Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T62460
|
||||
Former ID |
TTDNS00611
|
||||
Target Name |
JAK1
|
||||
Gene Name |
JAK1
|
||||
Synonyms |
Janus kinase 1; Tyrosine-protein kinase JAK1; JAK1
|
||||
Target Type |
Clinical Trial
|
||||
Disease | Essential thrombocythemia [ICD9: 238.71, 289.9; ICD10: D47.3, D75.2, D75.8] | ||||
Malignancies [ICD9: 140-239; ICD10: C00-C96] | |||||
Psoriasis [ICD9: 696; ICD10: L40] | |||||
Polycythemia vera [ICD9: 238.4; ICD10: D45] | |||||
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10: C25] | |||||
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
Rheumatold arthritis; Psoriasis; Diabetic nephropathy [ICD9: 250, 250.4, 580-599, 696, 710-719, 714; ICD10: E08-E13, E10.2, E11.2, E13.2, L40, M00-M25, M05-M06, N00-N29] | |||||
Systemic lupus erythematosus [ICD9: 710; ICD10: M32] | |||||
Function |
Tyrosine kinase of the non-receptor type, involved in theIFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor.
|
||||
BioChemical Class |
Kinase
|
||||
UniProt ID | |||||
EC Number |
EC 2.7.10.2
|
||||
Sequence |
MQYLNIKEDCNAMAFCAKMRSSKKTEVNLEAPEPGVEVIFYLSDREPLRLGSGEYTAEEL
CIRAAQACRISPLCHNLFALYDENTKLWYAPNRTITVDDKMSLRLHYRMRFYFTNWHGTN DNEQSVWRHSPKKQKNGYEKKKIPDATPLLDASSLEYLFAQGQYDLVKCLAPIRDPKTEQ DGHDIENECLGMAVLAISHYAMMKKMQLPELPKDISYKRYIPETLNKSIRQRNLLTRMRI NNVFKDFLKEFNNKTICDSSVSTHDLKVKYLATLETLTKHYGAEIFETSMLLISSENEMN WFHSNDGGNVLYYEVMVTGNLGIQWRHKPNVVSVEKEKNKLKRKKLENKHKKDEEKNKIR EEWNNFSYFPEITHIVIKESVVSINKQDNKKMELKLSSHEEALSFVSLVDGYFRLTADAH HYLCTDVAPPLIVHNIQNGCHGPICTEYAINKLRQEGSEEGMYVLRWSCTDFDNILMTVT CFEKSEQVQGAQKQFKNFQIEVQKGRYSLHGSDRSFPSLGDLMSHLKKQILRTDNISFML KRCCQPKPREISNLLVATKKAQEWQPVYPMSQLSFDRILKKDLVQGEHLGRGTRTHIYSG TLMDYKDDEGTSEEKKIKVILKVLDPSHRDISLAFFEAASMMRQVSHKHIVYLYGVCVRD VENIMVEEFVEGGPLDLFMHRKSDVLTTPWKFKVAKQLASALSYLEDKDLVHGNVCTKNL LLAREGIDSECGPFIKLSDPGIPITVLSRQECIERIPWIAPECVEDSKNLSVAADKWSFG TTLWEICYNGEIPLKDKTLIEKERFYESRCRPVTPSCKELADLMTRCMNYDPNQRPFFRA IMRDINKLEEQNPDIVSEKKPATEVDPTHFEKRFLKRIRDLGEGHFGKVELCRYDPEGDN TGEQVAVKSLKPESGGNHIADLKKEIEILRNLYHENIVKYKGICTEDGGNGIKLIMEFLP SGSLKEYLPKNKNKINLKQQLKYAVQICKGMDYLGSRQYVHRDLAARNVLVESEHQVKIG DFGLTKAIETDKEYYTVKDDRDSPVFWYAPECLMQSKFYIASDVWSFGVTLHELLTYCDS DSSPMALFLKMIGPTHGQMTVTRLVNTLKEGKRLPCPPNCPDEVYQLMRKCWEFQPSNRT SFQNLIEGFEALLK |
||||
Drugs and Mode of Action | |||||
Drug(s) | Ruxolitinib | Drug Info | Phase 4 | Essential thrombocythemia | [523729], [541031] |
ASP-015K | Drug Info | Phase 3 | Psoriasis | [525016], [543066] | |
Baricitinib | Drug Info | Phase 3 | Rheumatold arthritis; Psoriasis; Diabetic nephropathy | [524953], [542743] | |
Ruxolitinib | Drug Info | Phase 3 | Pancreatic cancer | [524723], [541031] | |
ABT-494 | Drug Info | Phase 2 | Rheumatoid arthritis | [525096] | |
GLPG-0634 | Drug Info | Phase 2 | Rheumatoid arthritis | [524620], [542835] | |
GSK2586184 | Drug Info | Phase 2 | Systemic lupus erythematosus | [524199] | |
INCB039110 | Drug Info | Phase 2 | Malignancies | [543090] | |
