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Information on EC 3.4.22.B69 - falcipain-2 and Organism(s) Plasmodium falciparum and UniProt Accession Q9N6S8

for references in articles please use BRENDA:EC3.4.22.B69
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EC Tree
     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.B69 falcipain-2
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This record set is specific for:
Plasmodium falciparum
UNIPROT: Q9N6S8
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Word Map
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The taxonomic range for the selected organisms is: Plasmodium falciparum
The expected taxonomic range for this enzyme is: Plasmodium
Reaction Schemes
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The enzyme plays a key role in the hydrolysis of hemoglobin by the parasite Plasmodium falciparum. Preferred cleavage sites display arginine in P1, leucine in P2, and phenylalanine in P1'
Synonyms
falcipain-2, falcipain 2, haemoglobinase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
falcipain-2
-
-
haemoglobinase
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-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
Hemoglobin + H2O
?
show the reaction diagram
-
-
-
?
VLK-4-nitroanilide + H2O
VLK + 4-nitronaniline
show the reaction diagram
-
-
-
?
Abz-KLRFSKQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-KLRSSKQ-EDDnp + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-KLRSXKQ-EDDnp + H2O
Abz-KLRS + XKQ-EDDnp
show the reaction diagram
-
-
-
-
?
Abz-KLRXSKQ-EDDnp + H2O
Abz-KLR + XSKQ-EDDnp
show the reaction diagram
-
-
-
-
?
Abz-KLXSSKQ-EDDnp + H2O
Abz-KLX + SSKQ-EDDnp
show the reaction diagram
-
-
-
-
?
Abz-KXRSSKQ-EDDnp + H2O
Abz-KXR + SSKQ-EDDnp
show the reaction diagram
-
-
-
-
?
Abz-MISLMKRPPGFSPFRSSRI-NH2 + H2O
?
show the reaction diagram
-
the peptide corresponds to the Met375 to Ile393 sequence of high molecular weight kininogen. The enzyme preferentially accommodates at the S1 subsite the positively charged residue Arg, followed by Gln. At the P2 position, the enzyme shows a clear preference for the hydrophobic aliphatic residue Leu over Phe. The subsite S3 of FP-2 shows a broad specificity with slight preference of Lys in the P3 position
the generated fragments are KRPPGFSPFR (Lys-bradykinin, 63%), RPPGFSPFR (bradykinin, 30%), and MKRPPGFSPFR (Met-Lys-bradykinin, 7%)
-
?
Abz-XLRSSKQ-EDDnp + H2O
Abz-XLR + SSKQ-EDDnp
show the reaction diagram
-
-
-
-
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Cbz-Phe-Arg-7-amido-4-methylcoumarin + H2O
Cbz-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
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-
-
-
?
D-Val-Leu-Arg-7-amido-4-methylcoumarin + H2O
D-Val-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
high molecular weight kininogen + H2O
Met-Lys-bradykinin + Lys-bradykinin + bradykinin + ?
show the reaction diagram
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-
-
-
?
N-benzyloxycarbonyl-Leu-Arg 7-amido-4-methylcoumarin + H2O
N-benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
Z-Phe-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
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-
-
-
?
additional information
?
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the falcipain-2 prodomain efficiently inhibits falcipain-2, falcipain-2', berghepain-2, falcipain-3, cathepsin K, cathepsin L, cathepsin B, and cruzain, but it does not inhibit cathepsin C, pepsin, alpha-chymotrypsin, and collagenase
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-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Hemoglobin + H2O
?
show the reaction diagram
-
-
-
?
high molecular weight kininogen + H2O
Met-Lys-bradykinin + Lys-bradykinin + bradykinin + ?
show the reaction diagram
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-
-
-
?
additional information
?
