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Literature summary for 1.1.1.205 extracted from

  • Johnson, C.R.; Gorla, S.K.; Kavitha, M.; Zhang, M.; Liu, X.; Striepen, B.; Mead, J.R.; Cuny, G.D.; Hedstrom, L.
    Phthalazinone inhibitors of inosine-5-monophosphate dehydrogenase from Cryptosporidium parvum (2013), Bioorg. Med. Chem. Lett., 23, 1004-1007.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
N-[4-chloro-3-(trifluoromethyl)phenyl]-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide noncompetitive with respect to NAD+, displays submicromolar activity in a Toxoplasma gondii model of Cryptosporidium parvum infection and displays good stability in mouse liver microsome. No antiparasitic activity is observed in mouse with once per day oral dosing of 250 mg/kg for 7 days Cryptosporidium parvum

Organism

Organism UniProt Comment Textmining
Cryptosporidium parvum Q8T6T2
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000032
-
 N-[4-chloro-3-(trifluoromethyl)phenyl]-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide pH not specified in the publication, temperature not specified in the publication Cryptosporidium parvum