Janus kinase 2

Target id: 2048

Nomenclature: Janus kinase 2

Abbreviated Name: JAK2

Family: Janus kinase (JakA) family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Janus kinase 2 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1132 9p24 JAK2 Janus kinase 2
Mouse - 1132 19 C1 Jak2 Janus kinase 2
Rat - 1132 1 q51-q53 Jak2 Janus kinase 2
Previous and Unofficial Names
Database Links
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structural basis of Jak2 inhibition by the type II inhibtor NVP-BBT594
Ligand:  NVP-BBT594
Resolution:  1.34Å
Species:  Human
References:  2
Image of receptor 3D structure from RCSB PDB
Description:  Discovery of 1-Methyl-1H-imidazole Derivatives as Potent Jak2 Inhibitors
PDB Id:  4C61
Ligand:  compound 19a [PMID: 24359159]
Resolution:  2.45Å
Species:  Human
References:  30
Image of receptor 3D structure from RCSB PDB
Description:  The structural basis of Janus Kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor (pyridone 6)
PDB Id:  2B7A
Ligand:  JAK inhibitor I
Resolution:  2.0Å
Species:  Human
References:  21
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
AZ960 Hs Inhibition 9.4 pKi 16
pKi 9.4 (Ki 4.5x10-10 M) [16]
delgocitinib Hs Inhibition 8.8 pKi 31
pKi 8.8 (Ki 1.7x10-9 M) [31]
Description: In an assay using the kinase domain of the recombinant human enzyme, a biotinylated peptide substrate, and [33P]ATP.
HG-10-102-01 Hs Inhibition <5.5 pKi 6
pKi <5.5 (Ki >3.2x10-6 M) [6]
NS-018 Hs Inhibition 9.1 pIC50 24
pIC50 9.1 (IC50 7.2x10-10 M) [24]
ruxolitinib Hs Inhibition 8.6 – 9.6 pIC50 17,27
pIC50 8.6 – 9.6 (IC50 2.8x10-9 – 2.4x10-10 M) [17,27]
JAK inhibitor I Hs Inhibition 9.0 pIC50 32
pIC50 9.0 (IC50 1x10-9 M) [32]
BMS-911543 Hs Inhibition 9.0 pIC50 26
pIC50 9.0 (IC50 1x10-9 M) [26]
compound 1d [PMID: 21493067] Hs Inhibition >9.0 pIC50 34
pIC50 >9.0 (IC50 <1x10-9 M) [34]
AT-9283 Hs Inhibition 8.9 pIC50 19
pIC50 8.9 (IC50 1.2x10-9 M) [19]
CEP-33779 Hs Inhibition 8.7 pIC50 11
pIC50 8.7 (IC50 1.8x10-9 M) [11]
XL019 Hs Inhibition 8.7 pIC50 12
pIC50 8.7 (IC50 2.2x10-9 M) [12]
fedratinib Hs Inhibition 8.5 pIC50 23,35
pIC50 8.5 (IC50 3x10-9 M) [23,35]
compound 19a [PMID: 24359159] Hs Inhibition >8.5 pIC50 30
pIC50 >8.5 (IC50 <3x10-9 M) [30]
gandotinib Hs Inhibition 8.4 pIC50 22
pIC50 8.4 (IC50 4x10-9 M) [22]
baricitinib Hs Inhibition 8.2 pIC50 13
pIC50 8.2 (IC50 5.7x10-9 M) [13]
cerdulatinib Hs Inhibition 8.2 pIC50 9
pIC50 8.2 (IC50 6x10-9 M) [9]
AZD1480 Hs Inhibition 8.1 pIC50 16
pIC50 8.1 (IC50 8x10-9 M) [16]
oclacitinib Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.75x10-8 M) [3]
momelotinib Hs Inhibition 7.7 pIC50 25
pIC50 7.7 (IC50 1.8x10-8 M) [25]
pacritinib Hs Inhibition 7.6 pIC50 36
pIC50 7.6 (IC50 2.3x10-8 M) [36]
decernotinib Hs Inhibition 7.6 pIC50 8
pIC50 7.6 (IC50 2.4x10-8 M) [8]
filgotinib Hs Inhibition 7.5 pIC50 33
pIC50 7.5 (IC50 2.8x10-8 M) [33]
TG02 Hs Inhibition 7.1 – 7.7 pIC50 15,37
pIC50 7.1 – 7.7 (IC50 7.3x10-8 – 1.9x10-8 M) [15,37]
RGB-286638 Hs Inhibition 7.3 pIC50 7
pIC50 7.3 (IC50 5x10-8 M) [7]
solcitinib Hs Inhibition 7.2 pIC50 4
pIC50 7.2 (IC50 6.7x10-8 M) [4]
itacitinib Hs Inhibition <7.0 pIC50 20
pIC50 <7.0 (IC50 >1x10-7 M) [20]
JAK3 inhibitor II Hs Inhibition <5.0 pIC50 5
pIC50 <5.0 (IC50 >1x10-5 M) [5]
AC430 Hs Inhibition - - 18
Inhibitor Comments
Pacritinib inhibits JAK2V617F mutant with an IC50 of 19nM [36].
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 10,38

