Target Validation Information
TTD ID	T20474
Target Name	DNA topoisomerase (TOP)
Type of Target	Clinical trial
Drug Potency against Target	2-Amino-6-(indan-5-ylamino)-3H-pyrimidin-4-one	Drug Info	Ki = 2000 nM	[2]
	5-Bromo-6-p-tolylamino-1H-pyrimidine-2,4-dione	Drug Info	Ki = 14000 nM	[2]
	6-(3-Bromo-phenylamino)-1H-pyrimidine-2,4-dione	Drug Info	Ki = 10300 nM	[3]
	6-(3-Ethyl-phenylamino)-1H-pyrimidine-2,4-dione	Drug Info	Ki = 2900 nM	[3]
	6-(3-Iodo-phenylamino)-1H-pyrimidine-2,4-dione	Drug Info	Ki = 4700 nM	[3]
	6-(Indan-5-ylamino)-1H-pyrimidine-2,4-dione	Drug Info	Ki = 420 nM	[3]
	6-(Naphthalen-2-ylamino)-1H-pyrimidine-2,4-dione	Drug Info	Ki = 6800 nM	[3]
	6-Benzylamino-1H-pyrimidine-2,4-dione	Drug Info	Ki = 7500 nM	[2]
	6-Benzylamino-5-bromo-1H-pyrimidine-2,4-dione	Drug Info	Ki = 9000 nM	[2]
	6-Benzylamino-5-iodo-1H-pyrimidine-2,4-dione	Drug Info	Ki = 9000 nM	[2]
	6-p-Tolylamino-1H-pyrimidine-2,4-dione	Drug Info	Ki = 17500 nM	[3]
	N*4*-Benzyl-6-chloro-pyrimidine-2,4-diamine	Drug Info	Ki = 17000 nM	[2]
	TOPOSTATIN	Drug Info	IC50 = 17000 nM	[1]
References
REF 1	Isoaurostatin, a novel topoisomerase inhibitor produced by Thermomonospora alba. J Nat Prod. 2001 Feb;64(2):204-7.
REF 2	Inhibitors of Bacillus subtilis DNA polymerase III. Influence of modifications in the pyrimidine ring of anilino- and (benzylamino)pyrimidines. J Med Chem. 1986 May;29(5):676-81.
REF 3	Inhibitors of Bacillus subtilis DNA polymerase III. 6-Anilinouracils and 6-(alkylamino)uracils. J Med Chem. 1980 Jan;23(1):34-8.

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