Literature summary for 3.4.22.B69 extracted from

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 (2015), Bioorg. Med. Chem., 23, 2221-2240 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
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	Plasmodium falciparum
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	Plasmodium falciparum

Organism

Organism	UniProt	Comment	Textmining
Plasmodium falciparum	Q9N6S8	-	-

Substrates and Products (Substrate)

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

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
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	Plasmodium falciparum
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	Plasmodium falciparum

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Release 2023.1 (January 2023)