Target Validation Information
Target ID T92777
Target Name Maltase-glucoamylase, intestinal
Target Type
Successful
Drug Potency against Target PONKORANOL Drug Info Ki = 170 nM [531131]
De-O-sulfonated kotalanol Drug Info Ki = 30 nM [531230]
SALACINOL Drug Info Ki = 1000 nM [531230]
KOTALANOL Drug Info Ki = 190 nM [531230]
Deoxynojirimycin Drug Info IC50 = 4600 nM [533823]
Acarbose Drug Info IC50 = 0.05 mM
4'-(p-toluenesulfonamide)-3,4-dihydroxy chalcone Drug Info Ki = 240 nM [527781]
1,4-dideoxy-1,4-imino-D-arabinito Drug Info IC50 = 840 nM [526274]
2,5-Dideoxy-2,5-imino-D-mannitol Drug Info IC50 = 2000 nM [526274]
References
Ref 531131Bioorg Med Chem Lett. 2010 Oct 1;20(19):5686-9. Epub 2010 Aug 11.Probing the active-site requirements of human intestinal N-terminal maltase glucoamylase: the effect of replacing the sulfate moiety by a methyl ether in ponkoranol, a naturally occurring |A-glucosidase inhibitor.
Ref 531230Bioorg Med Chem. 2010 Nov 15;18(22):7794-8. Epub 2010 Sep 29.Probing the active-site requirements of human intestinal N-terminal maltase-glucoamylase: Synthesis and enzyme inhibitory activities of asix-membered ring nitrogen analogue of kotalanol and its de-O-sulfonated derivative.
Ref 531230Bioorg Med Chem. 2010 Nov 15;18(22):7794-8. Epub 2010 Sep 29.Probing the active-site requirements of human intestinal N-terminal maltase-glucoamylase: Synthesis and enzyme inhibitory activities of asix-membered ring nitrogen analogue of kotalanol and its de-O-sulfonated derivative.
Ref 531230Bioorg Med Chem. 2010 Nov 15;18(22):7794-8. Epub 2010 Sep 29.Probing the active-site requirements of human intestinal N-terminal maltase-glucoamylase: Synthesis and enzyme inhibitory activities of asix-membered ring nitrogen analogue of kotalanol and its de-O-sulfonated derivative.
Ref 533823J Med Chem. 1994 Oct 28;37(22):3701-6.Nitrogen-in-the-ring pyranoses and furanoses: structural basis of inhibition of mammalian glycosidases.
Ref 527781Bioorg Med Chem Lett. 2005 Dec 15;15(24):5514-6. Epub 2005 Oct 3.Sulfonamide chalcone as a new class of alpha-glucosidase inhibitors.
Ref 526274J Nat Prod. 2002 Feb;65(2):198-202.New sugar-mimic alkaloids from the pods of Angylocalyx pynaertii.
Ref 526274J Nat Prod. 2002 Feb;65(2):198-202.New sugar-mimic alkaloids from the pods of Angylocalyx pynaertii.

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