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Target Report Card

Target Name and Classification

Target ID CHEMBL2971
Preferred Name Tyrosine-protein kinase JAK2
Synonyms JAK-2 | JAK2 | Janus kinase 2 | Tyrosine-protein kinase JAK2
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase jaka family
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase jakb family

Target Components

Component Description Relationship Accession
Tyrosine-protein kinase JAK2 SINGLE PROTEIN O60674

Target Relations

ChEMBL ID Pref Name Target Type

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1795071 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 FDA
CHEMBL2105759 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 PubMed
CHEMBL603469 LESTAURTINIB Tyrosine-protein kinase JAK2 inhibitor 3 PubMed
CHEMBL1078178 MOMELOTINIB Tyrosine-protein kinase JAK2 inhibitor 3 PubMed PubMed
CHEMBL1287853 FEDRATINIB Tyrosine-protein kinase JAK2 inhibitor 3 PubMed
CHEMBL2035187 PACRITINIB Tyrosine-protein kinase JAK2 inhibitor 3 Other PubMed PubMed PubMed
CHEMBL495727 AT-9283 Tyrosine-protein kinase JAK2 inhibitor 2 PubMed PubMed
CHEMBL1231124 AZD-1480 Tyrosine-protein kinase JAK2 inhibitor 2 PubMed PubMed
CHEMBL2107823 GANDOTINIB Tyrosine-protein kinase JAK2 inhibitor 2 PubMed PubMed
CHEMBL3545215 BMS-911543 Tyrosine-protein kinase JAK2 inhibitor 2 PubMed PubMed
CHEMBL3545217 NS-018 Tyrosine-protein kinase JAK2 inhibitor 2 PubMed
CHEMBL1944698 TG-02 Tyrosine-protein kinase JAK2 inhibitor 1 PubMed
CHEMBL3544962 CT-1578 Tyrosine-protein kinase JAK2 inhibitor 1 PubMed PubMed
CHEMBL3544997 LS-104 Tyrosine-protein kinase JAK2 inhibitor 1 PubMed
CHEMBL3545241 AC-430 Tyrosine-protein kinase JAK2 inhibitor 1 Other
CHEMBL3545328 XL-019 Tyrosine-protein kinase JAK2 inhibitor 1 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000096968
Ensembl ENSG00000096968
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0005886 (plasma membrane)
GO:0005901 (caveola)
GO:0005925 (focal adhesion)
GO:0012505 (endomembrane system)
GO:0016020 (membrane)
GO:0016363 (nuclear matrix)
GO:0031234 (extrinsic component of cytoplasmic side of plasma membrane)
GO:0031904 (endosome lumen)
GO:0045121 (membrane raft)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004715 (non-membrane spanning protein tyrosine kinase activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005102 (receptor binding)
GO:0005131 (growth hormone receptor binding)
GO:0005143 (interleukin-12 receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008022 (protein C-terminus binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO:0020037 (heme binding)
GO:0031702 (type 1 angiotensin receptor binding)
GO:0033130 (acetylcholine receptor binding)
GO:0035401 (histone kinase activity (H3-Y41 specific))
GO:0042169 (SH2 domain binding)
GO:0042393 (histone binding)
GO:0042802 (identical protein binding)
GO:0043548 (phosphatidylinositol 3-kinase binding)
GO:0043560 (insulin receptor substrate binding)
GO:0046872 (metal ion binding)
GO:0051428 (peptide hormone receptor binding)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000186 (activation of MAPKK activity)
GO:0002250 (adaptive immune response)
GO:0002376 (immune system process)
GO:0006325 (chromatin organization)
GO:0006468 (protein phosphorylation)
GO:0006915 (apoptotic process)
GO:0006919 (activation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0006979 (response to oxidative stress)
GO:0007165 (signal transduction)
GO:0007167 (enzyme linked receptor protein signaling pathway)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007259 (JAK-STAT cascade)
GO:0007260 (tyrosine phosphorylation of STAT protein)
GO:0007498 (mesoderm development)
GO:0007596 (blood coagulation)
GO:0008284 (positive regulation of cell proliferation)
GO:0008285 (negative regulation of cell proliferation)