Key to terms and symbols Click column headers to sort
Target used in screen: JAK2(JH1domain-catalytic)
Ligand Sp. Type Action Affinity Units
ruxolitinib Hs Inhibitor Inhibition 10.4 pKd
tofacitinib Hs Inhibitor Inhibition 9.2 pKd
fedratinib Hs Inhibitor Inhibition 9.0 pKd
tamatinib Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Hs Inhibitor Inhibition 8.4 pKd
staurosporine Hs Inhibitor Inhibition 8.0 pKd
JNJ-28312141 Hs Inhibitor Inhibition 8.0 pKd
PP-242 Hs Inhibitor Inhibition 8.0 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.8 pKd
KW-2449 Hs Inhibitor Inhibition 7.1 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.


Reference: 1,14

Key to terms and symbols Click column headers to sort
Target used in screen: JAK2/JAK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
JAK inhibitor I Hs Inhibitor Inhibition 1.4 -1.0 1.0
staurosporine Hs Inhibitor Inhibition 1.9 0.0 -1.5
K-252a Hs Inhibitor Inhibition 3.0 2.0 -1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 3.2 2.0 0.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 4.2 3.0 -1.0
tofacitinib Hs Inhibitor Inhibition 5.1
Gö 6976 Hs Inhibitor Inhibition 5.6 4.0 3.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 7.2 4.0 0.0
midostaurin Hs Inhibitor Inhibition 8.9 7.0 2.0
SB 218078 Hs Inhibitor Inhibition 14.2 86.0 82.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
CEP-33779, a selective JAK2 inhibitor has demonstrated efficacy in mouse models of rheumatoid arthritis [29] and colitis-induced colorectal cancer [28].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process ID:  2
GO Annotation:  Associated to GO processes
GO Processes:  innate immune response (GO:0045087) IBA
regulation of inflammatory response (GO:0050727) IDA
positive regulation of inflammatory response (GO:0050729) IEA
interferon-gamma-mediated signaling pathway (GO:0060333) TAS
regulation of interferon-gamma-mediated signaling pathway (GO:0060334) TAS
Immuno Process:  Immune regulation
Immuno Process ID:  6
GO Annotation:  Associated to GO processes
GO Processes:  erythrocyte differentiation (GO:0030218) ISS
regulation of inflammatory response (GO:0050727) IDA
positive regulation of inflammatory response (GO:0050729) IEA
regulation of interferon-gamma-mediated signaling pathway (GO:0060334) TAS
Immuno Process:  Immune system development
Immuno Process ID:  8
GO Annotation:  Associated to GO processes
GO Processes:  erythrocyte differentiation (GO:0030218) ISS
Immuno Process:  Cytokine production & signalling
Immuno Process ID:  9
GO Annotation:  Associated to GO processes
GO Processes:  cytokine-mediated signaling pathway (GO:0019221) IDA
positive regulation of interleukin-1 beta production (GO:0032731) IEA
positive regulation of tumor necrosis factor production (GO:0032760) ISS
tumor necrosis factor-mediated signaling pathway (GO:0033209) IDA
response to tumor necrosis factor (GO:0034612) IDA
interleukin-12-mediated signaling pathway (GO:0035722) IDA
interferon-gamma-mediated signaling pathway (GO:0060333) TAS
regulation of interferon-gamma-mediated signaling pathway (GO:0060334) TAS
response to interleukin-12 (GO:0070671) IDA
Immuno Process:  T cell (activation)
Immuno Process ID:  4
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  adaptive immune response (GO:0002250) IEA
Immuno Process:  B cell (activation)
Immuno Process ID:  5
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  adaptive immune response (GO:0002250) IEA
Clinically-Relevant Mutations and Pathophysiology
Disease:  Acute myeloid leukemia
Synonyms: Acute myelogenous leukemia
Disease Ontology: DOID:9119
OMIM: 601626
Orphanet: ORPHA519
Disease:  Budd-Chiari syndrome
OMIM: 600880
Orphanet: ORPHA131
Disease:  Familial thrombocytosis
Description: A rare chronic myeloproliferative neoplasm (MPN) causing overproduction of platelets.
Synonyms: essential thrombocythaemia
hemorrhagic thrombocythemia
hereditary thrombocythemia
primary thrombocytosis
Disease Ontology: DOID:2224
Orphanet: ORPHA71493
Disease:  Myelofibrosis
Synonyms: Myelofibrosis with myeloid metaplasia [Orphanet: ORPHA824]
Disease Ontology: DOID:4971
OMIM: 254450
Orphanet: ORPHA824
Disease:  Polycythemia vera
Disease Ontology: DOID:8997
OMIM: 263300
Orphanet: ORPHA729
Disease:  Thrombocythemia 3; THCYT3
Synonyms: Essential thrombocythemia [Orphanet: ORPHA3318]
Essential thrombocytosis [Orphanet: ORPHA3318]
OMIM: 614521
Orphanet: ORPHA3318


