Page last updated: 2024-08-07 16:49:15
Tyrosine-protein kinase JAK3
A tyrosine-protein kinase JAK3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P52333]
Synonyms
EC 2.7.10.2;
Janus kinase 3;
JAK-3;
Leukocyte janus kinase;
L-JAK
Research
Bioassay Publications (150)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 27 (18.00) | 29.6817 |
| 2010's | 91 (60.67) | 24.3611 |
| 2020's | 32 (21.33) | 2.80 |
Compounds (134)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| whi p154 | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
| 1-(2-naphthalenyl)-3-[(phenylmethyl)-propan-2-ylamino]-1-propanone | Homo sapiens (human) | IC50 | 9.0400 | 2 | 2 |
| 1-(2-naphthalenyl)-2-propen-1-one | Homo sapiens (human) | IC50 | 12,589,300,000,000.0000 | 1 | 1 |
| staurosporine aglycone | Homo sapiens (human) | IC50 | 0.0610 | 1 | 1 |
| beta-lapachone | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
| vitamin k 3 | Homo sapiens (human) | IC50 | 2.2000 | 1 | 1 |
| pd168393 | Homo sapiens (human) | IC50 | 6.5700 | 2 | 2 |
| sb 202190 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| pyrazolanthrone | Homo sapiens (human) | IC50 | 0.9570 | 2 | 2 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0084 | 15 | 15 |
| dehydroabietic acid | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| canertinib | Homo sapiens (human) | IC50 | 2.9400 | 2 | 2 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| nsc 95397 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| ag-213 | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| sulfuretin | Homo sapiens (human) | IC50 | 4.2600 | 1 | 1 |
| rottlerin | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| ag-490 | Homo sapiens (human) | IC50 | 79,432,800,000.0000 | 1 | 1 |
| palbociclib | Homo sapiens (human) | IC50 | 0.0631 | 1 | 1 |
| 2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-one | Homo sapiens (human) | IC50 | 0.0902 | 8 | 11 |
| gw-5074 | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| a 770041 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | GI50 | 0.5030 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | IC50 | 0.1469 | 63 | 75 |
| tofacitinib | Homo sapiens (human) | Ki | 0.0004 | 6 | 6 |
| sotrastaurin | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| l 783277 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| brivanib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pf 00299804 | Homo sapiens (human) | IC50 | 1,786.7850 | 2 | 2 |
| crizotinib | Homo sapiens (human) | IC50 | 1.3600 | 1 | 1 |
| 4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide | Homo sapiens (human) | Ki | 4.0000 | 1 | 1 |
| N-(2,4-dimethoxyphenyl)-N-[2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]carbamic acid (2,6-dimethylphenyl) ester | Homo sapiens (human) | IC50 | 0.4870 | 1 | 4 |
| dactolisib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| mf63 compound | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 4-methyl-3-(2-(2-morpholinoethylamino)quinazolin-6-yl)-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 0.0720 | 1 | 1 |
| azd 1480 | Homo sapiens (human) | IC50 | 1.3600 | 1 | 1 |
| fedratinib | Homo sapiens (human) | IC50 | 0.3917 | 3 | 3 |
| fedratinib | Homo sapiens (human) | Ki | 1.0020 | 1 | 1 |
| amg 458 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | IC50 | 0.0411 | 10 | 10 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | Homo sapiens (human) | IC50 | 0.1445 | 2 | 2 |
| az 960 | Homo sapiens (human) | GI50 | 0.3500 | 1 | 1 |
| az 960 | Homo sapiens (human) | IC50 | 0.0090 | 1 | 1 |
| defactinib | Homo sapiens (human) | IC50 | 0.5574 | 2 | 1 |
| incb-018424 | Homo sapiens (human) | IC50 | 0.7566 | 19 | 19 |
| incb-018424 | Homo sapiens (human) | Ki | 0.0032 | 3 | 3 |
| entrectinib | Homo sapiens (human) | IC50 | 0.3490 | 1 | 1 |
| baricitinib | Homo sapiens (human) | IC50 | 1.1256 | 11 | 11 |
| 4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide | Homo sapiens (human) | IC50 | 0.0080 | 2 | 2 |
| abt-348 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sb 1518 | Homo sapiens (human) | IC50 | 0.5200 | 2 | 2 |
| nvp-bsk805 | Homo sapiens (human) | IC50 | 0.6100 | 1 | 1 |
| gsk143 | Homo sapiens (human) | IC50 | 1.9953 | 1 | 1 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| glpg0634 | Homo sapiens (human) | GI50 | 10.0000 | 1 | 1 |
| glpg0634 | Homo sapiens (human) | IC50 | 3.5867 | 12 | 12 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| delgocitinib | Homo sapiens (human) | IC50 | 0.0220 | 3 | 3 |
| bms-911543 | Homo sapiens (human) | IC50 | 0.7833 | 3 | 3 |
| pf 956980 | Homo sapiens (human) | IC50 | 0.0564 | 3 | 3 |
| cep 33779 | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
| ceritinib | Homo sapiens (human) | IC50 | 7.9200 | 1 | 1 |
| cc-292 | Homo sapiens (human) | IC50 | 0.4626 | 4 | 4 |
| vx-509 | Homo sapiens (human) | IC50 | 0.1743 | 4 | 4 |
| vx-509 | Homo sapiens (human) | Ki | 0.0078 | 2 | 2 |
| chr-6494 | Homo sapiens (human) | IC50 | 0.1190 | 1 | 1 |
| acp-196 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| bmx-in-1 | Homo sapiens (human) | IC50 | 0.1750 | 1 | 1 |
| 9-(1-methyl-4-pyrazolyl)-1-[1-(1-oxoprop-2-enyl)-2,3-dihydroindol-6-yl]-2-benzo[h][1,6]naphthyridinone | Homo sapiens (human) | IC50 | 4.2580 | 2 | 2 |
