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Literature summary for 1.1.1.205 extracted from

  • Gorla, S.K.; Kavitha, M.; Zhang, M.; Liu, X.; Sharling, L.; Gollapalli, D.R.; Striepen, B.; Hedstrom, L.; Cuny, G.D.
    Selective and potent urea inhibitors of cryptosporidium parvum inosine 5-monophosphate dehydrogenase (2012), J. Med. Chem., 55, 7759-7771.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)-3-quinolin-7-ylurea displays high potency against Cryptosporidium parvum IMPDH, more than 1000fold selectivity versus human IMPDH type 2 and good stability in mouse liver microsomes Cryptosporidium parvum
1-(4-chloro-5-nitrocyclohexa-1,5-dien-1-yl)-3-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea displays high potency against Cryptosporidium parvum IMPDH, more than 1000fold selectivity versus human IMPDH type 2 and good stability in mouse liver microsomes Cryptosporidium parvum
1-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]-3-quinolin-7-ylurea displays high potency against Cryptosporidium parvum IMPDH, more than 1000fold selectivity versus human IMPDH type 2 and good stability in mouse liver microsomes Cryptosporidium parvum

Organism

Organism UniProt Comment Textmining
Cryptosporidium parvum Q8T6T2
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000066
-
pH 8.0, 25°C Cryptosporidium parvum 1-(4-chloro-5-nitrocyclohexa-1,5-dien-1-yl)-3-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)urea
0.0000008
-
pH 8.0, 25°C Cryptosporidium parvum 1-[2-[3-(prop-1-en-2-yl)phenyl]propan-2-yl]-3-quinolin-7-ylurea
0.0000009
-
pH 8.0, 25°C Cryptosporidium parvum 1-(2-[3-[(1E)-N-hydroxyethanimidoyl]phenyl]propan-2-yl)-3-quinolin-7-ylurea