Target Validation Information
TTD ID T92777
Target Name Intestinal maltase-glucoamylase (MGAM)
Type of Target
Successful
Drug Potency against Target Acarbose Drug Info IC50 = 0.05 mM
1,4-dideoxy-1,4-imino-D-arabinito Drug Info IC50 = 840 nM [1]
2,5-Dideoxy-2,5-imino-D-mannitol Drug Info IC50 = 2000 nM [1]
4'-(p-toluenesulfonamide)-3,4-dihydroxy chalcone Drug Info Ki = 240 nM [2]
De-O-sulfonated kotalanol Drug Info Ki = 30 nM [4]
Deoxynojirimycin Drug Info IC50 = 4600 nM [5]
KOTALANOL Drug Info Ki = 190 nM [4]
PONKORANOL Drug Info Ki = 170 nM [3]
SALACINOL Drug Info Ki = 1000 nM [4]
References
REF 1 New sugar-mimic alkaloids from the pods of Angylocalyx pynaertii. J Nat Prod. 2002 Feb;65(2):198-202.
REF 2 Sulfonamide chalcone as a new class of alpha-glucosidase inhibitors. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5514-6.
REF 3 Probing the active-site requirements of human intestinal N-terminal maltase glucoamylase: the effect of replacing the sulfate moiety by a methyl et... Bioorg Med Chem Lett. 2010 Oct 1;20(19):5686-9.
REF 4 Probing the active-site requirements of human intestinal N-terminal maltase-glucoamylase: Synthesis and enzyme inhibitory activities of a six-membe... Bioorg Med Chem. 2010 Nov 15;18(22):7794-8.
REF 5 Nitrogen-in-the-ring pyranoses and furanoses: structural basis of inhibition of mammalian glycosidases. J Med Chem. 1994 Oct 28;37(22):3701-6.

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