Target Validation Information
TTD ID	T74312
Target Name	Fms-like tyrosine kinase 3 (FLT-3)
Type of Target	Successful
Drug Potency against Target	Lestaurtinib	Drug Info	IC50 = 3 nM	[6]
	Sunitinib	Drug Info	IC50 = 25 nM	[9]
	Midostaurin	Drug Info	IC50 = 10 nM	[8]
	Tandutinib	Drug Info	IC50 = 10~100 nM	[7]
	(1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone	Drug Info	IC50 = 3200 nM	[2]
	(1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone	Drug Info	IC50 = 10000 nM	[2]
	(1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone	Drug Info	IC50 = 890 nM	[2]
	(5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone	Drug Info	IC50 = 2300 nM	[2]
	(5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone	Drug Info	IC50 = 570 nM	[2]
	(benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone	Drug Info	IC50 = 400 nM	[3]
	2-(3,4-dimethoxybenzamido)thiophene-3-carboxamide	Drug Info	IC50 = 2100 nM	[1]
	4-(4-aminophenyl)-1H-indazol-3yl-amine	Drug Info	IC50 = 43 nM	[4]
	AG1295	Drug Info	IC50 = 1100 nM	[3]
	Bis(5-acetoxybenzo[b]furan-2-yl)methanone	Drug Info	IC50 = 1700 nM	[3]
	Bis(5-aminobenzo[b]furan-2-yl)methanone	Drug Info	IC50 = 600 nM	[3]
	Bis(5-hydroxybenzo[b]furan-2-yl)methanone	Drug Info	IC50 = 3600 nM	[3]
	Bis(6-hydroxybenzo[b]furan-2-yl)methanone	Drug Info	IC50 = 1800 nM	[3]
	Bis(benzo[b]furan-2-yl)methanone	Drug Info	IC50 = 3500 nM	[3]
	Bis-(5-hydroxy-1H-indol-2-yl)-methanone	Drug Info	IC50 = 33 nM	[2]
	Di(1H-indol-2-yl)methanone	Drug Info	IC50 = 4600 nM	[2]
	N-[4-(3-amino-1H-indazol-4-yl)phenyl]benzamide	Drug Info	IC50 = 694 nM	[4]
	Tandutinib	Drug Info	IC50 = 170 nM	[5]
References
REF 1	Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3282-6.
REF 2	Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15.
REF 3	Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones. Bioorg Med Chem. 2007 Mar 1;15(5):2187-97.
REF 4	Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted ... J Med Chem. 2007 Apr 5;50(7):1584-97.
REF 5	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood. 2009 Oct 1;114(14):2984-92.
REF 6	The effects of lestaurtinib (CEP701) and PKC412 on primary AML blasts: the induction of cytotoxicity varies with dependence on FLT3 signaling in bo... Blood. 2006 Nov 15;108(10):3494-503.
REF 7	Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 8	A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.
REF 9	Investigational drugs targeting FLT3 for leukemia. Expert Opin Investig Drugs. 2009 Oct;18(10):1445-56.

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