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. 2019 Nov 11;176(Suppl 1):S297–S396. doi: 10.1111/bph.14752
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2047 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2048 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2049 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2269
Common abbreviation JAK1 JAK2 JAK3 Tyk2
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:6190, http://www.uniprot.org/uniprot/P23458 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:6192, http://www.uniprot.org/uniprot/O60674 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:6193, http://www.uniprot.org/uniprot/P52333 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:12440, http://www.uniprot.org/uniprot/P29597
EC number http://www.genome.jp/dbget‐bin/www_bget?ec:2.7.10.2 http://www.genome.jp/dbget‐bin/www_bget?ec:2.7.10.2 http://www.genome.jp/dbget‐bin/www_bget?ec:2.7.10.2 http://www.genome.jp/dbget‐bin/www_bget?ec:2.7.10.2
Inhibitors http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5688 (pIC50 8.5–10.1) [http://www.ncbi.nlm.nih.gov/pubmed/23061660?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/20130243?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7913 (pIC50 8) [http://www.ncbi.nlm.nih.gov/pubmed/24006460?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7839 (pIC50 9.1) [http://www.ncbi.nlm.nih.gov/pubmed/22829185?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7954 (pIC50 9) [http://www.ncbi.nlm.nih.gov/pubmed/22015772?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7949 (pIC50 8.9) [http://www.ncbi.nlm.nih.gov/pubmed/19143567?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7971 (pIC50 8.7) [http://www.ncbi.nlm.nih.gov/pubmed/23127890?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5716 (pIC50 8.5) [http://www.ncbi.nlm.nih.gov/pubmed/21106455?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/18394554?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7909 (pIC50 8.4) [http://www.ncbi.nlm.nih.gov/pubmed/23584399?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7949 (pIC50 9) [http://www.ncbi.nlm.nih.gov/pubmed/19143567?dopt=AbstractPlus]
Selective inhibitors http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8123 (pIC50 >9) [http://www.ncbi.nlm.nih.gov/pubmed/21493067?dopt=AbstractPlus]
Comments The JAK2V617F mutation, which causes constitutive activation, plays an oncogenic role in the pathogenesis of the myeloproliferative disorders, polycythemia vera, essential thrombocythemia, and idiopathic myelofibrosis [http://www.ncbi.nlm.nih.gov/pubmed/17151367?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/17131059?dopt=AbstractPlus]. Small molecule compounds which inhibit aberrant JAK2 activity are being developed as novel anti‐cancer pharmaceuticals.