-
-
the falcipain-2 prodomain efficiently inhibits falcipain-2, falcipain-2', berghepain-2, falcipain-3, cathepsin K, cathepsin L, cathepsin B, and cruzain, but it does not inhibit cathepsin C, pepsin, alpha-chymotrypsin, and collagenase
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
3-((2-chloro-6-methoxyquinolin-3-yl)methylene)-5-(2,4-dimethylphenyl)furan-2(3H)-one
IC50 value on parasite 0.50 microg/ml
3-((2-chloro-6-methoxyquinolin-3-yl)methylene)-5-(4-chlorophenyl)furan-2(3H)-one
IC50 value on parasite 0.61 micro/ml
3-(1-benzoyl-5-(4-flurophenyl)-4,5-dihydro-1H-pyrazol-3yl)-7-(diethyamino)-2H-chromen-2-one
-
amino[(2E)-2-[1-(4-methoxyphenyl)ethylidene]hydrazinyl]methanethiol
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benzyl (1-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]cyclohexyl)carbamate
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benzyl [1-[(2-oxoethyl)carbamoyl]cyclohexyl]carbamate
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benzyl [1-[(cyanomethyl)amino]-2-methyl-1-oxopropan-2-yl]carbamate
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benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
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N-((S)-1-(((S)-1-(((S)-1-(2-((4-fluorophenoxy)methyl)-4,5-dihydro-1H-imidazol-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)piperidine-1-carboxamide
compound inhibits the growth of the drug resistant parasite Dd2. IC50 value for strain 3D/ 0.0055 mM
N-((S)-1-(((S)-1-(((S)-2-((S)-2-((4-fluorophenoxy)methyl)pyrrolidin-1-yl)-2-oxo-1-phenylethyl)amino)-4-methyl-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)morpholine-4-carboxamide
compound exhibits potent anti-parasitic activity and a 7- to 12fold higher potency against drug resistant Dd2 and MCamp isolates, than the laboratory strain 3D7. IC50 value for strain 3D7 0.0009 mM
N-(cyanomethyl)-1-([[(1S,2S)-2-phenylcyclopropyl]carbonyl]amino)cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[(3-cyclopentylpropanoyl)amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[(cyclopentylacetyl)amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(2,3-dimethoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(2-methoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(4-methoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(furan-2-yl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(pyridin-3-yl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(thiophen-2-yl)propanoyl]amino]cyclohexanecarboxamide
-
N-[(2S)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(pyridin-3-yl)propan-2-yl]-3-(1H-imidazol-2-yl)benzamide
P2-modified aminonitrile based inhibitor, not cytotoxic to either cancer (HeLa) or normal (Huvec) human cell lines
N-[(2S)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(pyridin-3-yl)propan-2-yl]-3-(1H-tetrazol-1-yl)benzamide
compound shows more than 500fold selectivity for falcipain-2 over cathepsin B, K and L and about 30fold selectivity over cathepsin S. Not cytotoxic to either cancer (HeLa) or normal (Huvec) human cell lines
SERPINB3
potent cross-class inhibitor of cysteine cathepsins L, K, S and papain, inhibits proteolytic activities as well as specific hemoglobinolytic activity of FP2 via noncovalent interaction. Disease state mutant serpin-Gly351Ala displays better anti-protease activity against FP2
-
(1,1-dioxido-3-oxo-1,2-benzothiazol-2(3H)-yl)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
-
24% inhibition at 0.02 mM
(4-chloro-2-trifluoromethyl-phenyl)-carbamic acid 5-methyl-2-oxo-1-[(4-oxo-pent-2-enylcarbamoyl)-methyl]-2,3-dihydro-1H-benzo[e][1,4] diazepin-3-methyl ester
-
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(5Z)-3-(2,4-difluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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(5Z)-3-(3-methoxybenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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-
(5Z)-3-(4-fluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
(5Z)-3-(4-methylbenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
(5Z)-3-benzyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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-
(5Z)-3-ethyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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-
(5Z)-3-methyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
(5Z)-3-[4-(trifluoromethyl)benzyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
(5Z)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
(S)-2-(1-(4-benzylpiperidin-1-yl)-1-oxo-3-phenylpropan-2-yl)isoindoline-1,3-dione
-
-
(S)-2-(1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxobutan-2-yl)isoindoline-1,3-dione
-
-
(S)-2-(1-(4-benzylpiperidin-1-yl)-4-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
-
-
2,2'-((2S,2'S)-piperazine-1,4-diylbis(1-oxo-3-phenylpropane-2,1-diyl))bis(isoindoline-1,3-dione)
