Proteins > Casein kinase II subunit alpha
Page last updated: 2024-08-07 16:54:28
Casein kinase II subunit alpha
A casein kinase II subunit alpha that is encoded in the genome of human. [PRO:DNx]
Synonyms
CK II alpha;
EC 2.7.11.1
Research
Bioassay Publications (81)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (1.23) | 18.7374 |
| 1990's | 3 (3.70) | 18.2507 |
| 2000's | 22 (27.16) | 29.6817 |
| 2010's | 45 (55.56) | 24.3611 |
| 2020's | 10 (12.35) | 2.80 |
Compounds (129)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 4,5,6,7-tetrabromo-2-azabenzimidazole | Homo sapiens (human) | IC50 | 0.7354 | 13 | 12 |
| 4,5,6,7-tetrabromo-2-azabenzimidazole | Homo sapiens (human) | Ki | 0.6957 | 7 | 7 |
| chromone-2-carboxylic acid | Homo sapiens (human) | IC50 | 5.9800 | 1 | 1 |
| danthron | Homo sapiens (human) | Ki | 40.0000 | 1 | 1 |
| emodin | Homo sapiens (human) | IC50 | 1.0112 | 8 | 7 |
| emodin | Homo sapiens (human) | Ki | 9.4200 | 5 | 5 |
| n-(2-(methylamino)ethyl)-5-isoquinolinesulfonamide | Homo sapiens (human) | Ki | 950.0000 | 1 | 1 |
| n-(2-aminoethyl)-5-isoquinolinesulfonamide | Homo sapiens (human) | IC50 | 97.9200 | 1 | 5 |
| nsc 664704 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 6.9000 | 1 | 1 |
| mitoxantrone | Homo sapiens (human) | IC50 | 0.6600 | 1 | 1 |
| 1,2,5,8-tetrahydroxy anthraquinone | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
| 1,2,5,8-tetrahydroxy anthraquinone | Homo sapiens (human) | Ki | 0.0600 | 2 | 2 |
| 3,4-dichlorobenzoic acid | Homo sapiens (human) | IC50 | 5,000.0000 | 1 | 1 |
| dichlororibofuranosylbenzimidazole | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| dichlororibofuranosylbenzimidazole | Homo sapiens (human) | Ki | 10.6667 | 3 | 3 |
| boldine | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 27.6042 | 4 | 4 |
| norharman | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| cki 7 | Homo sapiens (human) | IC50 | 399.0833 | 1 | 6 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| 7-n-butyl-6-(4'-hydroxyphenyl)-5h-pyrrolo(2,3b)pyrazine | Homo sapiens (human) | IC50 | 100.0000 | 3 | 3 |
| purvalanol b | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| h 89 | Homo sapiens (human) | Ki | 56.8328 | 2 | 10 |
| purvalanol a | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 4,5,6,7-tetrabromobenzimidazole | Homo sapiens (human) | IC50 | 0.7800 | 5 | 4 |
| 4,5,6,7-tetrabromobenzimidazole | Homo sapiens (human) | Ki | 0.4103 | 7 | 7 |
| quercetin | Homo sapiens (human) | IC50 | 1.6500 | 5 | 5 |
| quercetin | Homo sapiens (human) | Ki | 1.1800 | 4 | 4 |
| apigenin | Homo sapiens (human) | IC50 | 0.8400 | 5 | 5 |
| apigenin | Homo sapiens (human) | Ki | 0.7400 | 3 | 3 |
| luteolin | Homo sapiens (human) | IC50 | 0.7500 | 2 | 2 |
| kaempferol | Homo sapiens (human) | IC50 | 0.7000 | 2 | 2 |
| baicalein | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| chrysin | Homo sapiens (human) | IC50 | 9.0000 | 1 | 1 |
| fisetin | Homo sapiens (human) | IC50 | 0.5667 | 3 | 3 |
| fisetin | Homo sapiens (human) | Ki | 0.2600 | 2 | 2 |
| morin | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| myricetin | Homo sapiens (human) | IC50 | 0.9400 | 3 | 3 |
| coumestrol | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
| coumestrol | Homo sapiens (human) | Ki | 7.6700 | 2 | 2 |
| ellagic acid | Homo sapiens (human) | IC50 | 0.0400 | 3 | 3 |
| ellagic acid | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| as 605240 | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
| casein kinase ii | Homo sapiens (human) | IC50 | 2.2300 | 5 | 5 |
| casein kinase ii | Homo sapiens (human) | Ki | 0.8093 | 6 | 6 |
| jnj-7706621 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 3,8-dibromo-7-hydroxy-4-methylchromen-2-one | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| gw-5074 | Homo sapiens (human) | IC50 | 0.2790 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | IC50 | 0.0170 | 1 | 1 |
| jnj 10198409 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| ps1145 | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| danusertib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| as 252424 | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
| mln8054 | Homo sapiens (human) | IC50 | 20.5000 | 1 | 1 |
| 2-({2-[(3-hydroxyphenyl)amino]pyrimidin-4-yl}amino)benzamide | Homo sapiens (human) | IC50 | 0.7300 | 1 | 1 |
| (e)-3-(2,3,4,5-tetrabromophenyl)acrylic acid | Homo sapiens (human) | IC50 | 0.1100 | 1 | 0 |
| (e)-3-(2,3,4,5-tetrabromophenyl)acrylic acid | Homo sapiens (human) | Ki | 0.0770 | 1 | 1 |
| cx 4945 | Homo sapiens (human) | IC50 | 0.5348 | 29 | 27 |
| cx 4945 | Homo sapiens (human) | Ki | 0.0004 | 3 | 3 |
| entrectinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| nms p937 | Homo sapiens (human) | IC50 | 0.8260 | 1 | 0 |
| nms-p118 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| cx 5011 | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| cx 5011 | Homo sapiens (human) | Ki | 0.4200 | 1 | 1 |
| palinurin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| ((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one) | Homo sapiens (human) | IC50 | 0.4150 | 2 | 2 |
| hymenialdisine | Homo sapiens (human) | IC50 | 7.0000 | 1 | 1 |
| XL413 | Homo sapiens (human) | IC50 | 0.2150 | 1 | 1 |
| 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) |
|---|
| 5-methylsalicylic acid | Homo sapiens (human) | INH | 100.0000 | 1 | 1 |
