Target Validation Information
Target ID T74312
Target Name FL cytokine receptor
Target Type
Successful
Drug Potency against Target Lestaurtinib Drug Info IC50 = 3 nM [552624]
N-[4-(3-amino-1H-indazol-4-yl)phenyl]benzamide Drug Info IC50 = 694 nM [528716]
2-(3,4-dimethoxybenzamido)thiophene-3-carboxamide Drug Info IC50 = 2100 nM [528114]
Tandutinib Drug Info IC50 = 10~100 nM [552727]
(1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone Drug Info IC50 = 890 nM [528209]
Bis-(5-hydroxy-1H-indol-2-yl)-methanone Drug Info IC50 = 33 nM [528209]
(5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone Drug Info IC50 = 2300 nM [528209]
Bis(5-acetoxybenzo[b]furan-2-yl)methanone Drug Info IC50 = 1700 nM [528608]
Bis(5-hydroxybenzo[b]furan-2-yl)methanone Drug Info IC50 = 3600 nM [528608]
Tandutinib Drug Info IC50 = 170 nM [530295]
(1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone Drug Info IC50 = 3200 nM [528209]
AG1295 Drug Info IC50 = 1100 nM [528608]
Di(1H-indol-2-yl)methanone Drug Info IC50 = 4600 nM [528209]
Bis(5-aminobenzo[b]furan-2-yl)methanone Drug Info IC50 = 600 nM [528608]
Bis(benzo[b]furan-2-yl)methanone Drug Info IC50 = 3500 nM [528608]
4-(4-aminophenyl)-1H-indazol-3yl-amine Drug Info IC50 = 43 nM [528716]
Bis(6-hydroxybenzo[b]furan-2-yl)methanone Drug Info IC50 = 1800 nM [528608]
(5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone Drug Info IC50 = 570 nM [528209]
(1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone Drug Info IC50 = 10000 nM [528209]
(benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone Drug Info IC50 = 400 nM [528608]
Sunitinib Drug Info IC50 = 25 nM [552968]
Midostaurin Drug Info IC50 = 10 nM [552773]
References
Ref 552624The effects of lestaurtinib (CEP701) and PKC412 on primary AML blasts: the induction of cytotoxicity varies with dependence on FLT3 signaling in both FLT3-mutated and wild-type cases. Blood. 2006 Nov 15;108(10):3494-503. Epub 2006 Jul 25.
Ref 528716J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.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 receptor tyrosine kinase inhibitor.
Ref 528114Bioorg Med Chem Lett. 2006 Jun 15;16(12):3282-6. Epub 2006 Mar 31.Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
Ref 552727Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
Ref 528209J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Ref 528209J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Ref 528209J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Ref 528608Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Ref 528608Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Ref 530295Blood. 2009 Oct 1;114(14):2984-92. Epub 2009 Aug 4.AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ref 528209J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Ref 528608Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Ref 528209J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Ref 528608Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Ref 528608Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Ref 528716J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.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 receptor tyrosine kinase inhibitor.
Ref 528608Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Ref 528209J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Ref 528209J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Ref 528608Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Ref 552968Investigational drugs targeting FLT3 for leukemia. Expert Opin Investig Drugs. 2009 Oct;18(10):1445-56. doi: 10.1517/13543780903179278.
Ref 552773A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358.

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