Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T52227 | ||||
Target Name | Candida Thymidylate synthase (Candi TMP1) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Fluorouracil | Drug Info | IC50 = 899 nM | [6] | |
Drug Info | IC50 = 100 nM | [1] | |||
Drug Info | IC50 = 19 nM | [3] | |||
1,3-propanediphosphonic acid | Drug Info | Ki = 2700 nM | [4] | ||
3-Amino-5,6-dihydro-2H-benzo[f]quinazolin-1-one | Drug Info | Ki = 7000 nM | [5] | ||
3-Methyl-2H-benzo[f]quinazolin-1-one | Drug Info | Ki = 5400 nM | [5] | ||
PREMETREXED | Drug Info | IC50 = 9500 nM | [2] | ||
References | |||||
REF 1 | Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methy... J Med Chem. 2005 Nov 17;48(23):7215-22. | ||||
REF 2 | Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical ... J Med Chem. 2006 Feb 9;49(3):1055-65. | ||||
REF 3 | Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual th... J Med Chem. 2009 Aug 13;52(15):4892-902. | ||||
REF 4 | Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs. J Med Chem. 2010 Sep 23;53(18):6539-49. | ||||
REF 5 | Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some sulfonamidobenzoylglutamate and related de... J Med Chem. 1993 Oct 29;36(22):3464-71. | ||||
REF 6 | 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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