Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.22.B69 extracted from

  • Ettari, R.; Zappala, M.; Micale, N.; Grazioso, G.; Giofre, S.; Schirmeister, T.; Grasso, S.
    Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors (2011), Eur. J. Med. Chem., 46, 2058-2065.
    View publication on PubMed
Search for more literature for 3.4.22.B69

Inhibitors

Inhibitors Comment Organism Structure
(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
-
 Plasmodium falciparum
2-[3-(isobutylamino-methyl)-2-oxo-5-phenyl-2,3-dihydrobenzo[e][1,4]diazepin-1-yl]-N-(4-oxo-pent-2-enyl)-acetamide
-
 Plasmodium falciparum
E-64
-
 Plasmodium falciparum
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
-
 Plasmodium falciparum
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 Plasmodium falciparum
[(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
-
 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.
Cbz-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Plasmodium falciparum Cbz-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
Hemoglobin + H2O
-
 Plasmodium falciparum ?
-
 ?

Synonyms

Synonyms Comment Organism
FP-2
-
 Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00029
-
 E-64 in 50 mM sodium acetate buffer, pH 5.5 containing 10 mM dithiothreitol, at 22°C Plasmodium falciparum
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 Plasmodium falciparum