Target Validation Information
Target ID T88285
Target Name Lactoylglutathione lyase
Target Type
Clinical Trial
Drug Potency against Target S-(N-ethyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 1180 nM [1]
S-(N-phenyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 160 nM [1]
S-(N-methyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 1700 nM [1]
S-(N-pentyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 170 nM [1]
S-(N-hexyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 16 nM [1]
S-(N-propyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 800 nM [1]
S-(N-4bromophenyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 14 nM [1]
S-(N-heptyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 18 nM [1]
PELARGONIDIN CHLORIDE Drug Info IC50 = 16400 nM [2]
S-p-bromobenzyl glutatione Drug Info Ki = 6280 nM [3]
S-(N-4chlorophenyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 46 nM [1]
CYANIDIN Drug Info IC50 = 11700 nM [2]
BAICALEIN Drug Info IC50 = 11000 nM [4]
S-(N-butyl-N-hydroxycarbamoyl)glutathione Drug Info Ki = 180 nM [1]
References
REF 1Role of hydrophobic interactions in binding S-(N-aryl/alkyl-N-hydroxycarbamoyl)glutathiones to the active site of the antitumor target enzyme glyoxalase I. J Med Chem. 2000 Oct 19;43(21):3981-6.
REF 2Bioorg Med Chem. 2010 Oct 1;18(19):7029-33. Epub 2010 Aug 9.Delphinidin, a dietary anthocyanidin in berry fruits, inhibits human glyoxalase I.
REF 3J Med Chem. 2009 Aug 13;52(15):4650-6.Inhibition of glyoxalase I: the first low-nanomolar tight-binding inhibitors.
REF 4Bioorg Med Chem. 2008 Apr 1;16(7):3969-75. Epub 2008 Jan 24.Structure-activity relationship of human GLO I inhibitory natural flavonoids and their growth inhibitory effects.

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