Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T89918 | ||||
Target Name | Glycinamide ribonucleotide formyltransferase (GART) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | 10-trifluoroacetyl-DDACTHF | Drug Info | Ki = 30 nM | [1] | |
DDATHF | Drug Info | IC50 = 780 nM | [3] | ||
Dideazaacyclotetrahydrofolic acid | Drug Info | Ki = 1700 nM | [2] | ||
Dideazafolate | Drug Info | Ki = 2000 nM | [4] | ||
References | |||||
REF 1 | Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase. J Med Chem. 2006 May 18;49(10):2998-3002. | ||||
REF 2 | Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase. J Med Chem. 2008 Sep 11;51(17):5441-8. | ||||
REF 3 | Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis ... J Med Chem. 2010 Feb 11;53(3):1306-18. | ||||
REF 4 | N10-substituted 5,8-dideazafolate inhibitors of glycinamide ribonucleotide transformylase. J Med Chem. 1987 Jul;30(7):1254-6. | ||||
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