GO:0008631 (intrinsic apoptotic signaling pathway in response to oxidative stress)
GO:0009755 (hormone-mediated signaling pathway)
GO:0010667 (negative regulation of cardiac muscle cell apoptotic process)
GO:0010811 (positive regulation of cell-substrate adhesion)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0016477 (cell migration)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0019221 (cytokine-mediated signaling pathway)
GO:0022408 (negative regulation of cell-cell adhesion)
GO:0030041 (actin filament polymerization)
GO:0030154 (cell differentiation)
GO:0030218 (erythrocyte differentiation)
GO:0030335 (positive regulation of cell migration)
GO:0031103 (axon regeneration)
GO:0031959 (mineralocorticoid receptor signaling pathway)
GO:0032024 (positive regulation of insulin secretion)
GO:0032496 (response to lipopolysaccharide)
GO:0032516 (positive regulation of phosphoprotein phosphatase activity)
GO:0032731 (positive regulation of interleukin-1 beta production)
GO:0032760 (positive regulation of tumor necrosis factor production)
GO:0033160 (positive regulation of protein import into nucleus, translocation)
GO:0033194 (response to hydroperoxide)
GO:0033209 (tumor necrosis factor-mediated signaling pathway)
GO:0034612 (response to tumor necrosis factor)
GO:0035409 (histone H3-Y41 phosphorylation)
GO:0035556 (intracellular signal transduction)
GO:0035722 (interleukin-12-mediated signaling pathway)
GO:0038083 (peptidyl-tyrosine autophosphorylation)
GO:0038155 (interleukin-23-mediated signaling pathway)
GO:0042127 (regulation of cell proliferation)
GO:0042531 (positive regulation of tyrosine phosphorylation of STAT protein)
GO:0042976 (activation of Janus kinase activity)
GO:0042981 (regulation of apoptotic process)
GO:0043065 (positive regulation of apoptotic process)
GO:0043388 (positive regulation of DNA binding)
GO:0043392 (negative regulation of DNA binding)
GO:0043524 (negative regulation of neuron apoptotic process)
GO:0045087 (innate immune response)
GO:0045429 (positive regulation of nitric oxide biosynthetic process)
GO:0045597 (positive regulation of cell differentiation)
GO:0045822 (negative regulation of heart contraction)
GO:0046425 (regulation of JAK-STAT cascade)
GO:0046677 (response to antibiotic)
GO:0046777 (protein autophosphorylation)
GO:0048008 (platelet-derived growth factor receptor signaling pathway)
GO:0050727 (regulation of inflammatory response)
GO:0050729 (positive regulation of inflammatory response)
GO:0050731 (positive regulation of peptidyl-tyrosine phosphorylation)
GO:0050867 (positive regulation of cell activation)
GO:0051091 (positive regulation of sequence-specific DNA binding transcription factor activity)
GO:0051770 (positive regulation of nitric-oxide synthase biosynthetic process)
GO:0060333 (interferon-gamma-mediated signaling pathway)
GO:0060334 (regulation of interferon-gamma-mediated signaling pathway)
GO:0060396 (growth hormone receptor signaling pathway)
GO:0060397 (JAK-STAT cascade involved in growth hormone signaling pathway)
GO:0060399 (positive regulation of growth hormone receptor signaling pathway)
GO:0060548 (negative regulation of cell death)
GO:0061180 (mammary gland epithelium development)
GO:0070102 (interleukin-6-mediated signaling pathway)
GO:0070106 (interleukin-27-mediated signaling pathway)
GO:0070671 (response to interleukin-12)
GO:0070757 (interleukin-35-mediated signaling pathway)
GO:0097191 (extrinsic apoptotic signaling pathway)
GO:0097296 (activation of cysteine-type endopeptidase activity involved in apoptotic signaling pathway)
GO:1902728 (positive regulation of growth factor dependent skeletal muscle satellite cell proliferation)
GO:1904037 (positive regulation of epithelial cell apoptotic process)
GO:1904707 (positive regulation of vascular smooth muscle cell proliferation)
Wikipedia Janus_kinase_2