-
-
2,2'-((2S,2'S)-piperazine-1,4-diylbis(3-methyl-1-oxobutane-2,1-diyl))bis(isoindoline-1,3-dione)
-
-
2,2'-((2S,2'S)-piperazine-1,4-diylbis(4-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
-
-
2,2'-((2S,2'S,3R,3'R)-piperazine-1,4-diylbis(3-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
-
-
2-((2S,3S)-1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
-
-
2-[(2S)-1-(morpholin-4-yl)-1-oxo-3-phenylpropan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S)-1-oxo-3-phenyl-1-(piperidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S)-1-oxo-3-phenyl-1-(pyrrolidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S)-3-methyl-1-(morpholin-4-yl)-1-oxobutan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S)-3-methyl-1-oxo-1-(piperidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S)-4-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S)-4-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S)-4-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S,3R)-3-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S,3R)-3-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[(2S,3R)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
-
2-[3-(isobutylamino-methyl)-2-oxo-5-phenyl-2,3-dihydrobenzo[e][1,4]diazepin-1-yl]-N-(4-oxo-pent-2-enyl)-acetamide
-
-
3,3'-(3,7,12,17-tetramethylporphyrin-2,18-diyl)dipropanoic acid
-
-
3-adamantyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-(2-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-(4-cyanophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-(4-methoxyphenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-cyclohexylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-methylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenoxypiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dichlorobenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dimethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,5-ditrifluoromethylbenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-bromobenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-chlorobenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3,4-difluorobenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-carboxybenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-fluorobenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-isopropylbenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methoxybenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methylbenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-chlorobenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-fluorobenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methoxybenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methylbenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethylbenzylidene)
-
-
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-benzylidene-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(4-pyridylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[2-oxo-2-(piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
3-[4-(benzylsulfamoyl)phenyl]-N-(2,3-dihydro-1,4-benzodioxin-6-yl)propanamide
-
less than 5% inhibition at 0.01 mM
3-[4-[(2-phenylethyl)sulfamoyl]phenyl]-N-(5-phenyl-1,3,4-thiadiazol-2-yl)propanamide
-
94.5% inhibition at 0.01 mM
3-[4-[(2-phenylethyl)sulfamoyl]phenyl]-N-(pyridin-2-ylmethyl)propanamide
-
10.7% inhibition at 0.01 mM
3-[4-[(2-phenylethyl)sulfamoyl]phenyl]-N-(thiophen-2-ylmethyl)propanamide
-
15.2% inhibition at 0.01 mM
3-[4-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]-N-(2,3-dihydro-1,4-benzodioxin-6-yl)propanamide
-
32.7% inhibition at 0.01 mM
3-[4-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]-N-(5-ethyl-1,3,4-thiadiazol-2-yl)propanamide
-
45.1% inhibition at 0.01 mM
artemisinin
-
-
artesunate
-
-
auranofin
-
30% inhibition at 0.02 mM
chicken egg white cystatin
-
-
-
Chloroquine
-
-
Chloroquine diphosphate
-
-
chloro[N-[1-(hydroxy-kappaO)-3-methylbutan-2-yl]pyridine-2-carboxamidato(2-)-kappa2N1,N2]aurate(2-)
-
43% inhibition at 0.02 mM
cisplatin
-
43% inhibition at 0.02 mM
coproporphyrin
-
-
deuteroporphyrin IX 2,4 (4,2) hydroxyvinyl
-
-
deuteroporphyrin IX 2-vinyl, 4-hydroxymethyl
-
-
dichloro[3-(propan-2-yl)-2-(pyridin-2-yl-kappaN)-4,5-dihydro-1,3-oxazol-3-ium-kappaN]aurate(1-) hexafluorophosphate
-
59% inhibition at 0.02 mM
heme
-
heme inhibits falcipain-2 activity against both human hemoglobin and chromogenic peptide substrates through a noncompetitive-like mechanism
isohematoporphyrin IX
-
-
leupeptide
-
-
-
mesoporphyrin IX dimethyl ester
-
-
methyl (2E)-4-[({(3R)-3-[({[4-chloro-2-(trifluoromethyl)phenyl]carbamoyl}oxy)methyl]-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-1-yl}acetyl)amino]but-2-enoate
-
-
N-(1,3-benzothiazol-2-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
41.5% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[4-[(2-phenylethyl)sulfamoyl]phenyl]acetamide