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Identification by Inverse Virtual Screening of magnolol-based scaffold as new tankyrase-2 inhibitors.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Design, synthesis, and evaluation of 4,5,6,7-tetrahydrobenzo[MedChemComm, , Sep-01, Volume: 9, Issue:9, 2018
Synthesis, in vitro antiproliferative activity and kinase profile of new benzimidazole and benzotriazole derivatives.Bioorganic chemistry, , Volume: 72, 2017
Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Identification of protein kinase CK2 inhibitors using solvent dipole ordering virtual screening.European journal of medicinal chemistry, , Volume: 96, 2015
Ethyl 2-(benzylidene)-7-methyl-3-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylate analogues as a new scaffold for protein kinase casein kinase 2 inhibitor.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Synthesis of novel chiral TBBt derivatives with hydroxyl moiety. Studies on inhibition of human protein kinase CK2α and cytotoxicity properties.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2.European journal of medicinal chemistry, , Volume: 65, 2013
Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 19, Issue:11, 2009
Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
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
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).The Biochemical journal, , Sep-15, Volume: 374, Issue:Pt 3, 2003
[no title available],
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
A new family of densely functionalized fused-benzoquinones as potent human protein kinase CK2 inhibitors.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Identification of protein kinase CK2 inhibitors using solvent dipole ordering virtual screening.European journal of medicinal chemistry, , Volume: 96, 2015
Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2.European journal of medicinal chemistry, , Volume: 65, 2013
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 19, Issue:11, 2009
Inhibition of protein kinase CK2 by anthraquinone-related compounds. A structural insight.The Journal of biological chemistry, , Jan-17, Volume: 278, Issue:3, 2003
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).The Biochemical journal, , Sep-15, Volume: 374, Issue:Pt 3, 2003
[no title available],
New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation.Bioorganic & medicinal chemistry, , 11-01, Volume: 28, Issue:21, 2020
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Design and synthesis of novel protein kinase CK2 inhibitors on the base of 4-aminothieno[2,3-d]pyrimidines.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Design and synthesis of novel protein kinase CK2 inhibitors on the base of 4-aminothieno[2,3-d]pyrimidines.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 19, Issue:11, 2009
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).The Biochemical journal, , Sep-15, Volume: 374, Issue:Pt 3, 2003
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Novel 8-arylated purines as inhibitors of glycogen synthase kinase.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
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 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
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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 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
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.Journal of medicinal chemistry, , Jan-16, Volume: 46, Issue:2, 2003
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity.The Journal of biological chemistry, , Oct-18, Volume: 271, Issue:42, 1996
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma The Journal of biological chemistry, , Mar-25, Volume: 265, Issue:9, 1990
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
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Thiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2.Bioorganic & medicinal chemistry, , 10-01, Volume: 26, Issue:18, 2018
Synthesis, in vitro antiproliferative activity and kinase profile of new benzimidazole and benzotriazole derivatives.Bioorganic chemistry, , Volume: 72, 2017
Computational Tools To Model Halogen Bonds in Medicinal Chemistry.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Synthesis of novel polybrominated benzimidazole derivatives-potential CK2 inhibitors with anticancer and proapoptotic activity.Bioorganic & medicinal chemistry, , Feb-15, Volume: 24, Issue:4, 2016
CK2α and CK2α' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives.European journal of medicinal chemistry, , Volume: 47, Issue:1, 2012
Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2.Bioorganic & medicinal chemistry, , Feb-15, Volume: 17, Issue:4, 2009
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 2004
[no title available],
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Discovery and characterization of synthetic 4'-hydroxyflavones-New CK2 inhibitors from flavone family.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2.European journal of medicinal chemistry, , Volume: 46, Issue:3, 2011
Biotinylated quercetin as an intrinsic photoaffinity proteomics probe for the identification of quercetin target proteins.Bioorganic & medicinal chemistry, , Aug-15, Volume: 19, Issue:16, 2011
