Page last updated: 2024-08-07 17:03:04
Tyrosine-protein kinase ITK/TSK
A tyrosine-protein kinase ITK/TSK that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q08881]
Synonyms
EC 2.7.10.2;
Interleukin-2-inducible T-cell kinase;
IL-2-inducible T-cell kinase;
Kinase EMT;
T-cell-specific kinase;
Tyrosine-protein kinase Lyk
Research
Bioassay Publications (36)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 15 (41.67) | 29.6817 |
| 2010's | 11 (30.56) | 24.3611 |
| 2020's | 10 (27.78) | 2.80 |
Compounds (86)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| pd168393 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 5.3379 | 3 | 3 |
| staurosporine | Homo sapiens (human) | Ki | 0.0061 | 1 | 2 |
| canertinib | Homo sapiens (human) | IC50 | 5.6500 | 1 | 1 |
| repsox | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| vx-745 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 0.2280 | 1 | 1 |
| sulfuretin | Homo sapiens (human) | IC50 | 2.0200 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 14.8500 | 1 | 1 |
| a 770041 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | IC50 | 0.0815 | 1 | 8 |
| N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide | Homo sapiens (human) | IC50 | 0.0146 | 2 | 2 |
| N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | IC50 | 16.0000 | 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 |
| 4-methyl-3-(2-(2-morpholinoethylamino)quinazolin-6-yl)-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| amg 458 | Homo sapiens (human) | IC50 | 0.0620 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | IC50 | 0.0471 | 13 | 13 |
| acp-196 | Homo sapiens (human) | IC50 | 10.6667 | 3 | 3 |
| prn694 | Homo sapiens (human) | IC50 | 0.0032 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| staurosporine | Homo sapiens (human) | Kd | 0.0190 | 2 | 2 |
| gefitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.2900 | 2 | 2 |
| vatalanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| ruboxistaurin | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| canertinib | Homo sapiens (human) | Kd | 5.6000 | 2 | 2 |
| birb 796 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| cyc 202 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| enzastaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| lapatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| sorafenib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| tandutinib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| dasatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| zd 6474 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| bosutinib | Homo sapiens (human) | Kd | 1.7000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 0.0130 | 3 | 3 |
| jnj-7706621 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 0.3500 | 2 | 2 |
| ekb 569 | Homo sapiens (human) | Kd | 2.5000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 1.2000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| hki 272 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| azd 6244 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 0.1900 | 2 | 2 |
| bibw 2992 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 0.4000 | 1 | 1 |
| brivanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.9900 | 2 | 2 |
| kw 2449 | Homo sapiens (human) | Kd | 0.2400 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| crizotinib | Homo sapiens (human) | Kd | 2.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| motesanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| mln8054 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.0340 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 0.4900 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pci 32765 | Homo sapiens (human) | Kd | 0.0600 | 2 | 2 |
| quizartinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| incb-018424 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 0.0690 | 1 | 1 |
| acp-196 | Homo sapiens (human) | Kd | 11.0000 | 2 | 2 |
| prn694 | Homo sapiens (human) | EC50 | 0.1570 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 0.5300 | 2 | 2 |
| nintedanib | Homo sapiens (human) | Kd | 0.2100 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|---|---|
| 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] |
| 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] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|---|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| 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] |
| cell-cell junction | cellular component | A cell junction that forms a connection between two or more cells of an organism; excludes direct cytoplasmic intercellular bridges, such as ring canals in insects. [GOC:aruk, GOC:bc, GOC:dgh, GOC:hb, GOC:mah, PMID:21422226, PMID:28096264] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|---|---|
| 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] |
Involved In
This protein is involved in 12 target(s):
| Target | Category | Definition |
|---|---|---|
| positive regulation of cytokine production | biological process | Any process that activates or increases the frequency, rate or extent of production of a cytokine. [GOC:add, ISBN:0781735149] |
| 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] |
| cellular defense response | biological process | A defense response that is mediated by cells. [GOC:ebc] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| activation of phospholipase C activity | biological process | The initiation of the activity of the inactive enzyme phospolipase C as the result of The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand. [GOC:dph, GOC:mah, GOC:tb, PMID:8280098] |
| 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] |
| T cell activation | biological process | The change in morphology and behavior of a mature or immature T cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149] |
| gamma-delta T cell activation | biological process | The change in morphology and behavior of a gamma-delta T cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:add] |
| T cell receptor signaling pathway | biological process | The series of molecular signals initiated by the cross-linking of an antigen receptor on a T cell. [GOC:add] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| B cell receptor signaling pathway | biological process | The series of molecular signals initiated by the cross-linking of an antigen receptor on a B cell. [GOC:add] |
| NK T cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a NK T cell. [GOC:add, ISBN:0781735149, PMID:10704459] |