-
less than 5% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
23% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-[(3,4-dimethoxyphenyl)sulfamoyl]phenyl]propanamide
-
6.3% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-[(3-methoxyphenyl)sulfamoyl]phenyl]propanamide
-
17.9% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-[(2-phenylethyl)sulfamoyl]benzamide
-
less than 5% inhibition at 0.01 mM
N-(3,4-dimethoxyphenyl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
15% inhibition at 0.01 mM
N-(3-hydroxy-4-methoxyphenyl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
13.6% inhibition at 0.01 mM
N-(4-oxo-pent-2-enyl)-2-(2-oxo-5-phenyl-3-morpholin-1-ylmethyl-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)-acetamide
-
-
N-(4-oxo-pent-2-enyl)-2-(2-oxo-5-phenyl-3-piperidin-1-ylmethyl-2,3-dihydro-benzo[e][1,4] diazepin-1-yl)-acetamide
-
80% inhibition at 0.1 mM, no inhibition at 0.03 mM
N-(5-ethyl-1,3,4-thiadiazol-2-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
46.5% inhibition at 0.01 mM
N-(5-ethyl-1,3,4-thiadiazol-2-yl)-3-[4-[(4-fluorophenyl)sulfamoyl]phenyl]propanamide
-
72.9% inhibition at 0.01 mM
N-methyl mesoporphyrin
-
-
N-methyl protoporphyrin IX
-
-
potassium bis(1,1-dioxido-3-oxo-1,2-benzothiazol-2(3H)-yl)aurate(1-)
-
66% inhibition at 0.02 mM
protoporphyrin IX
-
-
RLLGAP-(cis-4-aminocyclohexane carboxylic acid)-QLVSGI
-
-
RLLGAP-(cis-4-aminocyclohexane carboxylic acid)-QLVSGI-betaAla-betaAla-PW
-
-
RLLGAP-gamma-aminobutyric acid-QLVSGI
-
-
RLLGAP-gamma-aminobutyric acid-QLVSGI-betaAla-betaAla-PW
-
-
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI
-
63% inhibition at 0.005 mM
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI-betaAla-betaAla-PW
-
-
RLLGAPV-gamma-aminobutyric acid-RQLVSGI
-
57% inhibition at 0.005 mM
RLLGAPV-gamma-aminobutyric acid-RQLVSGI-betaAla-betaAla-PW
-
-
[(3R)-2-oxo-1-(2-oxo-2-[[(2E)-4-oxopent-2-en-1-yl]amino]ethyl)-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]methyl [4-chloro-2-(trifluoromethyl)phenyl]carbamate
-
-
[(5Z)-2,4-dioxo-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidin-3-yl]acetic acid
-
-
[3-benzyl-2-(pyridin-2-yl-kappaN)-4,5-dihydro-1,3-oxazol-3-ium-kappaN](dichloro)aurate(1-) hexafluorophosphate
-
54% inhibition at 0.02 mM
additional information
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2440
Abz-KLRFSKQ-EDDnp
-
in 0.1 M sodium acetate, pH 5.5, at 37°C
1850
Abz-KLRSSKQ-EDDnp
-
in 0.1 M sodium acetate, pH 5.5, at 37°C
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000065
benzyl [1-[(2-oxoethyl)carbamoyl]cyclohexyl]carbamate
pH and temperature not specified in the publication
0.0012
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
pH and temperature not specified in the publication
0.0002
N-((S)-1-(((S)-1-(((S)-1-(2-((4-fluorophenoxy)methyl)-4,5-dihydro-1H-imidazol-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)piperidine-1-carboxamide
pH 5.5, 23°C
0.0011
N-((S)-1-(((S)-1-(((S)-2-((S)-2-((4-fluorophenoxy)methyl)pyrrolidin-1-yl)-2-oxo-1-phenylethyl)amino)-4-methyl-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)morpholine-4-carboxamide
pH 5.5, 23°C
0.0021
N-(cyanomethyl)-1-([[(1S,2S)-2-phenylcyclopropyl]carbonyl]amino)cyclohexanecarboxamide
pH and temperature not specified in the publication
0.0082
N-(cyanomethyl)-1-[(3-cyclopentylpropanoyl)amino]cyclohexanecarboxamide
pH and temperature not specified in the publication
0.0076
N-(cyanomethyl)-1-[(cyclopentylacetyl)amino]cyclohexanecarboxamide
pH and temperature not specified in the publication
0.0073
N-(cyanomethyl)-1-[[3-(2,3-dimethoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
pH and temperature not specified in the publication
0.0052
N-(cyanomethyl)-1-[[3-(2-methoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
pH and temperature not specified in the publication
0.0089
N-(cyanomethyl)-1-[[3-(4-methoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
pH and temperature not specified in the publication
0.0172
N-(cyanomethyl)-1-[[3-(furan-2-yl)propanoyl]amino]cyclohexanecarboxamide
pH and temperature not specified in the publication
0.0094
N-(cyanomethyl)-1-[[3-(pyridin-3-yl)propanoyl]amino]cyclohexanecarboxamide
pH and temperature not specified in the publication
0.0088
N-(cyanomethyl)-1-[[3-(thiophen-2-yl)propanoyl]amino]cyclohexanecarboxamide
pH and temperature not specified in the publication
0.000338
SERPINB3
pH not specified in the publication, temperature not specified in the publication
-
0.1
2-[3-(isobutylamino-methyl)-2-oxo-5-phenyl-2,3-dihydrobenzo[e][1,4]diazepin-1-yl]-N-(4-oxo-pent-2-enyl)-acetamide
-
Ki above 0.1 mM, in 50 mM sodium acetate buffer, pH 5.5 containing 10 mM dithiothreitol, at 22°C
0.0000065
chicken egg white cystatin
-
in 100 mM NaOAc, 10 mM dithiothreitol, at 22°C, pH not specified in the publication
-
0.00029
E-64
