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Literature summary for 2.7.1.1 extracted from

  • Davis, M.I.; Patrick, S.; Blanding, W.M.; Dwivedi, V.; Suryadi, J.; Golden, J.E.; Coussens, N.P.; Lee, O.W.; Shen, M.; Boxer, M.B.; Hall, M.D.; Sharlow, E.R.; Drew, M.E.; Morris, J.C.
    Identification of novel Plasmodium falciparum hexokinase inhibitors with anti-parasitic activity (2016), Antimicrob. Agents Chemother., 60, 6023-6033.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.1

Application

Application Comment Organism
analysis high-throughput assay for screening small molecule collections to identify inhibitors of the Plasmodium falciparum hexokinase. The assay employs an ADP-GloTM reporter system in a 1536-well plate format, is robust with a signal-to-background of 3.4, a percent coefficient of variation of 6.8 and a Z'-factor of 0.75 Plasmodium falciparum

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
(1R)-6-bromo-3-ethenyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol weak activity on hexokinase, 51% growth inhibition on asexual stage Plasmodium falciparum parasite Plasmodium falciparum
dimethyl 2-[[(2E)-3-(4-ethoxyphenyl)prop-2-enoyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3,4-dicarboxylate among most potent inhibitors identified in screen, lacks activity against parasites Plasmodium falciparum
dimethyl 2-[[4-(3-methylphenoxy)butanoyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3,4-dicarboxylate among most potent inhibitors identified in screen, lacks activity against parasites Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q02155
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IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0011
-
 pH 7.9, 22°C Plasmodium falciparum dimethyl 2-[[(2E)-3-(4-ethoxyphenyl)prop-2-enoyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3,4-dicarboxylate
0.0019
-
 pH 7.9, 22°C Plasmodium falciparum dimethyl 2-[[4-(3-methylphenoxy)butanoyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3,4-dicarboxylate
0.0274
-
 pH 7.9, 22°C Plasmodium falciparum (1R)-6-bromo-3-ethenyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol