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Target has curated data in GtoImmuPdb
Target id: 1549
Nomenclature: casein kinase 2, alpha 1 polypeptide subunit
Abbreviated Name: CK2-A1
Family: Casein kinase 2 (CK2) family
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 391 | 20p13 | CSNK2A1 | casein kinase 2 alpha 1 | |
Mouse | - | 391 | 2 G3 | Csnk2a1 | casein kinase 2, alpha 1 polypeptide | |
Rat | - | 391 | 3q41 | Csnk2a1 | casein kinase 2 alpha 1 |
Previous and Unofficial Names |
casein kinase 2 | casein kinase II subunit alpha | CK II alpha |
Database Links | |
Alphafold | P68400 (Hs), Q60737 (Mm), P19139 (Rn) |
BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL3629 (Hs), CHEMBL3537 (Mm), CHEMBL3988629 (Rn) |
Ensembl Gene | ENSG00000101266 (Hs), ENSMUSG00000074698 (Mm), ENSRNOG00000005276 (Rn) |
Entrez Gene | 1457 (Hs), 12995 (Mm), 116549 (Rn) |
Human Protein Atlas | ENSG00000101266 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:1457 (Hs), mmu:12995 (Mm), rno:116549 (Rn) |
OMIM | 115440 (Hs) |
Pharos | P68400 (Hs) |
RefSeq Nucleotide | NM_001895 (Hs), NM_007788 (Mm), NM_053824 (Rn) |
RefSeq Protein | NP_001886 (Hs), NP_031814 (Mm), NP_446276 (Rn) |
SynPHARM |
81435 (in complex with compound 1a [PMID: 24900749]) 81423 (in complex with CX-4945) |
UniProtKB | P68400 (Hs), Q60737 (Mm), P19139 (Rn) |
Wikipedia | CSNK2A1 (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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Inhibitor Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
The CK2 inhibitor TBB (PubChem CID 1694) has an IC50 of 500nM vs. the human CK2α catalytic subunit CSNK2A1 [3]. |
DiscoveRx KINOMEscan® screen | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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: 4,11 |
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Target used in screen: CSNK2A1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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: 1,7 |
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Target used in screen: CK2/CK2a | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
CSNK2A1 is included in Guide to IMMUNOPHARMACOLOGY as it is a subunit of the casein kinase 2 complex. |
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. Battistutta R, Cozza G, Pierre F, Papinutto E, Lolli G, Sarno S, O'Brien SE, Siddiqui-Jain A, Haddach M, Anderes K et al.. (2011) Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer. Biochemistry, 50 (39): 8478-88. [PMID:21870818]
3. Battistutta R, Mazzorana M, Sarno S, Kazimierczuk Z, Zanotti G, Pinna LA. (2005) Inspecting the structure-activity relationship of protein kinase CK2 inhibitors derived from tetrabromo-benzimidazole. Chem Biol, 12 (11): 1211-9. [PMID:16298300]
4. 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]
5. Dowling JE, Alimzhanov M, Bao L, Block MH, Chuaqui C, Cooke EL, Denz CR, Hird A, Huang S, Larsen NA et al.. (2013) Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo. ACS Med Chem Lett, 4 (8): 800-5. [PMID:24900749]
6. Ferguson AD, Sheth PR, Basso AD, Paliwal S, Gray K, Fischmann TO, Le HV. (2011) Structural basis of CX-4945 binding to human protein kinase CK2. FEBS Lett, 585 (1): 104-10. [PMID:21093442]
7. 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]
8. Janeczko M, Orzeszko A, Kazimierczuk Z, Szyszka R, Baier A. (2012) CK2α and CK2α' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives. Eur J Med Chem, 47 (1): 345-50. [PMID:22115617]
9. Kinoshita T, Sekiguchi Y, Fukada H, Nakaniwa T, Tada T, Nakamura S, Kitaura K, Ohno H, Suzuki Y, Hirasawa A et al.. (2011) A detailed thermodynamic profile of cyclopentyl and isopropyl derivatives binding to CK2 kinase. Mol Cell Biochem, 356 (1-2): 97-105. [PMID:21735094]
10. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E et al.. (2011) Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J Med Chem, 54 (2): 635-54. [PMID:21174434]
11. 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]
Casein kinase 2 (CK2) family: casein kinase 2, alpha 1 polypeptide subunit. Last modified on 23/08/2017. Accessed on 07/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1549.