0.002
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI
-
in 100 mM NaOAc, 10 mM dithiothreitol, at 22°C, pH not specified in the publication
0.0025
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI-betaAla-betaAla-PW
-
in 100 mM NaOAc, 10 mM dithiothreitol, at 22°C, pH not specified in the publication
0.0025
RLLGAPV-gamma-aminobutyric acid-RQLVSGI
-
in 100 mM NaOAc, 10 mM dithiothreitol, at 22°C, pH not specified in the publication
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000027
N-[(2S)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(pyridin-3-yl)propan-2-yl]-3-(1H-imidazol-2-yl)benzamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.000003
N-[(2S)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(pyridin-3-yl)propan-2-yl]-3-(1H-tetrazol-1-yl)benzamide
Plasmodium falciparum
pH not specified in the publication, temperature not specified in the publication
0.02908
(5Z)-3-(2,4-difluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
(5Z)-3-(3-methoxybenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
(5Z)-3-(4-fluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.04335
(5Z)-3-(4-methylbenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.03624
(5Z)-3-benzyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
(5Z)-3-ethyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
(5Z)-3-methyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
(5Z)-3-[4-(trifluoromethyl)benzyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.04784
(5Z)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.01216
(S)-2-(1-(4-benzylpiperidin-1-yl)-1-oxo-3-phenylpropan-2-yl)isoindoline-1,3-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.04824
(S)-2-(1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxobutan-2-yl)isoindoline-1,3-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.04423
(S)-2-(1-(4-benzylpiperidin-1-yl)-4-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.0527
2,2'-((2S,2'S)-piperazine-1,4-diylbis(1-oxo-3-phenylpropane-2,1-diyl))bis(isoindoline-1,3-dione)
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.01689
2,2'-((2S,2'S)-piperazine-1,4-diylbis(3-methyl-1-oxobutane-2,1-diyl))bis(isoindoline-1,3-dione)
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.203
2,2'-((2S,2'S)-piperazine-1,4-diylbis(4-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.00597
2,2'-((2S,2'S,3R,3'R)-piperazine-1,4-diylbis(3-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.05379
2-((2S,3S)-1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.04943
2-[(2S)-1-(morpholin-4-yl)-1-oxo-3-phenylpropan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.03605
2-[(2S)-1-oxo-3-phenyl-1-(piperidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.0876
2-[(2S)-1-oxo-3-phenyl-1-(pyrrolidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.2056
2-[(2S)-3-methyl-1-(morpholin-4-yl)-1-oxobutan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.1305
2-[(2S)-3-methyl-1-oxo-1-(piperidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.1416
2-[(2S)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.1393
2-[(2S)-4-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.2179
2-[(2S)-4-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.2362
2-[(2S)-4-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.06057
2-[(2S,3R)-3-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.1067
2-[(2S,3R)-3-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.1464
2-[(2S,3R)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.002
3,3'-(3,7,12,17-tetramethylporphyrin-2,18-diyl)dipropanoic acid
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.02908
3-adamantyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.01264
3-[2-oxo-2-(4-(2-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.01625
3-[2-oxo-2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.01123
3-[2-oxo-2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.01224
3-[2-oxo-2-(4-(4-cyanophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-(4-methoxyphenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-cyclohexylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-methylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.03375
3-[2-oxo-2-(4-phenoxypiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dichlorobenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dimethoxybenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.03528
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,5-ditrifluoromethylbenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.02388
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-bromobenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.0158
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-chlorobenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.03528
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3,4-difluorobenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-carboxybenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.03325
