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Table 3Compound representatives of initial hit series

Isofagomine is an imino sugar previously reported to chaperone glucocerebrosidase. NCGC00092410 is a non-imino sugar previously reported to inhibit purified glucocerebrosidase.

CompoundSeries (PubChem CID)TypePurified N370SPurified WTSpleen N370SSpleen WT
Isofagomine447607Inhibitor50–60nM10–15nM70–80nM100nM
NCGC00092410Quinoline

5067281
Inhibitor560–1000nM70–80nM> 10μM> 10μM
MLS000393962Quinazoline

2477651
InhibitorInactive1.6–2.5μM450nM1000nM
NCGC00159568Thiourea

9893924
Inhibitor2500μM710nM580nM350nM

From: Identification of Modulators of the N370S Mutant Form of Glucocerebrosidase as a Potential Therapy for Gaucher Disease - Chemotype 2

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

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