Ruxolitinib | Drug Info | Approved | High-risk myelofibrosis | [524601], [533122], [541031], [556264] | |
INCB47986 | Drug Info | Discontinued in Phase 2 | Rheumatoid arthritis | [549472] | |
Modulator | ABT-494 | Drug Info | [532777] | ||
Baricitinib | Drug Info | [532777] | |||
GLPG-0634 | Drug Info | [532469], [532777] | |||
GSK2586184 | Drug Info | [533157] | |||
Ruxolitinib | Drug Info | [531783] | |||
Inhibitor | ASP-015K | Drug Info | [543544] | ||
compound 19a | Drug Info | [532598] | |||
INCB039110 | Drug Info | [543544] | |||
INCB47986 | Drug Info | [532777] | |||
WHI-P154 | Drug Info | [529228] | |||
ZM-39923 | Drug Info | [525732] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | PI3K-Akt signaling pathway | ||||
Osteoclast differentiation | |||||
Signaling pathways regulating pluripotency of stem cells | |||||
Jak-STAT signaling pathway | |||||
Leishmaniasis | |||||
Toxoplasmosis | |||||
Tuberculosis | |||||
Hepatitis C | |||||
Hepatitis B | |||||
Measles | |||||
Influenza A | |||||
HTLV-I infection | |||||
Herpes simplex infection | |||||
Epstein-Barr virus infection | |||||
Pathways in cancer | |||||
Viral carcinogenesis | |||||
Pancreatic cancer | |||||
NetPath Pathway | IL2 Signaling Pathway | ||||
PANTHER Pathway | Angiogenesis | ||||
Interferon-gamma signaling pathway | |||||
JAK/STAT signaling pathway | |||||
PDGF signaling pathway | |||||
Pathway Interaction Database | p73 transcription factor network | ||||
IL4-mediated signaling events | |||||
IL27-mediated signaling events | |||||
Signaling events mediated by TCPTP | |||||
SHP2 signaling | |||||
IL2-mediated signaling events | |||||
IL2 signaling events mediated by PI3K | |||||
IFN-gamma pathway | |||||
IL6-mediated signaling events | |||||
PDGFR-alpha signaling pathway | |||||
IL2 signaling events mediated by STAT5 | |||||
Reactome | Interleukin-6 signaling | ||||
MAPK3 (ERK1) activation | |||||
MAPK1 (ERK2) activation | |||||
GPVI-mediated activation cascade | |||||
ISG15 antiviral mechanism | |||||
Interleukin-7 signaling | |||||
gamma signalling through PI3Kgamma | |||||
Interleukin-2 signaling | |||||
RAF/MAP kinase cascade | |||||
Interferon gamma signaling | |||||
Regulation of IFNG signaling | |||||
Interferon alpha/beta signaling | |||||
Interleukin receptor SHC signaling | |||||
Regulation of IFNA signaling | |||||
WikiPathways | Type II interferon signaling (IFNG) | ||||
Interferon type I signaling pathways | |||||
TGF Beta Signaling Pathway | |||||
IL-2 Signaling Pathway | |||||
IL-4 Signaling Pathway | |||||
IL-6 signaling pathway | |||||
TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer | |||||
IL-3 Signaling Pathway | |||||
Interleukin-2 signaling | |||||
Interleukin-7 signaling | |||||
JAK/STAT | |||||
PDGF Pathway | |||||
Oncostatin M Signaling Pathway | |||||
Interleukin-11 Signaling Pathway | |||||
Prostate Cancer | |||||
TSLP Signaling Pathway | |||||
IL-9 Signaling Pathway | |||||
Type III interferon signaling | |||||
IL17 signaling pathway | |||||
IL-7 Signaling Pathway | |||||
