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 552624 | The 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 528716 | J 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 528114 | Bioorg 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 552727 | Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93. | ||||
Ref 528209 | J 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 528209 | J 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 528209 | J 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 528608 | Bioorg 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 528608 | Bioorg 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 530295 | Blood. 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 528209 | J 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 528608 | Bioorg 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 528209 | J 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 528608 | Bioorg 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 528608 | Bioorg 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 528716 | J 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 528608 | Bioorg 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 528209 | J 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 528209 | J 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 528608 | Bioorg 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 552968 | Investigational drugs targeting FLT3 for leukemia. Expert Opin Investig Drugs. 2009 Oct;18(10):1445-56. doi: 10.1517/13543780903179278. | ||||
Ref 552773 | A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358. |
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