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).The Biochemical journal, , Sep-15, Volume: 374, Issue:Pt 3, 2003
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Identification of protein kinase CK2 inhibitors using solvent dipole ordering virtual screening.European journal of medicinal chemistry, , Volume: 96, 2015
Discovery and characterization of synthetic 4'-hydroxyflavones-New CK2 inhibitors from flavone family.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 19, Issue:11, 2009
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).The Biochemical journal, , Sep-15, Volume: 374, Issue:Pt 3, 2003
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Design and synthesis of novel protein kinase CK2 inhibitors on the base of 4-aminothieno[2,3-d]pyrimidines.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Discovery and characterization of synthetic 4'-hydroxyflavones-New CK2 inhibitors from flavone family.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Discovery and characterization of synthetic 4'-hydroxyflavones-New CK2 inhibitors from flavone family.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Inhibitory Properties of ATP-Competitive Coumestrol and Boldine Are Correlated to Different Modulations of CK2 Flexibility.Journal of natural products, , 04-26, Volume: 82, Issue:4, 2019
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2.European journal of medicinal chemistry, , Volume: 65, 2013
Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 19, Issue:11, 2009
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Synthesis of novel chiral TBBt derivatives with hydroxyl moiety. Studies on inhibition of human protein kinase CK2α and cytotoxicity properties.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
CK2α and CK2α' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives.European journal of medicinal chemistry, , Volume: 47, Issue:1, 2012
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 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
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 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
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
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.Proceedings of the National Academy of Sciences of the United States of America, , Mar-06, Volume: 104, Issue:10, 2007
Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy.Journal of medicinal chemistry, , 12-23, Volume: 64, Issue:24, 2021
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Recent advances in development of hetero-bivalent kinase inhibitors.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
A novel class of selective CK2 inhibitors targeting its open hinge conformation.European journal of medicinal chemistry, , Jun-01, Volume: 195, 2020
Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 28, Issue:8, 2018
Thiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2.Bioorganic & medicinal chemistry, , 10-01, Volume: 26, Issue:18, 2018
Novel non-ATP competitive small molecules targeting the CK2 α/β interface.Bioorganic & medicinal chemistry, , 07-15, Volume: 26, Issue:11, 2018
Oligo-aspartic acid conjugates with benzo[c][2,6]naphthyridine-8-carboxylic acid scaffold as picomolar inhibitors of CK2.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
Design and synthesis of novel protein kinase CK2 inhibitors on the base of 4-aminothieno[2,3-d]pyrimidines.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2.European journal of medicinal chemistry, , Volume: 65, 2013
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.Journal of medicinal chemistry, , Jan-27, Volume: 54, Issue:2, 2011
7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 21, Issue:22, 2011
[no title available],
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
Small molecule modulators targeting protein kinase CK1 and CK2.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.Journal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Enables
This protein enables 7 target(s):
| Target | Category | Definition |
|---|
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| 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] |
| kinase activity | molecular function | Catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [ISBN:0198506732] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| Hsp90 protein binding | molecular function | Binding to Hsp90 proteins, any of a group of heat shock proteins around 90kDa in size. [GOC:ai] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 4 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] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| 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] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| PML body | cellular component | A class of nuclear body; they react against SP100 auto-antibodies (PML, promyelocytic leukemia); cells typically contain 10-30 PML bodies per nucleus; alterations in the localization of PML bodies occurs after viral infection. [GOC:ma, PMID:10944585] |
| 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] |
| 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] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| PcG protein complex | cellular component | A chromatin-associated multiprotein complex containing Polycomb Group proteins. In Drosophila, Polycomb group proteins are involved in the long-term maintenance of gene repression, and PcG protein complexes associate with Polycomb group response elements (PREs) in target genes to regulate higher-order chromatin structure. [PMID:9372908] |
| protein kinase CK2 complex | cellular component | A protein complex that possesses protein serine/threonine kinase activity, and contains two catalytic alpha subunits and two regulatory beta subunits. Protein kinase CK2 complexes are found in nearly every subcellular compartment, and can phosphorylate many protein substrates in addition to casein. [GOC:mah, PMID:10994779] |
| Sin3-type complex | cellular component | Any of a number of evolutionarily conserved histone deacetylase complexes (HDACs) containing a core consisting of a paired amphipathic helix motif protein (e.g. Sin3p in S. cerevisiae, Pst1 in S. pombe or Sin3A in mammals) at least one class I histone deacetylase (e.g. Rpd3p in S. cerevisiae, Clr6 in S. pombe, or HDAC1 and HDAC2 in mammals), and at least one WD40 repeat protein (e.g. Ume1p in S. cerevisiae, Prw1 in S. pombe, or RbAp46 and RbAp48 in mammals). These complexes also contain a variable number of other proteins that direct histone binding, DNA binding, or add other functionality to the complex. [PMID:15565322, PMID:18292778] |
Involved In
This protein is involved in 24 target(s):
| Target | Category | Definition |
|---|
| double-strand break repair | biological process | The repair of double-strand breaks in DNA via homologous and nonhomologous mechanisms to reform a continuous DNA helix. [GOC:elh] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
| DNA damage response | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
| 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] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| Wnt signaling pathway | biological process | The series of molecular signals initiated by binding of a Wnt protein to a frizzled family receptor on the surface of a target cell and ending with a change in cell state. [PMID:11532397] |
| negative regulation of translation | 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 proteins by the translation of mRNA or circRNA. [GOC:isa_complete] |
| peptidyl-serine phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| peptidyl-threonine phosphorylation | biological process | The phosphorylation of peptidyl-threonine to form peptidyl-O-phospho-L-threonine. [RESID:AA0038] |
| positive regulation of Wnt signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of Wnt signal transduction. [GOC:dph, GOC:go_curators, GOC:tb] |
| positive regulation of cell growth | biological process | Any process that activates or increases the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
| negative regulation of proteasomal ubiquitin-dependent protein catabolic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the breakdown of a protein or peptide by hydrolysis of its peptide bonds, initiated by the covalent attachment of ubiquitin, and mediated by the proteasome. [GOC:mah] |
| negative regulation of cysteine-type endopeptidase activity involved in apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of a cysteine-type endopeptidase activity involved in the apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| positive regulation of protein catabolic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of a protein by the destruction of the native, active configuration, with or without the hydrolysis of peptide bonds. [GOC:go_curators] |
| rhythmic process | biological process | Any process pertinent to the generation and maintenance of rhythms in the physiology of an organism. [GOC:jid] |
| protein stabilization | biological process | Any process involved in maintaining the structure and integrity of a protein and preventing it from degradation or aggregation. [GOC:ai] |
| chaperone-mediated protein folding | biological process | The process of inhibiting aggregation and assisting in the covalent and noncovalent assembly of single chain polypeptides or multisubunit complexes into the correct tertiary structure that is dependent on interaction with a chaperone. [GOC:dph, GOC:vw] |
| symbiont-mediated disruption of host cell PML body | biological process | The process in which an organism effects a change that impairs the structure or function of the host PML body. A PML body is a nuclear body that reacts against SP100 auto-antibodies (PML = promyelocytic leukemia). The host is defined as the larger of the organisms involved in a symbiotic interaction. [GOC:BHF, GOC:jl] |
| positive regulation of aggrephagy | biological process | Any process that activates or increases the frequency, rate or extent of aggrephagy. [GO_REF:0000058, GOC:pad, GOC:PARL, GOC:TermGenie, PMID:25686248] |
| regulation of chromosome separation | biological process | Any process that modulates the frequency, rate or extent of chromosome separation. [GO_REF:0000058, GOC:bhm, GOC:TermGenie, PMID:21795393] |
| negative regulation of double-strand break repair via homologous recombination | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of double-strand break repair via homologous recombination. [GOC:vw] |
| negative regulation of apoptotic signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of apoptotic signaling pathway. [GOC:mtg_apoptosis] |
| regulation of cell cycle | biological process | Any process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb] |