| at 9283 | Homo sapiens (human) | IC50 | 0.0011 | 4 | 4 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tofacitinib | Homo sapiens (human) | fIC50 | 0.0750 | 2 | 2 |
| tofacitinib | Homo sapiens (human) | IC90 | 0.1600 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | INH | 0.0030 | 1 | 1 |
| baricitinib | Homo sapiens (human) | INH | 0.1800 | 1 | 1 |
Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 27, Issue:18, 2017
Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.Chemistry & biology, , Sep-22, Volume: 15, Issue:9, 2008
Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38α MAPK, CK1δ and JAK2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1ACS medicinal chemistry letters, , Oct-13, Volume: 7, Issue:10, 2016
Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 19, Issue:12, 2009
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Simplified staurosporine analogs as potent JAK3 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 17, Issue:2, 2007
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 18, Issue:22, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Pyridones in drug discovery: Recent advances.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 38, 2021
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors.Chemistry & biology, , Mar-25, Volume: 18, Issue:3, 2011
Virtual screening to successfully identify novel janus kinase 3 inhibitors: a sequential focused screening approach.Journal of medicinal chemistry, , Nov-13, Volume: 51, Issue:21, 2008
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.Proceedings of the National Academy of Sciences of the United States of America, , Dec-18, Volume: 104, Issue:51, 2007
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.Bioorganic & medicinal chemistry letters, , Apr-22, Volume: 12, Issue:8, 2002
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
[no title available]Journal of medicinal chemistry, , 08-11, Volume: 65, Issue:15, 2022
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Design, synthesis and structure-activity relationship studies of pyrido[2,3-d]pyrimidin-7-ones as potent Janus Kinase 3 (JAK3) covalent inhibitors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 64, 2022
Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Synthesis and evaluation of hydrazinyl-containing pyrrolo[2,3-d]pyrimidine series as potent, selective and oral JAK1 inhibitors for the treatment of rheumatoid arthritis.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 74, 2022
Discovery and Biological Evaluation of Journal of medicinal chemistry, , 01-28, Volume: 64, Issue:2, 2021
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.Bioorganic & medicinal chemistry, , 01-15, Volume: 28, Issue:2, 2020
Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors.Bioorganic & medicinal chemistry, , 04-15, Volume: 27, Issue:8, 2019
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
Discovery of novel selective Janus kinase 2 (JAK2) inhibitors bearing a 1H-pyrazolo[3,4-d]pyrimidin-4-amino scaffold.Bioorganic & medicinal chemistry, , 04-15, Volume: 27, Issue:8, 2019
Discovery of potent anti-inflammatory 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl) pyrimidin-2-amines for use as Janus kinase inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.Journal of medicinal chemistry, , 02-08, Volume: 61, Issue:3, 2018
Structure-based design and synthesis of 1H-pyrazolo[3,4-d]pyrimidin-4-amino derivatives as Janus kinase 3 inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 26, Issue:17, 2018
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.Journal of medicinal chemistry, , 12-13, Volume: 61, Issue:23, 2018
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.Journal of medicinal chemistry, , 12-14, Volume: 60, Issue:23, 2017
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.ACS chemical biology, , 12-16, Volume: 11, Issue:12, 2016
Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.Cell chemical biology, , Nov-17, Volume: 23, Issue:11, 2016
Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 24, Issue:4, 2014
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 24, Issue:21, 2014
Linear propargylic alcohol functionality attached to the indazole-7-carboxamide as a JAK1-specific linear probe group.Bioorganic & medicinal chemistry, , Feb-01, Volume: 22, Issue:3, 2014
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.Bioorganic & medicinal chemistry letters, , May-01, Volume: 23, Issue:9, 2013
Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 23, Issue:9, 2013
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.Journal of medicinal chemistry, , Jan-10, Volume: 56, Issue:1, 2013
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 19, Issue:20, 2009
Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 16, Issue:21, 2006
Features of selective kinase inhibitors.Chemistry & biology, , Volume: 12, Issue:6, 2005
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.Science (New York, N.Y.), , Oct-31, Volume: 302, Issue:5646, 2003
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.Bioorganic & medicinal chemistry, , 01-15, Volume: 28, Issue:2, 2020
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of quinoline-based irreversible BTK inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.Bioorganic & medicinal chemistry, , 01-15, Volume: 28, Issue:2, 2020
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.European journal of medicinal chemistry, , May-01, Volume: 169, 2019
Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
[no title available]European journal of medicinal chemistry, , May-05, Volume: 131, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
[no title available]Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.Journal of medicinal chemistry, , 02-08, Volume: 61, Issue:3, 2018
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 24, Issue:4, 2014
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.Bioorganic & medicinal chemistry letters, , May-01, Volume: 23, Issue:9, 2013
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.Journal of medicinal chemistry, , Jul-12, Volume: 55, Issue:13, 2012
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
[no title available]European journal of medicinal chemistry, , Jun-05, Volume: 218, 2021
Discovery of potent anti-inflammatory 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl) pyrimidin-2-amines for use as Janus kinase inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.Journal of medicinal chemistry, , 02-08, Volume: 61, Issue:3, 2018
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.Journal of medicinal chemistry, , 03-25, Volume: 64, Issue:6, 2021
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).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 Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis.Journal of medicinal chemistry, , 12-22, Volume: 65, Issue:24, 2022
Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 38, 2021
Discovery and Biological Evaluation of Journal of medicinal chemistry, , 01-28, Volume: 64, Issue:2, 2021
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
Design, synthesis and evaluation of (MedChemComm, , Mar-01, Volume: 9, Issue:3, 2018
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
[no title available],
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.ACS medicinal chemistry letters, , Aug-13, Volume: 6, Issue:8, 2015
Monomeric Targeted Protein Degraders.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.Journal of medicinal chemistry, , 01-26, Volume: 60, Issue:2, 2017
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.Bioorganic & medicinal chemistry, , 01-15, Volume: 28, Issue:2, 2020
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.Bioorganic & medicinal chemistry, , 01-15, Volume: 28, Issue:2, 2020
Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
[no title available]European journal of medicinal chemistry, , May-05, Volume: 131, 2017
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of quinoline-based irreversible BTK inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Design, synthesis, biological activity evaluation of 3-(4-phenyl-1H-imidazol-2-yl)-1H-pyrazole derivatives as potent JAK 2/3 and aurora A/B kinases multi-targeted inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Discovery and development of aurora kinase inhibitors as anticancer agents.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| protein phosphatase binding | molecular function | Binding to a protein phosphatase. [GOC:jl] |
| growth hormone receptor binding | molecular function | Binding to a growth hormone receptor. [GOC:ai] |
| non-membrane spanning protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + protein L-tyrosine = ADP + protein L-tyrosine phosphate by a non-membrane spanning protein. [EC:2.7.10.2] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| cytoskeleton | cellular component | A cellular structure that forms the internal framework of eukaryotic and prokaryotic cells. The cytoskeleton includes intermediate filaments, microfilaments, microtubules, the microtrabecular lattice, and other structures characterized by a polymeric filamentous nature and long-range order within the cell. The various elements of the cytoskeleton not only serve in the maintenance of cellular shape but also have roles in other cellular functions, including cellular movement, cell division, endocytosis, and movement of organelles. [GOC:mah, PMID:16959967, PMID:27419875] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| extrinsic component of plasma membrane | cellular component | The component of a plasma membrane consisting of gene products and protein complexes that are loosely bound to one of its surfaces, but not integrated into the hydrophobic region. [GOC:curators, GOC:dos] |
| extrinsic component of cytoplasmic side of plasma membrane | cellular component | The component of a plasma membrane consisting of gene products and protein complexes that are loosely bound to its cytoplasmic surface, but not integrated into the hydrophobic region. [GOC:mah] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Involved In
This protein is involved in 31 target(s):
| Target | Category | Definition |
|---|
| adaptive immune response | biological process | An immune response mediated by cells expressing specific receptors for antigens produced through a somatic diversification process, and allowing for an enhanced secondary response to subsequent exposures to the same antigen (immunological memory). [GO_REF:0000022, GOC:add, ISBN:0781735149] |
