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Literature summary for 3.4.22.B69 extracted from

  • 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 (2015), Bioorg. Med. Chem., 23, 1817-1827.
    View publication on PubMed
Search for more literature for 3.4.22.B69

Inhibitors

Inhibitors Comment Organism Structure
(S)-2-(1-(4-benzylpiperidin-1-yl)-1-oxo-3-phenylpropan-2-yl)isoindoline-1,3-dione
-
 Plasmodium falciparum
(S)-2-(1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxobutan-2-yl)isoindoline-1,3-dione
-
 Plasmodium falciparum
(S)-2-(1-(4-benzylpiperidin-1-yl)-4-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
-
 Plasmodium falciparum
2,2'-((2S,2'S)-piperazine-1,4-diylbis(1-oxo-3-phenylpropane-2,1-diyl))bis(isoindoline-1,3-dione)
-
 Plasmodium falciparum
2,2'-((2S,2'S)-piperazine-1,4-diylbis(3-methyl-1-oxobutane-2,1-diyl))bis(isoindoline-1,3-dione)
-
 Plasmodium falciparum
2,2'-((2S,2'S)-piperazine-1,4-diylbis(4-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
-
 Plasmodium falciparum
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
2-((2S,3S)-1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
-
 Plasmodium falciparum
2-[(2S)-1-(morpholin-4-yl)-1-oxo-3-phenylpropan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S)-1-oxo-3-phenyl-1-(piperidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S)-1-oxo-3-phenyl-1-(pyrrolidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S)-3-methyl-1-(morpholin-4-yl)-1-oxobutan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S)-3-methyl-1-oxo-1-(piperidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S)-4-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S)-4-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S)-4-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S,3R)-3-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S,3R)-3-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
2-[(2S,3R)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
 Plasmodium falciparum
artemisinin
-
 Plasmodium falciparum
Chloroquine diphosphate
-
 Plasmodium falciparum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Hemoglobin + H2O Plasmodium falciparum
-
 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Hemoglobin + H2O
-
 Plasmodium falciparum ?
-
 ?
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O
-
 Plasmodium falciparum Z-Leu-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
Fp2
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000066
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum Chloroquine diphosphate
0.000159
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum artemisinin
0.00597
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2,2'-((2S,2'S,3R,3'R)-piperazine-1,4-diylbis(3-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
0.01216
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum (S)-2-(1-(4-benzylpiperidin-1-yl)-1-oxo-3-phenylpropan-2-yl)isoindoline-1,3-dione
0.01689
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2,2'-((2S,2'S)-piperazine-1,4-diylbis(3-methyl-1-oxobutane-2,1-diyl))bis(isoindoline-1,3-dione)
0.03605
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-1-oxo-3-phenyl-1-(piperidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
0.04423
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum (S)-2-(1-(4-benzylpiperidin-1-yl)-4-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
0.04824
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum (S)-2-(1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxobutan-2-yl)isoindoline-1,3-dione
0.04943
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-1-(morpholin-4-yl)-1-oxo-3-phenylpropan-2-yl]-1H-isoindole-1,3(2H)-dione
0.0527
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2,2'-((2S,2'S)-piperazine-1,4-diylbis(1-oxo-3-phenylpropane-2,1-diyl))bis(isoindoline-1,3-dione)
0.05379
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-((2S,3S)-1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
0.06057
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S,3R)-3-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
0.0876
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-1-oxo-3-phenyl-1-(pyrrolidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
0.1067
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S,3R)-3-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
0.1305
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-3-methyl-1-oxo-1-(piperidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
0.1393
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-4-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
0.1416
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
0.1464
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S,3R)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
0.203
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2,2'-((2S,2'S)-piperazine-1,4-diylbis(4-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
0.2056
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-3-methyl-1-(morpholin-4-yl)-1-oxobutan-2-yl]-1H-isoindole-1,3(2H)-dione
0.2179
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-4-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
0.2362
-
 in 100 mM acetate buffer pH 5.5, at 37°C Plasmodium falciparum 2-[(2S)-4-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione