Target Validation Information
TTD ID	T75596
Target Name	Methionine aminopeptidase 2 (METAP2)
Type of Target	Clinical trial
Drug Potency against Target	2-(4-fluorophenylsulfonamido)-1-naphthoic acid	Drug Info	IC50 = 15 nM	[2]
	2-(phenylsulfonamido)-1-naphthoic acid	Drug Info	IC50 = 19 nM	[2]
	2-(phenylsulfonamido)-5-propylbenzoic acid	Drug Info	IC50 = 1100 nM	[2]
	2-(pyridin-2-yl)-1H-benzo[d]imidazol-5-amine	Drug Info	IC50 = 9300 nM
	2-(pyridin-2-yl)-1H-benzo[d]imidazole	Drug Info	IC50 = 13300 nM
	2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine	Drug Info	IC50 = 8000 nM
	2-(thiazol-4-yl)-1H-benzo[d]imidazol-5-amine	Drug Info	IC50 = 10100 nM
	3,5-dimethyl-2-(phenylsulfonamido)benzoic acid	Drug Info	IC50 = 350 nM	[2]
	3-anilino-5-benzylthio-1,2,4-triazole	Drug Info	Ki = 0.5 nM	[4]
	5-bromo-2-(4-chlorophenylsulfonamido)benzoic acid	Drug Info	IC50 = 9100 nM	[2]
	5-butyl-2-(phenylsulfonamido)benzoic acid	Drug Info	IC50 = 10000 nM	[2]
	5-chloro-2-(pyridin-2-yl)-1H-benzo[d]imidazole	Drug Info	IC50 = 18100 nM
	5-ethyl-2-(phenylsulfonamido)benzoic acid	Drug Info	IC50 = 90 nM	[2]
	5-methyl-2-(phenylsulfonamido)benzoic acid	Drug Info	IC50 = 1400 nM	[3]
	5-methyl-2-(pyridin-2-yl)-1H-benzo[d]imidazole	Drug Info	IC50 = 7700 nM
	5-p-Tolyl-1H-[1,2,3]triazole	Drug Info	IC50 = 10 nM	[1]
	OXYQUINOLINE	Drug Info	IC50 = 5600 nM
References
REF 1	4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo. J Med Chem. 2005 Sep 8;48(18):5644-7.
REF 2	Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7.
REF 3	Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of a... J Med Chem. 2006 Jun 29;49(13):3832-49.
REF 4	Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore. J Med Chem. 2007 Aug 9;50(16):3777-85.

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