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. 2017 Sep 7;7:10836. doi: 10.1038/s41598-017-11022-5

Table 1.

Characterization of UGM inhibitors identified by HTS of the Spectrum library using ADP-TAMRA. IC50 was determined with 20 µM UDP-Galf (UPLC) and 10 mM sodium dithionite and for the NADPH oxidation was determined with 250 µM NADPH and no substrate.

Name Chemical Structure IC50 (µM) Type of Inhibition Ki(µM)
UPLC NADPH oxidation
(2S)-hesperetin graphic file with name 41598_2017_11022_Figa_HTML.gif 40 ± 3 32 ± 7 Competitive (NADPH) 6 ± 1
(2S)-naringenin graphic file with name 41598_2017_11022_Figb_HTML.gif 161 ± 11 233 ± 28 Competitive (NADPH) 74 ± 24
Chrysin graphic file with name 41598_2017_11022_Figc_HTML.gif 24 ± 4 >1 mM — —