Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T92308 | ||||
Target Name | DNA [cytosine-5]-methyltransferase (DNMT) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Azacitidine | Drug Info | IC50 = 36800 nM | [4] | |
(L-)-S-adenosyl-L-homocysteine | Drug Info | IC50 = 4000 nM | [3] | ||
(L-)-S-adenosyl-L-homocysteine | Drug Info | IC50 = 800 nM | [2] | ||
S-tubercidinylhomocysteine | Drug Info | IC50 = 1500 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. | ||||
REF 4 | Mechanism 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. | ||||
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