Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00187

Target Information
NameTyrosine-protein kinase JAK2    
Type of targetClinical trial target    
SynonymsJAK-2    
Janus kinase 2    
DiseaseHodgkin's disease, unspecified
[ICD9: 201   ICD10: C81]
[1]
Leukemia, unspecified
[ICD9: 208.9   ICD10: C91-C95]
[2]
Vascular disease
[ICD9: 325, 430-459   ICD10: G45-G46, I60-I95]
[3]
Drug(s)BaricitinibPhase IIIRheumatoid arthritis, psoriasis and diabetic nephropathy
INCB018424Phase IIIMyelofibrosis, Polycythemia?vera[4]
INCB18424Phase IIIMyelofibrosis; Psoriasis; Rheumatoid arthritis and Multiple myeloma Prostate cancer[5][6]
PacritinibPhase IIIMyelofibrosis (see also lymphoma)
SAR302503Phase IIIMyelofibrosis
BaricitinibPhase IIDiabetic nephropathy
BaricitinibPhase IIPsoriasis
BaricitinibPhase IIRheumatoid arthritis
INCB28050Phase IIRheumatold arthritis[6]
ITF2357Phase IIMyelofibrosis, Essential thrombocythemia, Polycythemia?vera[4][7]
LY2784544Phase IIMyeloproliferative disorders
LY2784544Phase IIMyeloproliferative neoplasms
RuxolitinibPhase IIEssential thrombocythemia vera (ET),
RuxolitinibPhase IIPOlycythemia vera
RuxolitinibPhase IIPancreatic cancer
SAR302503Phase IIPolycythemia vera, myelofibrosis (combination therapy)
BMS-911543Phase I/IIMyelofibrosis
NS-018Phase I/IIMyelofibrosis
TG101348Phase I/IIMyelofibrosis[4]
AC430Phase ILeukemia
AZD1480Phase ISolid Tumors
JAK2 inhibitorPhase ICancer
SB1578Phase ICancer
XL019Phase IPolycythemia Vera[4]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayAdipocytokine signaling pathway
Chemokine signaling pathway
Jak-STAT signaling pathway
UniProt IDO60674
PDB Structure2B7A; 2W1I; 2XA4; 3E62; 3E63; 3E64; 3FUP; 3IO7; 3IOK; 3JY9; 3KCK; 3KRR; 3LPB; 3Q32; 3RVG; 3TJC; 3TJD; 3UGC; 3ZMM; 4AQC; 4BBE; 4BBF; 4E4M; 4E6D; 4E6Q; 4F08; 4F09; 4FVP; 4FVQ; 4FVR; 4HGE; 4IVA.    
FunctionTyrosine kinase of the non-receptor type, involved in interleukin 3 signal transduction.    
SequenceMGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSG EYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYF PRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLG MAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQF SQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSR GKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLR EALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQT GLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNC YQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKI RNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASM MSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWA MHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVP PECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAEL ANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRD PTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIE ILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQI CKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFW YAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIE LLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
Target ValidationClick to Find Target Validation Information.    
Inhibitor5-phenyl-1H-indazol-3-amine[8]
AG490[3]
CP-690550[9]
INCB018424[4]
INCB18424[5][6]
INCB28050[6]
ITF2357[4][7]
NSC-1771,   Thiram[10]
TG101348[4]
Tyrphostin AG490[2]
XL019[4]
atropisomer 1[11]
MultitargetINCB18424[5][6]
INCB28050[6]
ITF2357[4][7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Molecular basis of targeted chemotherapy: novel concepts with special reference to the treatment of Hodgkin's disease. Ann Oncol. 1998;9 Suppl 5:S125-8. To Reference
Ref 2The JAK2 inhibitor AG490 predominantly abrogates the growth of human B-precursor leukemic cells with 11q23 translocation or Philadelphia chromosome. Leukemia. 2001 Nov;15(11):1758-68. To Reference
Ref 3Jak2 tyrosine kinase mediates oxidative stress-induced apoptosis in vascular smooth muscle cells. J Biol Chem. 2004 Aug 13;279(33):34547-52. Epub 2004 May 24. To Reference
Ref 4Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Jun 24. [Epub ahead of print] To Reference
Ref 5Incyte's Selective JAK1 / 2 Inhibitor, INCB18424, Demonstrates Rapid And Durable Clinical Benefits In Myelofibrosis Patients. Incyte Corporation. 2008 To Reference
Ref 6Incyte. Product Development Pipeline. 2009. To Reference
Ref 7Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. To Reference
Ref 8Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 9Bioorg Med Chem Lett. 2006 Nov 1;16(21):5633-8. Epub 2006 Aug 24.Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3. To Reference
Ref 10Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 11J Med Chem. 2009 Dec 24;52(24):7938-41.Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole. 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