3.4.22.B69: falcipain-2

This is an abbreviated version!
For detailed information about falcipain-2, go to the full flat file.

Word Map on EC 3.4.22.B69

3.4.22.B69

plasmodium

falciparum

antimalarial

malaria

hemoglobin

falcipain-3

antiplasmodial

papain-family

chloroquine-resistant

hemoglobinases

rhodesain

prodomains

plasmepsins

hemozoin

cruzain

thiosemicarbazone

chloroquine-sensitive

Reaction

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, FP-2, Fp2, haemoglobinase

ECTree

3 Hydrolases

3.4 Acting on peptide bonds (peptidases)

3.4.22 Cysteine endopeptidases

3.4.22.B69 falcipain-2

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Results	in table
1	AA Sequence
4	Cloned(Commentary)
3	Crystallization (Commentary)
2	General Information
88	IC50 Value
150	Inhibitors
2	kcat/KM [mM/s]
21	Ki Value [mM]
2	Localization
1	Molecular Weight [Da]
13	Natural Substrates/ Products (Substrates)
24	Organism
1	pH Optimum
3	Purification (Commentary)
1	Reaction
23	Reference
1	Renatured (Commentary)
33	Substrates and Products (Substrate)
1	Subunits
15	Synonyms

IC50 Value

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IC50 Value on EC 3.4.22.B69 - falcipain-2

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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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

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

731483

0.002

3,3'-(3,7,12,17-tetramethylporphyrin-2,18-diyl)dipropanoic acid

Plasmodium falciparum

at pH 5.5 and 37°C

731224

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

731753

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

717366

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

717366

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

717366

0.000159

artemisinin

Plasmodium falciparum

in 100 mM acetate buffer pH 5.5, at 37°C

731483

0.003

bilirubin

Plasmodium falciparum

at pH 5.5 and 37°C

731224

0.000066

Chloroquine diphosphate

Plasmodium falciparum

in 100 mM acetate buffer pH 5.5, at 37°C

731483

0.0009

coproporphyrin

Plasmodium falciparum

at pH 5.5 and 37°C

731224

0.00048

deuteroporphyrin IX 2,4 (4,2) hydroxyvinyl

Plasmodium falciparum

at pH 5.5 and 37°C

731224

0.00062

deuteroporphyrin IX 2-vinyl, 4-hydroxymethyl

Plasmodium falciparum

at pH 5.5 and 37°C

731224

0.000017 - 0.000047

E-64

2 entries

0.000515

heme

Plasmodium falciparum

at pH 5.5 and 37°C

731224

0.002

isohematoporphyrin IX

Plasmodium falciparum

at pH 5.5 and 37°C

731224

0.005

mesoporphyrin IX dimethyl ester

Plasmodium falciparum

IC50 above 0.005 mM, at pH 5.5 and 37°C

731224

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

717366

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

717366

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

717366

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

717366

0.005

N-methyl mesoporphyrin

Plasmodium falciparum

IC50 above 0.005 mM, at pH 5.5 and 37°C

731224

0.00037

N-methyl protoporphyrin IX

Plasmodium falciparum

at pH 5.5 and 37°C

731224

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

Q9N6S8

pH not specified in the publication, temperature not specified in the publication

753004

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

Q9N6S8

pH not specified in the publication, temperature not specified in the publication

753004

0.00055

protoporphyrin IX

Plasmodium falciparum

at pH 5.5 and 37°C

731224

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

731753

additional information

3-(1-benzoyl-5-(4-flurophenyl)-4,5-dihydro-1H-pyrazol-3yl)-7-(diethyamino)-2H-chromen-2-one

2 entries