4E2M5_TRYCC
Trypanosoma cruzi (strain CL Brener)
244
1
25711
TrEMBL
Secretory Pathway (Reliability: 1)
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PDB
SCOP
CATH
UNIPROT
ORGANISM
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
12000
-
x * 12000, non-adsorbed (to concanavalin A-Sepharose) cruzipain isoform, SDS-PAGE
33000
40000
about 40000 Da, calculated from amino acid sequence
50000
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 12000, non-adsorbed (to concanavalin A-Sepharose) cruzipain isoform, SDS-PAGE
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
additional information
glycoprotein
N-glycosylation at Asn254, no O-glycosylation or phosphorylation
glycoprotein
-
presence of sialic acid in N-linked oligosaccharide chains and O-linked N-acetylglucosamine
glycoprotein
-
sulfated high-mannose type oligosaccharides, lactosaminic glycans and fucosylated oligosaccharides