Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00090

Target Information
NameFL cytokine receptor    
Type of targetSuccessful target    
SynonymsCD135 antigen    
FLT3 tyrosine kinase    
Receptor tyrosine kinase FLT3    
Stem cell tyrosine kinase 1    
Tyrosine-protein kinase receptor FLT3    
DiseaseAcute myeloid leukemia
[ICD9: 205.0   ICD10: C92.0]
Autoimmune diseases
[ICD9: 279.4   ICD10: D84.9, M35.9]
MLL-rearranged acute lymphoblastic leukemias
[ICD9: 204.0, 208.9   ICD10: C91-C95, C91.0]
Drug(s)PonatinibApprovedChronic, accelerated or blast-phase chronic myeloid leukaemia
SunitinibLaunchedAdvanced renal cell carcinoma[6][7][8][9]
Sunitinib malatePhase IVMetastatic Renal Cell Carcinoma; Gastrointestinal Stromal Tumors[10][11][8]
PacritinibPhase IIIMyelofibrosis (see also lymphoma)
MidostaurinPhase IIColon, breast, CLL, AML, GIST, solid tumours & non-Hodgkin's lymphoma[8][12]
PLX3397Phase IIAcute myeloid leukemia
PLX3397Phase IIGlioblastoma
PLX3397Phase IIGlioblastoma (GBM)
PLX3397Phase IIHodgkin lymphoma
PLX3397Phase IIMetastatic Breast cancer
PLX3397Phase IIMetastatic Prostate cancer
PLX3397Phase IIProstate Caner
QuizartinibPhase IIRelapsed/refractory AML
SunitinibPhase IIAdvanced renal cell carcinoma[6][7][8][9]
Sunitinib malatePhase IISoft Tissue Sarcoma[10][11][8]
TandutinibPhase IIGlioblatoma; Gliosarcoma; Anaplastic Astrocytoma; Anaplastic Oligodendroglioma; Anaplastic Mixed Oligoastrocytoma[8][13]
PLX3397Phase I/IIAcute myelogenous lymphoma (AML)
SU5614Phase I/IIAirway inflammation[7]
4SC-203Phase ISolid tumors[14]
CDX-301Phase IHSC transplantation
MidostaurinPhase IBreast & colorectal cancer[8][12]
TandutinibWithdrawnAcute Myelogenous Leukemia[8][13]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC
PathwayAcute myeloid leukemia
Cytokine-cytokine receptor interaction
Hematopoietic cell lineage
Pathways in cancer
UniProt IDP36888
PDB Structure1RJB; 3QS7; 3QS9.    
FunctionReceptor for the fl cytokine, and has a tyrosine-protein kinase activity.    
Target ValidationClick to Find Target Validation Information.    
Inhibitor (1H-indol-2-yl)[15]
2- (3,4-dimethoxybenzamido)thiophene-3-carboxamide[17]
4- (4-aminophenyl)-1H-indazol-3yl-amine[18]
Bis- (5-hydroxy-1H-indol-2-yl)-methanone[15]
N-[4- (3-amino-1H-indazol-4-yl)phenyl]benzamide[18]
Sunitinib malate[10][11][8]
bis (5-acetoxybenzo[b]furan-2-yl)methanone[16]
bis (5-aminobenzo[b]furan-2-yl)methanone[16]
bis (5-hydroxybenzo[b]furan-2-yl)methanone[16]
bis (6-hydroxybenzo[b]furan-2-yl)methanone[16]
bis (benzo[b]furan-2-yl)methanone[16]
di (1H-indol-2-yl)methanone[15]
Sunitinib malate[10][11][8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Pediatric AML primary samples with FLT3/ITD mutations are preferentially killed by FLT3 inhibition. Blood. 2004 Sep 15;104(6):1841-9. Epub 2004 May 27. To Reference
Ref 2Mutant FLT3 signaling contributes to a block in myeloid differentiation. Leuk Lymphoma. 2005 Dec;46(12):1679-87. To Reference
Ref 3Inhibition of FLT3 signaling targets DCs to ameliorate autoimmune disease. Proc Natl Acad Sci U S A. 2005 Nov 15;102(46):16741-6. Epub 2005 Nov 4. To Reference
Ref 4Inhibition of FLT3 in MLL. Validation of a therapeutic target identified by gene expression based classification. Cancer Cell. 2003 Feb;3(2):173-83. To Reference
Ref 5Biologic and clinical significance of the FLT3 transcript level in acute myeloid leukemia. Blood. 2004 Mar 1;103(5):1901-8. Epub 2003 Nov 6. To Reference
Ref 6FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML. Drug Resist Updat. 2009 Jun;12(3):81-9. Epub 2009 May 20. To Reference
Ref 7FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro. Cancer Res. 2009 Apr 1;69(7):3032-41. Epub 2009 Mar 24. To Reference
Ref 8A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 9Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. To Reference
Ref 10Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 11Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. Epub 2008 Oct 29. To Reference
Ref 12CBL exon 8/9 mutants activate the FLT3 pathway and cluster in core binding factor/11q deletion acute myeloid leukemia/myelodysplastic syndrome subtypes. Clin Cancer Res. 2009 Apr 1;15(7):2238-47. Epub 2009 Mar 10. To Reference
Ref 13Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 142011 Pipeline of 4SC AG. To Reference
Ref 15J 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. To Reference
Ref 16Bioorg 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. To Reference
Ref 17Bioorg 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. To Reference
Ref 18J 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. To Reference
Ref 19Identification of Ki23819, a highly potent inhibitor of kinase activity of mutant FLT3 receptor tyrosine kinase. Leukemia. 2005 Jun;19(6):930-5. To Reference
Ref 20Blood. 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). To Reference


Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.

Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore

All rights reserved.

Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links


Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543