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-fluorobenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.02389
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-isopropylbenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methoxybenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.04533
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methylbenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.04497
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-chlorobenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-fluorobenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methoxybenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.04571
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methylbenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.01344
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.01804
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethylbenzylidene)
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.0388
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-benzylidene-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(4-pyridylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.05
3-[2-oxo-2-(piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
0.0027
3-[4-[(2-phenylethyl)sulfamoyl]phenyl]-N-(5-phenyl-1,3,4-thiadiazol-2-yl)propanamide
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, 10 mM dithiothreitol, at 22°C
0.0132
3-[4-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]-N-(2,3-dihydro-1,4-benzodioxin-6-yl)propanamide
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, 10 mM dithiothreitol, at 22°C
0.0098
3-[4-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]-N-(5-ethyl-1,3,4-thiadiazol-2-yl)propanamide
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, 10 mM dithiothreitol, at 22°C
0.000159
artemisinin
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.003
bilirubin
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.000066
Chloroquine diphosphate
Plasmodium falciparum
-
in 100 mM acetate buffer pH 5.5, at 37°C
0.0009
coproporphyrin
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.00048
deuteroporphyrin IX 2,4 (4,2) hydroxyvinyl
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.00062
deuteroporphyrin IX 2-vinyl, 4-hydroxymethyl
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.000017 - 0.000047
E-64
0.000515
heme
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.002
isohematoporphyrin IX
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.005
mesoporphyrin IX dimethyl ester
Plasmodium falciparum
-
IC50 above 0.005 mM, at pH 5.5 and 37°C
0.0089
N-(1,3-benzothiazol-2-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, 10 mM dithiothreitol, at 22°C
0.0542
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, 10 mM dithiothreitol, at 22°C
0.0081
N-(5-ethyl-1,3,4-thiadiazol-2-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, 10 mM dithiothreitol, at 22°C
0.007
N-(5-ethyl-1,3,4-thiadiazol-2-yl)-3-[4-[(4-fluorophenyl)sulfamoyl]phenyl]propanamide
Plasmodium falciparum
-
in 100 mM sodium acetate, pH 5.5, 10 mM dithiothreitol, at 22°C
0.005
N-methyl mesoporphyrin
Plasmodium falciparum
-
IC50 above 0.005 mM, at pH 5.5 and 37°C
0.00037
N-methyl protoporphyrin IX
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.00055
protoporphyrin IX
Plasmodium falciparum
-
at pH 5.5 and 37°C
0.05
[(5Z)-2,4-dioxo-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidin-3-yl]acetic acid
Plasmodium falciparum
-
IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C
additional information
3-(1-benzoyl-5-(4-flurophenyl)-4,5-dihydro-1H-pyrazol-3yl)-7-(diethyamino)-2H-chromen-2-one
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
Q9N6S8_PLAFA
484
0
55908
TrEMBL
-
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37000
-
1 * 37000, SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
-
1 * 37000, SDS-PAGE
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
docking of serpinB3
molecular docking of inhibitors
in complex with the inhibitory C-terminal domain of inhibitors of cysteine protease from Plasmodium berghei, sitting drop vapor diffusion method, using 200 mM sodium acetate, 27.5 mM CdCl2, 100 mM MES (pH 5.0)
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
Ni-NTA column chromatography
-
Ni-NTA resin column chromatography, HiTrap Q anion-exchange column chromatography, and Superdex 75 gel filtration
-
nickel affinity column chromatography and Q Sepharose column chromatography
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli
expressed in Escherichia coli
-
expressed in Escherichia coli Origami(DE3) cells
-
RENATURED/Commentary
ORGANISM
UNIPROT
LITERATURE
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Pandey, K.C.; Barkan, D.T.; Sali, A.; Rosenthal, P.J.
