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Target has curated data in GtoImmuPdb
Target id: 1994
Nomenclature: C-terminal Src kinase
Abbreviated Name: CSK
Family: Csk family
Annotation status:
Annotated and awaiting review. Please contact us if you can help with reviewing.
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Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 450 | 15q24.1 | CSK | C-terminal Src kinase | |
Mouse | - | 450 | 9 B | Csk | c-src tyrosine kinase | |
Rat | - | 450 | 8 q24 | Csk | C-terminal Src kinase |
Previous and Unofficial Names ![]() |
tyrosine-protein kinase CSK | c-src tyrosine kinase | CSK, non-receptor tyrosine kinase |
Database Links ![]() |
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BRENDA | 2.7.10.2 |
CATH/Gene3D | 3.30.505.10 |
Ensembl Gene | ENSG00000103653 (Hs), ENSMUSG00000032312 (Mm), ENSRNOG00000019374 (Rn) |
Entrez Gene | 1445 (Hs), 12988 (Mm), 315707 (Rn) |
Human Protein Atlas | ENSG00000103653 (Hs) |
KEGG Enzyme | 2.7.10.2 |
KEGG Gene | hsa:1445 (Hs), mmu:12988 (Mm), rno:315707 (Rn) |
OMIM | 124095 (Hs) |
RefSeq Nucleotide | NM_001127190 (Hs), NM_007783 (Mm), NM_001030039 (Rn) |
RefSeq Protein | NP_001120662 (Hs), NP_031809 (Mm), NP_001025210 (Rn) |
UniProtKB | P41240 (Hs), P41241 (Mm), P32577 (Rn) |
Wikipedia | CSK (Hs) |
Selected 3D Structures ![]() |
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Enzyme Reaction ![]() |
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Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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DiscoveRx KINOMEscan® screen ![]() |
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A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 3,10 |
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Target used in screen: CSK | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen ![]() |
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A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Reference: 1,4 |
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Target used in screen: CSK/CSK | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
CSK is an inhibitory regulator of Src family kinases, a family of protein tyrosine kinases indispensable to the initiation of signal transduction via ITAM-bearing immunoreceptors, and cytokine, growth factor, and pattern recognition receptor signalling. CSK phosphorylates an inhibitory tyrosine residue at the C terminus of Src kinases, leading to autoinhibition. CSK-induced Src kinase inhibition can also be mediated by binding to PEST family receptor tyrosine phosphatases [9], which are recognised modulators in immunity, autoimmunity, and autoinflammatory disorders. |
Immuno Process Associations | |||||||||||||||
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Gene Expression and Pathophysiology Comments | |
An intronic CSK polymorphism (associated with increased CSK expression) is identified as a risk allele for SLE. Carriers of the risk allele show increased B-cell receptor (BCR)-mediated activation of mature B cells and a higher circulating immunoglobulin M level, compared to non-carriers [6]. |
Biologically Significant Variants ![]() |
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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]
2. Bain J, McLauchlan H, Elliott M, Cohen P. (2003) The specificities of protein kinase inhibitors: an update. Biochem. J., 371 (Pt 1): 199-204. [PMID:12534346]
3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]
4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]
5. Lamers MB, Antson AA, Hubbard RE, Scott RK, Williams DH. (1999) Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine. J. Mol. Biol., 285 (2): 713-25. [PMID:9878439]
6. Manjarrez-Orduño N, Marasco E, Chung SA, Katz MS, Kiridly JF, Simpfendorfer KR, Freudenberg J, Ballard DH, Nashi E, Hopkins TJ et al.. (2012) CSK regulatory polymorphism is associated with systemic lupus erythematosus and influences B-cell signaling and activation. Nat. Genet., 44 (11): 1227-30. [PMID:23042117]
7. Tan L, Nomanbhoy T, Gurbani D, Patricelli M, Hunter J, Geng J, Herhaus L, Zhang J, Pauls E, Ham Y et al.. (2015) Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2). J. Med. Chem., 58 (1): 183-96. [PMID:25075558]
8. Tian S, Quan H, Xie C, Guo H, Lü F, Xu Y, Li J, Lou L. (2011) YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci., 102 (7): 1374-80. [PMID:21443688]
9. Veillette A, Rhee I, Souza CM, Davidson D. (2009) PEST family phosphatases in immunity, autoimmunity, and autoinflammatory disorders. Immunol. Rev., 228 (1): 312-24. [PMID:19290936]
10. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]
Csk family: C-terminal Src kinase. Last modified on 23/05/2017. Accessed on 18/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1994.