Target Validation Information
Target ID T92308
Target Name DNA (cytosine-5)-methyltransferase
Target Type
Successful
Drug Potency against Target S-tubercidinylhomocysteine Drug Info IC50 = 1500 nM [530075]
Azacitidine Drug Info IC50 = 36800 nM [552817]
S-Adenosylhomocysteine Drug Info IC50 = 4000 nM [530577]
(L-)-S-adenosyl-L-homocysteine Drug Info IC50 = 800 nM [530076]
References
Ref 530075Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51. Epub 2009 Mar 28.SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes.
Ref 552817Mechanism of action of key enzymes associated with cancer propagation and their inhibition by various chemotherapeutic agents. Mini Rev Med Chem. 2008 Apr;8(4):388-98.
Ref 530577Bioorg Med Chem. 2010 Jan 15;18(2):822-9. Epub 2009 Nov 27.Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation.
Ref 530076Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6. Epub 2009 Mar 28.Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors.

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