Regulatory elements within the prodomain of falcipain-2, a cysteine protease of the malaria parasite Plasmodium falciparum
PLoS ONE
4
e5694
2009
Plasmodium falciparum
Manually annotated by BRENDA team
Hansen, G.; Schwarzloh, B.; Rennenberg, A.; Heussler, V.T.; Hilgenfeld, R.
The macromolecular complex of ICP and falcipain-2 from Plasmodium: preparation, crystallization and preliminary X-ray diffraction analysis
Acta Crystallogr. Sect. F
67
1406-1410
2011
Plasmodium falciparum
Manually annotated by BRENDA team
Huang, H.; Lu, W.; Li, X.; Cong, X.; Ma, H.; Liu, X.; Zhang, Y.; Che, P.; Ma, R.; Li, H.; Shen, X.; Jiang, H.; Huang, J.; Zhu, J.
Design and synthesis of small molecular dual inhibitor of falcipain-2 and dihydrofolate reductase as antimalarial agent
Bioorg. Med. Chem. Lett.
22
958-962
2012
Plasmodium falciparum
Manually annotated by BRENDA team
Ettari, R.; Zappala, M.; Micale, N.; Grazioso, G.; Giofre, S.; Schirmeister, T.; Grasso, S.
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors
Eur. J. Med. Chem.
46
2058-2065
2011
Plasmodium falciparum
Manually annotated by BRENDA team
Rizzi, L.; Sundararaman, S.; Cendic, K.; Vaiana, N.; Korde, R.; Sinha, D.; Mohmmed, A.; Malhotra, P.; Romeo, S.
Design and synthesis of protein-protein interaction mimics as Plasmodium falciparum cysteine protease, falcipain-2 inhibitors
Eur. J. Med. Chem.
46
2083-2090
2011
Plasmodium falciparum
Manually annotated by BRENDA team
Micale, N.; Cinellu, M.A.; Maiore, L.; Sannella, A.R.; Severini, C.; Schirmeister, T.; Gabbiani, C.; Messori, L.
Selected gold compounds cause pronounced inhibition of Falcipain 2 and effectively block P. falciparum growth in vitro
J. Inorg. Biochem.
105
1576-1579
2011
Plasmodium falciparum
Manually annotated by BRENDA team
Ehmke, V.; Kilchmann, F.; Heindl, C.; Cui, K.; Huang, J.; Schirmeister, T.; Diederich, F.
Peptidomimetic nitriles as selective inhibitors for the malarial cysteine protease falcipain-2
MedChemComm
2
800-804
2011
Plasmodium falciparum (Q9N6S8)
-
Manually annotated by BRENDA team
Marques, A.F.; Gomes, P.S.; Oliveira, P.L.; Rosenthal, P.J.; Pascutti, P.G.; Lima, L.M.
Allosteric regulation of the Plasmodium falciparum cysteine protease falcipain-2 by heme
Arch. Biochem. Biophys.
573
92-99
2015
Plasmodium falciparum
Manually annotated by BRENDA team
Singh, A.K.; Rajendran, V.; Pant, A.; Ghosh, P.C.; Singh, N.; Latha, N.; Garg, S.; Pandey, K.C.; Singh, B.K.; Rathi, B.
Design, synthesis and biological evaluation of functionalized phthalimides: A new class of antimalarials and inhibitors of falcipain-2, a major hemoglobinase of malaria parasite
Bioorg. Med. Chem.
23
1817-1827
2015
Plasmodium falciparum
Manually annotated by BRENDA team
Sharma, R.K.; Younis, Y.; Mugumbate, G.; Njoroge, M.; Gut, J.; Rosenthal, P.J.; Chibale, K.
Synthesis and structure-activity-relationship studies of thiazolidinediones as antiplasmodial inhibitors of the Plasmodium falciparum cysteine protease falcipain-2
Eur. J. Med. Chem.
90
507-518
2015
Plasmodium falciparum, Plasmodium falciparum W2
Manually annotated by BRENDA team
Omotuyi, I.O.; Hamada, T.
