Proteins > Tyrosine-protein kinase ZAP-70
Page last updated: 2024-08-07 16:40:56
Tyrosine-protein kinase ZAP-70
A tyrosine-protein kinase ZAP-70 that is encoded in the genome of human. [PRO:CL, UniProtKB:P43403]
Synonyms
EC 2.7.10.2;
70 kDa zeta-chain associated protein;
Syk-related tyrosine kinase
Research
Bioassay Publications (42)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 21 (50.00) | 29.6817 |
| 2010's | 20 (47.62) | 24.3611 |
| 2020's | 1 (2.38) | 2.80 |
Compounds (103)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tyrphostin a23 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n(6),n(6)-dimethyladenine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nu6102 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| ag 1879 | Homo sapiens (human) | IC50 | 100,000.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0175 | 8 | 8 |
| birb 796 | Homo sapiens (human) | IC50 | 25.0000 | 2 | 2 |
| bms 387032 | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| vx-745 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| 7-butyl-6-(4-methoxyphenyl)-5H-pyrrolo[2,3-b]pyrazine | Homo sapiens (human) | Ki | 2.6303 | 1 | 1 |
| alvocidib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| semaxinib | Homo sapiens (human) | IC50 | 20.7000 | 1 | 1 |
| orantinib | Homo sapiens (human) | IC50 | 28.4000 | 1 | 1 |
| a 419259 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| b 43 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| a 770041 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| ((3z)-n-(3-chlorophenyl)-3-((3,5-dimethyl-4-((4-methylpiperazin-1-yl)carbonyl)-1h-pyrrol-2-yl)methylene)-n-methyl-2-oxo-2,3-dihydro-1h-indole-5-sulfonamide) | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| l 783277 | Homo sapiens (human) | IC50 | 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) | IC50 | 0.0420 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 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 | 50.0000 | 1 | 1 |
| nvp-aew541 | Homo sapiens (human) | IC50 | 10.0000 | 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 |
| pha 767491 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Ki | 8.2000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | IC50 | 1.5980 | 1 | 1 |
| 4-methyl-3-(2-(2-morpholinoethylamino)quinazolin-6-yl)-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| pha 848125 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| entrectinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| p505-15 | Homo sapiens (human) | IC50 | 0.6443 | 3 | 3 |
| gsk143 | Homo sapiens (human) | IC50 | 19.9526 | 1 | 1 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| urmc-099 | Homo sapiens (human) | IC50 | 5.0500 | 1 | 1 |
| ceritinib | Homo sapiens (human) | IC50 | 9.7000 | 1 | 1 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor.European journal of medicinal chemistry, , Jul-05, Volume: 219, 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 pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors.Bioorganic & medicinal chemistry, , Oct-15, Volume: 16, Issue:20, 2008
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
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
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 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
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
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
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
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 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
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
Syk inhibitors with high potency in presence of blood.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
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
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proceedings of the National Academy of Sciences of the United States of America, , Jan-02, Volume: 104, Issue:1, 2007
Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
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
Discovery and profiling of a selective and efficacious Syk inhibitor.Journal of medicinal chemistry, , Feb-26, Volume: 58, Issue:4, 2015
Syk inhibitors with high potency in presence of blood.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| phosphotyrosine residue binding | molecular function | Binding to a phosphorylated tyrosine residue within a protein. [PMID:14636584] |
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| 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] |
| signaling receptor binding | molecular function | Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| immunological synapse | cellular component | An area of close contact between a lymphocyte (T-, B-, or natural killer cell) and a target cell formed through the clustering of particular signaling and adhesion molecules and their associated membrane rafts on both the lymphocyte and the target cell and facilitating activation of the lymphocyte, transfer of membrane from the target cell to the lymphocyte, and in some situations killing of the target cell through release of secretory granules and/or death-pathway ligand-receptor interaction. [GOC:mgi_curators, PMID:11244041, PMID:11376300] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| 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] |
| 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] |
| 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 2 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| T cell receptor complex | cellular component | A protein complex that contains a disulfide-linked heterodimer of T cell receptor (TCR) chains, which are members of the immunoglobulin superfamily, and mediates antigen recognition, ultimately resulting in T cell activation. The TCR heterodimer is associated with the CD3 complex, which consists of the nonpolymorphic polypeptides gamma, delta, epsilon, zeta, and, in some cases, eta (an RNA splice variant of zeta) or Fc epsilon chains. [GOC:mah, ISBN:0781735149] |
Involved In
This protein is involved in 19 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] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
| T cell differentiation | biological process | The process in which a precursor cell type acquires characteristics of a more mature T-cell. A T cell is a type of lymphocyte whose definin characteristic is the expression of a T cell receptor complex. [GO_REF:0000022, GOC:jid, 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] |
| 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] |
| B cell activation | biological process | The change in morphology and behavior of a mature or immature B cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149] |
| beta selection | biological process | The process in which successful recombination of a T cell receptor beta chain into a translatable protein coding sequence leads to rescue from apoptosis and subsequent proliferation of an immature T cell. [ISBN:0781735149, PMID:12220932] |
| negative thymic T cell selection | biological process | The process of elimination of immature T cells in the thymus which react strongly with self-antigens. [ISBN:0781735149, PMID:12414722] |
| positive regulation of alpha-beta T cell differentiation | biological process | Any process that activates or increases the frequency, rate or extent of alpha-beta T cell differentiation. [GOC:ai] |
| positive regulation of alpha-beta T cell proliferation | biological process | Any process that activates or increases the frequency, rate or extent of alpha-beta T cell proliferation. [GOC:ai] |
| positive regulation of calcium-mediated signaling | biological process | Any process that activates or increases the frequency, rate or extent of calcium-mediated signaling. [GOC:ai] |
| 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] |
| T cell aggregation | biological process | The adhesion of one T cell to one or more other T cells via adhesion molecules. [GOC:sl, PMID:12972508] |
| T cell migration | biological process | The movement of a T cell within or between different tissues and organs of the body. [CL:0000084, GOC:BHF, GOC:mah] |
| cell surface receptor protein tyrosine kinase 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 tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| 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] |
| 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] |