| negative regulation of dendritic cell cytokine production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of dendritic cell cytokine production. [GOC:add] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| enzyme-linked receptor protein signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell, where the receptor possesses catalytic activity or is closely associated with an enzyme such as a protein kinase, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| tyrosine phosphorylation of STAT protein | biological process | The process of introducing a phosphate group to a tyrosine residue of a STAT (Signal Transducer and Activator of Transcription) protein. [GOC:jl, PMID:10918594] |
| peptidyl-tyrosine phosphorylation | biological process | The phosphorylation of peptidyl-tyrosine to form peptidyl-O4'-phospho-L-tyrosine. [RESID:AA0039] |
| B cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a B cell. A B cell is a lymphocyte of B lineage with the phenotype CD19-positive and capable of B cell mediated immunity. [GO_REF:0000022, GOC:mah] |
| negative regulation of interleukin-10 production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-10 production. [GOC:mah] |
| negative regulation of interleukin-12 production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-12 production. [GOC:mah] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| interleukin-15-mediated signaling pathway | biological process | The series of molecular signals initiated by interleukin-15 binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:signaling] |
| interleukin-4-mediated signaling pathway | biological process | The series of molecular signals initiated by interleukin-4 binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:signaling] |
| interleukin-2-mediated signaling pathway | biological process | The series of molecular signals initiated by interleukin-2 binding to its receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:nhn, GOC:signaling] |
| interleukin-9-mediated signaling pathway | biological process | The series of molecular signals initiated by interleukin-9 binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:nhn, GOC:signaling] |
| T cell homeostasis | biological process | The process of regulating the proliferation and elimination of T cells such that the total number of T cells within a whole or part of an organism is stable over time in the absence of an outside stimulus. [GOC:mgi_curators, ISBN:0781735149] |
| innate immune response | biological process | Innate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu] |
| negative regulation of FasL production | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of FasL. [GOC:go_curators] |
| negative regulation of T-helper 1 cell differentiation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of T-helper 1 cell differentiation. [GOC:go_curators] |
| regulation of receptor signaling pathway via JAK-STAT | biological process | Any process that modulates the frequency, rate or extent of receptor signaling via JAK-STAT. [GOC:bf] |
| negative regulation of T cell activation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of T cell activation. [GOC:ai] |
| growth hormone receptor signaling pathway via JAK-STAT | biological process | The process in which STAT proteins (Signal Transducers and Activators of Transcription) are activated by members of the JAK (janus activated kinase) family of tyrosine kinases, following the binding of physiological ligands to the growth hormone receptor. Once activated, STATs dimerize and translocate to the nucleus and modulate the expression of target genes. [GOC:BHF, GOC:dph, PMID:11445442] |
| regulation of T cell apoptotic process | biological process | Any process that modulates the occurrence or rate of T cell death by apoptotic process. [GOC:add, GOC:mtg_apoptosis, ISBN:0781765196] |
| negative regulation of thymocyte apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of thymocyte death by apoptotic process. [GOC:add, GOC:mtg_apoptosis, ISBN:0781765196] |
| response to interleukin-2 | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an interleukin-2 stimulus. [GOC:mah] |
| response to interleukin-4 | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an interleukin-4 stimulus. [GOC:mah] |
| response to interleukin-15 | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an interleukin-15 stimulus. [GOC:mah] |
| response to interleukin-9 | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an interleukin-9 stimulus. [GOC:mah, GOC:yaf] |
| regulation of apoptotic process | biological process | Any process that modulates the occurrence or rate of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| cell differentiation | biological process | The cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732] |
| cell surface receptor signaling pathway via JAK-STAT | biological process | A cell surface receptor signaling pathway in which ligand binding causes the receptor to dimerize, bringing the receptor-associated JAKs into close proximity. The JAKs then phosphorylate and activate each other on tyrosine residues.This leads to the activation of associated STAT protein, causing the STATs to dissociate from the receptor, translocate to the nucleus. The pathway ends with regulation of target gene expression by STAT proteins. [PMID:12039028] |
| cytokine-mediated signaling pathway | biological process | The series of molecular signals initiated by the binding of a cytokine to a receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, PMID:19295629] |