Show »

1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1039-45. [PMID:22037377]

2. Andraos R, Qian Z, Bonenfant D, Rubert J, Vangrevelinghe E, Scheufler C, Marque F, Régnier CH, De Pover A, Ryckelynck H et al.. (2012) Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent. Cancer Discov2 (6): 512-23. [PMID:22684457]

3. Berlinski PJ, Birchmeier MJ, Bowman JW, Gonzales AJ, Kamerling SG, Mann DW, Mitton-Fry MJ. (2010) Pyrrolo[2,3-d]pyrimidine compounds. Patent number: WO2010020905. Assignee: Pfizer Inc.. Priority date: 20/08/2008. Publication date: 25/02/2010.

4. Blanc J. (2010) Novel compound useful for the treatment of degenerative and inflammatory diseases. Patent number: WO2010149771. Assignee: Galapagos Nv, Menet, Christel Jeanne Marie. Priority date: 26/06/2009. Publication date: 29/12/2010.

5. Changelian PS, Moshinsky D, Kuhn CF, Flanagan ME, Munchhof MJ, Harris TM, Whipple DA, Doty JL, Sun J, Kent CR et al.. (2008) The specificity of JAK3 kinase inhibitors. Blood111 (4): 2155-7. [PMID:18094329]

6. Chen H, Chan BK, Drummond J, Estrada AA, Gunzner-Toste J, Liu X, Liu Y, Moffat J, Shore D, Sweeney ZK et al.. (2012) Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling. J. Med. Chem.55 (11): 5536-45. [PMID:22591441]

7. Cirstea D, Hideshima T, Santo L, Eda H, Mishima Y, Nemani N, Hu Y, Mimura N, Cottini F, Gorgun G et al.. (2013) Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia27 (12): 2366-75. [PMID:23807770]

8. Clark JD, Flanagan ME, Telliez JB. (2014) Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases. J. Med. Chem.57 (12): 5023-38. [PMID:24417533]

9. Coffey G, Betz A, DeGuzman F, Pak Y, Inagaki M, Baker DC, Hollenbach SJ, Pandey A, Sinha U. (2014) The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J. Pharmacol. Exp. Ther.351 (3): 538-48. [PMID:25253883]

10. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1046-51. [PMID:22037378]

11. Dugan BJ, Gingrich DE, Mesaros EF, Milkiewicz KL, Curry MA, Zulli AL, Dobrzanski P, Serdikoff C, Jan M, Angeles TS et al.. (2012) A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. J. Med. Chem.55 (11): 5243-54. [PMID:22594690]

12. Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H et al.. (2012) SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg. Med. Chem. Lett.22 (24): 7653-8. [PMID:23127890]

13. Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF et al.. (2010) Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J. Immunol.184 (9): 5298-307. [PMID:20363976]

14. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J.451 (2): 313-28. [PMID:23398362]

15. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al.. (2012) TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Leukemia26 (2): 236-43. [PMID:21860433]

16. Gozgit JM, Bebernitz G, Patil P, Ye M, Parmentier J, Wu J, Su N, Wang T, Ioannidis S, Davies A et al.. (2008) Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J. Biol. Chem.283 (47): 32334-43. [PMID:18775810]

17. Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA et al.. (2012) Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. J. Med. Chem.55 (22): 10090-107. [PMID:23061660]

18. Holladay MW, Setti E. (2014) Optically active pyrazolylaminoquinazoline, and pharmaceutical compositions and methods of use thereof. Patent number: US8703943. Assignee: Ambit Biosciences Corporation. Priority date: 01/09/2010. Publication date: 22/04/2014.

