Literature summary for 3.4.22.B69 extracted from

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 (2018), Bioorg. Med. Chem. Lett., 28, 1540-1544 .

Search for more literature for 3.4.22.B69

Inhibitors

Inhibitors	Comment	Organism	Structure
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	Plasmodium falciparum
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	Plasmodium falciparum

Organism

Organism	UniProt	Comment	Textmining
Plasmodium falciparum	Q9N6S8	-	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000027	-	pH not specified in the publication, temperature not specified in the publication	Plasmodium falciparum	N-[(2S)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(pyridin-3-yl)propan-2-yl]-3-(1H-imidazol-2-yl)benzamide
0.000003	-	pH not specified in the publication, temperature not specified in the publication	Plasmodium falciparum	N-[(2S)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(pyridin-3-yl)propan-2-yl]-3-(1H-tetrazol-1-yl)benzamide

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)