Target Cross References - Protein

canSAR O60674
CGD Thrombocythemia 3
Human Protein Atlas ENSG00000096968
IntAct O60674
Guide to Pharmacology 2048
Open Targets ENSG00000096968
PharmGKB PA29989
Pharos O60674 (Tclin)
Reactome R-HSA-1059683 (Interleukin-6 signaling.)
R-HSA-110056 (MAPK3 (ERK1) activation.)
R-HSA-112411 (MAPK1 (ERK2) activation.)
R-HSA-114604 (GPVI-mediated activation cascade.)
R-HSA-1170546 (Prolactin receptor signaling.)
R-HSA-1433557 (Signaling by SCF-KIT.)
R-HSA-2586552 (Signaling by Leptin.)
R-HSA-3214858 (RMTs methylate histone arginines.)
R-HSA-392451 (G beta:gamma signalling through PI3Kgamma.)
R-HSA-512988 (Interleukin-3, 5 and GM-CSF signaling.)
R-HSA-5673000 (RAF activation.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-6785807 (Interleukin-4 and 13 signaling.)
R-HSA-6788467 (IL-6-type cytokine receptor ligand interactions.)
R-HSA-6802946 (Signaling by moderate kinase activity BRAF mutants.)
R-HSA-6802949 (Signaling by RAS mutants.)
R-HSA-6802952 (Signaling by BRAF and RAF fusions.)
R-HSA-6802955 (Paradoxical activation of RAF signaling by kinase inactive BRAF.)
R-HSA-69231 (Cyclin D associated events in G1.)
R-HSA-877300 (Interferon gamma signaling.)
R-HSA-877312 (Regulation of IFNG signaling.)
R-HSA-8854691 (Interleukin-20 family signaling.)
R-HSA-8984722 (Interleukin-35 Signalling.)
R-HSA-9020591 (Interleukin-12 signaling.)
R-HSA-9020933 (Interleukin-23 signaling.)
R-HSA-9020956 (Interleukin-27 signaling.)
R-HSA-912526 (Interleukin receptor SHC signaling.)
R-HSA-982772 (Growth hormone receptor signaling.)
R-HSA-983231 (Factors involved in megakaryocyte development and platelet production.)
UniProt O14636 O60674 O75297

Target Cross References - Domain

InterPro IPR000299 (FERM_domain.)
IPR000719 (Prot_kinase_dom.)
IPR000980 (SH2.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom_sf.)
IPR011993 (PH-like_dom_sf.)
IPR016251 (Tyr_kinase_non-rcpt_Jak/Tyk2.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR019749 (Band_41_domain.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR020693 (Tyr_kinase_non-rcpt_Jak2.)
IPR035588 (PTK_Jak2_rpt1.)
IPR035589 (PTKc_Jak2_rpt2.)
IPR035860 (JAK2_SH2.)
IPR035963 (FERM_2.)
IPR036860 (SH2_dom_sf.)
IPR037838 (JAK2_FERM_C-lobe.)
Pfam PF00017 (SH2)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 2B7A 2W1I 2XA4 3E62 3E63 3E64 3FUP 3IO7 3IOK 3JY9 3KCK 3KRR 3LPB 3Q32 3RVG 3TJC 3TJD 3UGC 3ZMM 4AQC 4BBE 4BBF 4C61 4C62 More...
CREDO 2B7A 2W1I 2XA4 3E62 3E63 3E64 3FUP 3IO7 3IOK 3JY9 3KCK 3KRR 3LPB 3Q32 3RVG 3TJC 3TJD 3UGC 3ZMM 4AQC 4BBE 4BBF 4C61 4C62 More...