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Target Report Card

Target Name and Classification

Target ID CHEMBL2971
Target Type SINGLE PROTEIN
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 jakb family
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase jaka family

Target Components

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

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3301392 JAK2/TYK2 PROTEIN COMPLEX
CHEMBL3301390 JAK1/JAK2/TYK2 PROTEIN COMPLEX
CHEMBL3038492 JAK2/JAK1 PROTEIN COMPLEX
CHEMBL2363062 Janus Kinase (JAK) PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1795071 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 FDA
CHEMBL603469 LESTAURTINIB Tyrosine-protein kinase JAK2 inhibitor 3 PubMed
CHEMBL1078178 MOMELOTINIB Tyrosine-protein kinase JAK2 inhibitor 3
CHEMBL1287853 FEDRATINIB Tyrosine-protein kinase JAK2 inhibitor 3
CHEMBL2035187 PACRITINIB Tyrosine-protein kinase JAK2 inhibitor 3 Other PubMed PubMed
CHEMBL2105759 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 3
CHEMBL495727 AT-9283 Tyrosine-protein kinase JAK2 inhibitor 2
CHEMBL1231124 AZD-1480 Tyrosine-protein kinase JAK2 inhibitor 2 PubMed PubMed
CHEMBL2107823 GANDOTINIB Tyrosine-protein kinase JAK2 inhibitor 2 PubMed
CHEMBL3545024 INCB-39110 Tyrosine-protein kinase JAK2 2
CHEMBL3545215 BMS-911543 Tyrosine-protein kinase JAK2 inhibitor 2 PubMed
CHEMBL3545217 NS-018 Tyrosine-protein kinase JAK2 inhibitor 2 PubMed
CHEMBL1944698 TG-02 Tyrosine-protein kinase JAK2 inhibitor 1
CHEMBL3544962 CT-1578 Tyrosine-protein kinase JAK2 inhibitor 1
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
More...

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:0005901 (caveola)
GO:0012505 (endomembrane system)
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:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004715 (non-membrane spanning protein tyrosine kinase activity)
GO:0005102 (receptor binding)
GO:0005131 (growth hormone receptor binding)
GO:0005143 (interleukin-12 receptor binding)
GO:0005524 (ATP binding)
GO:0019901 (protein kinase binding)
GO:0020037 (heme binding)
GO:0035401 (histone kinase activity (H3-Y41 specific))
GO:0042169 (SH2 domain binding)
GO:0042393 (histone binding)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000186 (activation of MAPKK activity)
GO:0002250 (adaptive immune response)
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:0006928 (cellular component movement)
GO:0006928 (movement of cell or subcellular component)
GO:0007165 (signal transduction)
GO:0007167 (enzyme linked receptor protein signaling pathway)
GO:0007173 (epidermal growth factor receptor 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:0007262 (STAT protein import into nucleus)
GO:0007264 (small GTPase mediated signal transduction)
GO:0007265 (Ras protein signal transduction)
GO:0007411 (axon guidance)
GO:0007498 (mesoderm development)
GO:0007596 (blood coagulation)
GO:0008284 (positive regulation of cell proliferation)
GO:0008285 (negative regulation of cell proliferation)
GO:0008286 (insulin receptor signaling pathway)
GO:0008543 (fibroblast growth factor receptor signaling pathway)
GO:0008631 (intrinsic apoptotic signaling pathway in response to oxidative stress)
GO:0008636 (activation of caspase activity by protein phosphorylation)
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 cascade)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
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:0034050 (host programmed cell death induced by symbiont)
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:0038095 (Fc-epsilon receptor signaling pathway)
GO:0042127 (regulation of cell proliferation)
GO:0042503 (tyrosine phosphorylation of Stat3 protein)
GO:0042506 (tyrosine phosphorylation of Stat5 protein)
GO:0042508 (tyrosine phosphorylation of Stat1 protein)
GO:0042517 (positive regulation of tyrosine phosphorylation of Stat3 protein)
GO:0042523 (positive regulation of tyrosine phosphorylation of Stat5 protein)
GO:0042977 (activation of JAK2 kinase activity)
GO:0042981 (regulation of apoptotic process)
GO:0043065 (positive regulation of apoptosis)
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:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046677 (response to antibiotic)
GO:0046777 (protein autophosphorylation)
GO:0048008 (platelet-derived growth factor receptor signaling pathway)
GO:0048010 (vascular endothelial growth factor receptor signaling pathway)
GO:0048011 (neurotrophin TRK 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:0051773 (positive regulation of nitric-oxide synthase 2 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:0061180 (mammary gland epithelium development)
GO:0070671 (response to interleukin-12)
GO:0071222 (cellular response to lipopolysaccharide)
GO:0071549 (cellular response to dexamethasone stimulus)
GO:0097191 (extrinsic apoptotic signaling pathway)
GO:0097296 (activation of cysteine-type endopeptidase activity involved in apoptotic signaling pathway)
Wikipedia Janus_kinase_2

Target Cross References - Protein

canSAR O60674
CGD Thrombocythemia 3
Human Protein Atlas ENSG00000096968
IntAct O60674
PharmGKB PA29989
UniProt O14636 O60674 O75297

Target Cross References - Domain

InterPro IPR000299 (FERM_domain.)
IPR000719 (Prot_kinase_cat_dom.)
IPR000719 (Prot_kinase_dom.)
IPR000980 (SH2.)
IPR001245 (Ser-Thr/Tyr-Pkinase.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR008266 (Tyr_kinase_AS.)
IPR008266 (Tyr_prot_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR016251 (Tyr_kinase_non-rcpt_Jak/Tyk2.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR019748 (FERM_central.)
IPR019749 (Band_41_domain.)
IPR020635 (Tyr_Pkinase_cat_dom.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR020693 (Tyr_kinase_non-rcpt_Jak2.)
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...
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