| 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 530075 | Bioorg 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 552817 | 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. | ||||
| Ref 530577 | Bioorg 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 530076 | Bioorg 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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