Dynamical footprint of falcipain-2 catalytic triad in hemoglobin-beta-bound state
J. Biomol. Struct. Dyn.
33
1027-1036
2015
Plasmodium falciparum
Manually annotated by BRENDA team
Grazioso, G.; Legnani, L.; Toma, L.; Ettari, R.; Micale, N.; De Micheli, C.
Mechanism of falcipain-2 inhibition by alpha,beta-unsaturated benzo[1,4]diazepin-2-one methyl ester
J. Comput. Aided Mol. Des.
26
1035-1043
2012
Plasmodium falciparum
Manually annotated by BRENDA team
Bertoldo, J.B.; Chiaradia-Delatorre, L.D.; Mascarello, A.; Leal, P.C.; Cordeiro, M.N.; Nunes, R.J.; Sarduy, E.S.; Rosenthal, P.J.; Terenzi, H.
Synthetic compounds from an in house library as inhibitors of falcipain-2 from Plasmodium falciparum
J. Enzyme Inhib. Med. Chem.
30
299-307
2015
Plasmodium falciparum
Manually annotated by BRENDA team
Cotrin, S.S.; Gouvea, I.E.; Melo, P.M.; Bagnaresi, P.; Assis, D.M.; Araujo, M.S.; Juliano, M.A.; Gazarini, M.L.; Rosenthal, P.J.; Juliano, L.; Carmona, A.K.
Substrate specificity studies of the cysteine peptidases falcipain-2 and falcipain-3 from Plasmodium falciparum and demonstration of their kininogenase activity
Mol. Biochem. Parasitol.
187
111-116
2013
Plasmodium falciparum
Manually annotated by BRENDA team
Alam, B.; Biswas, S.
Inhibition of Plasmodium falciparum cysteine protease falcipain-2 by a human cross-class inhibitor serpinB3 A mechanistic insight
Biochim. Biophys. Acta
1867
854-865
2019
Plasmodium falciparum (Q9N6S8), Plasmodium falciparum
Manually annotated by BRENDA team
Chakka, S.K.; Kalamuddin, M.; Sundararaman, S.; Wei, L.; Mundra, S.; Mahesh, R.; Malhotra, P.; Mohmmed, A.; Kotra, L.P.
Identification of novel class of falcipain-2 inhibitors as potential antimalarial agents
Bioorg. Med. Chem.
23
2221-2240
2015
Plasmodium falciparum (Q9N6S8)
Manually annotated by BRENDA team
Nizi, E.; Sferrazza, A.; Fabbrini, D.; Nardi, V.; Andreini, M.; Graziani, R.; Gennari, N.; Bresciani, A.; Paonessa, G.; Harper, S.
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins
Bioorg. Med. Chem. Lett.
28
1540-1544
2018
Plasmodium falciparum (Q9N6S8), Plasmodium falciparum
Manually annotated by BRENDA team
Himangini, Z.; Pathak, D.P.; Sharma, V.; Kumar, S.
Designing novel inhibitors against falcipain-2 of Plasmodium falciparum
Bioorg. Med. Chem. Lett.
28
1566-1569
2018
Plasmodium berghei, Plasmodium falciparum (Q9N6S8), Plasmodium falciparum
Manually annotated by BRENDA team
Akhter, M.; Saha, R.; Tanwar, O.; Mumtaz Alam, M.; Zaman, M.
Synthesis and antimalarial activity of quinoline-substituted furanone derivatives and their identification as selective falcipain-2 inhibitors
Med. Chem. Res.
24
879-890
2015
Plasmodium falciparum (Q9N6S8)
-
Manually annotated by BRENDA team
Ghogomu, J.; Nkungli, N.
DFT studies and topological analyses of electron density on acetophenone and propiophenone thiosemicarbazone derivatives as covalent inhibitors of falcipain-2, a major Plasmodium falciparum cysteine protease
Phys. Chem. Res.
5
795-817
2017
Plasmodium falciparum (Q9N6S8)
-
Manually annotated by BRENDA team
Hernandez Gonzalez, J.E.; Hernandez Alvarez, L.; Pascutti, P.G.; Valiente, P.A.
Predicting binding modes of reversible peptide-based inhibitors of falcipain-2 consistent with structure-activity relationships
Proteins
85
1666-1683
2017
Plasmodium falciparum (Q9N6S8), Plasmodium falciparum
Manually annotated by BRENDA team