19. Howard S, Berdini V, Boulstridge JA, Carr MG, Cross DM, Curry J, Devine LA, Early TR, Fazal L, Gill AL et al.. (2009) Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J. Med. Chem.52 (2): 379-88. [PMID:19143567]

20. Huang T, Xue C-B, Wang A, Kong L, Ye HF, Yao W, Rodgers JD, Shepard S, Wang H, Shao L et al.. (2011) Piperidin-4-yl azetidine derivatives as jak1 inhibitors. Patent number: WO2011112662. Assignee: Incyte Corporation. Priority date: 10/03/2010. Publication date: 15/09/2011.

21. Lucet IS, Fantino E, Styles M, Bamert R, Patel O, Broughton SE, Walter M, Burns CJ, Treutlein H, Wilks AF et al.. (2006) The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor. Blood107 (1): 176-83. [PMID:16174768]

22. Ma L, Clayton JR, Walgren RA, Zhao B, Evans RJ, Smith MC, Heinz-Taheny KM, Kreklau EL, Bloem L, Pitou C et al.. (2013) Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F. Blood Cancer J3: e109. [PMID:23584399]

23. Malerich JP, Lam JS, Hart B, Fine RM, Klebansky B, Tanga MJ, D'Andrea A. (2010) Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3. Bioorg. Med. Chem. Lett.20 (24): 7454-7. [PMID:21106455]

24. Nakaya Y, Shide K, Niwa T, Homan J, Sugahara S, Horio T, Kuramoto K, Kotera T, Shibayama H, Hori K et al.. (2011) Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J1 (7): e29. [PMID:22829185]

25. Pardanani A, Lasho T, Smith G, Burns CJ, Fantino E, Tefferi A. (2009) CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia23 (8): 1441-5. [PMID:19295546]

26. Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL et al.. (2012) Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia.26 (2): 280-8. [PMID:22015772]

27. Quintás-Cardama A, Vaddi K, Liu P, Manshouri T, Li J, Scherle PA, Caulder E, Wen X, Li Y, Waeltz P et al.. (2010) Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood115 (15): 3109-17. [PMID:20130243]

28. Seavey MM, Lu LD, Stump KL, Wallace NH, Hockeimer W, O'Kane TM, Ruggeri BA, Dobrzanski P. (2012) Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Mol. Cancer Ther.11 (4): 984-93. [PMID:22334590]

29. Stump KL, Lu LD, Dobrzanski P, Serdikoff C, Gingrich DE, Dugan BJ, Angeles TS, Albom MS, Ator MA, Dorsey BD et al.. (2011) A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis. Arthritis Res. Ther.13 (2): R68. [PMID:21510883]

30. Su Q, Ioannidis S, Chuaqui C, Almeida L, Alimzhanov M, Bebernitz G, Bell K, Block M, Howard T, Huang S et al.. (2013) Discovery of 1-Methyl-1H-imidazole Derivatives as Potent Jak2 Inhibitors. J. Med. Chem.,  [Epub ahead of print]. [PMID:24359159]

31. Tanimoto A, Ogawa Y, Oki C, Kimoto Y, Nozawa K, Amano W, Noji S, Shiozaki M, Matsuo A, Shinozaki Y et al.. (2015) Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo. Inflamm. Res.64 (1): 41-51. [PMID:25387665]

32. Thompson JE, Cubbon RM, Cummings RT, Wicker LS, Frankshun R, Cunningham BR, Cameron PM, Meinke PT, Liverton N, Weng Y et al.. (2002) Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg. Med. Chem. Lett.12 (8): 1219-23. [PMID:11934592]

33. Van Rompaey L, Galien R, van der Aar EM, Clement-Lacroix P, Nelles L, Smets B, Lepescheux L, Christophe T, Conrath K, Vandeghinste N et al.. (2013) Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J. Immunol.191 (7): 3568-77. [PMID:24006460]

34. Wang T, Ioannidis S, Almeida L, Block MH, Davies AM, Lamb ML, Scott DA, Su M, Zhang HJ, Alimzhanov M et al.. (2011) In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. Bioorg. Med. Chem. Lett.21 (10): 2958-61. [PMID:21493067]

35. Wernig G, Kharas MG, Okabe R, Moore SA, Leeman DS, Cullen DE, Gozo M, McDowell EP, Levine RL, Doukas J et al.. (2008) Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell13 (4): 311-20. [PMID:18394554]

36. William AD, Lee AC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Tan E, Chen D, Williams M, Sun ET et al.. (2011) Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma. J. Med. Chem.54 (13): 4638-58. [PMID:21604762]

37. William AD, Lee AC, Goh KC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Lee CP, Wang H, Williams M et al.. (2012) Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer. J. Med. Chem.55 (1): 169-96. [PMID:22148278]

38. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol.17 (11): 1241-9. [PMID:21095574]

How to cite this page

Janus kinase (JakA) family: Janus kinase 2. Last modified on 10/11/2017. Accessed on 24/02/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2048.