Target Validation Information
TTD ID T65501
Target Name DNA [cytosine-5]-methyltransferase 3B (DNMT3B)
Type of Target
Clinical trial
Drug Potency against Target (L-)-S-adenosyl-L-homocysteine Drug Info IC50 = 250 nM [3]
(L-)-S-adenosyl-L-homocysteine Drug Info IC50 = 200 nM [2]
NSC-622445 Drug Info IC50 = 17000 nM [3]
S-tubercidinylhomocysteine Drug Info IC50 = 300 nM [1]
References
REF 1 SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes. Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51.
REF 2 Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors. Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6.
REF 3 Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation. Bioorg Med Chem. 2010 Jan 15;18(2):822-9.

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