Leptin signaling pathway | |||||
TSH signaling pathway | |||||
Integrated Breast Cancer Pathway | |||||
Integrated Cancer pathway | |||||
Interleukin-3, 5 and GM-CSF signaling | |||||
Interferon gamma signaling | |||||
Interferon alpha/beta signaling | |||||
IL-5 Signaling Pathway | |||||
References | |||||
Ref 523729 | ClinicalTrials.gov (NCT01493414) INC424 for Patients With Myelofibrosis, Post Polycythemia Myelofibrosis or Post-essential Thrombocythemia Myelofibrosis. U.S. National Institutes of Health. | ||||
Ref 524199 | ClinicalTrials.gov (NCT01777256) An Adaptive Phase II Study to Evaluate the Efficacy, Pharmacodynamics, Safety and Tolerability of GSK2586184. U.S. National Institutes of Health. | ||||
Ref 524601 | ClinicalTrials.gov (NCT02038036) Ruxolitinib Efficacy and Safety in Patients With HU Resistant or Intolerant Polycythemia Vera vs Best Available Therapy.. U.S. National Institutes of Health. | ||||
Ref 524620 | ClinicalTrials.gov (NCT02048618) Efficacy and Safety of GLPG0634 in Subjects With Active Crohn's Disease. U.S. National Institutes of Health. | ||||
Ref 524723 | ClinicalTrials.gov (NCT02117479) Study of Ruxolitinib in Pancreatic Cancer Patients (Janus 1). U.S. National Institutes of Health. | ||||
Ref 524953 | ClinicalTrials.gov (NCT02265705) A Study of Baricitinib (LY3009104) in Participants With Rheumatoid Arthritis (RA). U.S. National Institutes of Health. | ||||
Ref 525016 | ClinicalTrials.gov (NCT02308163) A Study to Evaluate Safety and Efficacy of ASP015K in Patients With Rheumatoid Arthritis (RA) Who Had an Inadequate Response to DMARDs. U.S. National Institutes of Health. | ||||
Ref 525096 | ClinicalTrials.gov (NCT02365649) A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study of ABT-494 for the Induction of Symptomatic and Endoscopic Remission in Subjects With Moderately to Severely Active Crohn's Disease Who Have Inadequately Responded to or Are Intolerant to Anti-TNF Therapy (Celest Study). U.S. National Institutes of Health. | ||||
Ref 533122 | Ruxolitinib versus standard therapy for the treatment of polycythemia vera. N Engl J Med. 2015 Jan 29;372(5):426-35. | ||||
Ref 541031 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5688). | ||||
Ref 542743 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7792). | ||||
Ref 542835 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7913). | ||||
Ref 543066 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8315). | ||||
Ref 543090 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8364). | ||||
Ref 525732 | Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000 Mar 20;10(6):575-9. | ||||
Ref 529228 | The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7. Epub 2007 Dec 19. | ||||
Ref 532469 | Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013 Oct 1;191(7):3568-77. | ||||
Ref 532598 | Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. J Med Chem. 2014 Jan 9;57(1):144-58. | ||||
Ref 532777 | Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.