Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T51565 Target Info
Target Name Casein kinase II alpha (CSNK2A1)
Synonyms
Protein kinase CK2; Casein kinase II subunit alpha; CK2A1; CK II alpha; CK II
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Target Type Clinical trial Target
Gene Name CSNK2A1
Biochemical Class Kinase
UniProt ID
CSK21_HUMAN
Co-Targets of This Target  Top
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
Synonyms
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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Representative Drug(s) CX-4945 Drug Info IC50 = 55 nM [1]
Co-Target Name Serine/threonine-protein kinase pim-1 (PIM1) Clinical trial Target
UniProt ID PIM1_HUMAN
Gene Name PIM1
Synonyms
Pim-1 proto-oncogene, serine/threonine kinase; PIM
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Representative Drug(s) CX-4945 Drug Info IC50 = 46 nM [1]
Co-Target Name Serine/threonine-protein kinase pim-2 (PIM2) Clinical trial Target
UniProt ID PIM2_HUMAN
Gene Name PIM2
Synonyms
Pim-2h; PIM2
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Representative Drug(s) CX-4945 Drug Info IC50 = 186 nM [2]
Co-Target Name CDC-like kinase 2 (CLK2) Patented-recorded Target
UniProt ID CLK2_HUMAN
Gene Name CLK2
Synonyms
Dual specificity protein kinase CLK2
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Representative Drug(s) CX-4945 Drug Info IC50 = 3.8 nM [3]
Co-Target Name Dual-specificity tyrosine-phosphorylation regulated kinase 1B (DYRK1B) Patented-recorded Target
UniProt ID DYR1B_HUMAN
Gene Name DYRK1B
Synonyms
Minibrain-related kinase; MIRK; Dual specificity tyrosine-phosphorylation-regulated kinase 1B
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Representative Drug(s) CX-4945 Drug Info IC50 = 6.4 nM [4]
Co-Target Name Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A) Patented-recorded Target
UniProt ID DYR1A_HUMAN
Gene Name DYRK1A
Synonyms
hMNB; Protein kinase minibrain homolog; MNBH; MNB; HP86; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; Dual specificity YAK1-related kinase; DYRK
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Representative Drug(s) CX-4945 Drug Info IC50 = 6.8 nM [4]
Co-Target Name Casein kinase II alpha prime (CSNK2A2) Patented-recorded Target
UniProt ID CSK22_HUMAN
Gene Name CSNK2A2
Synonyms
Casein kinase II subunit alpha'; CK2A2; CK II alpha'
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Representative Drug(s) CX-4945 Drug Info IC50 = 11 nM [5]
Co-Target Name NF-kappa-B-activating kinase (TBK1) Patented-recorded Target
UniProt ID TBK1_HUMAN
Gene Name TBK1
Synonyms
TANK-binding kinase 1; T2K; Serine/threonine-protein kinase TBK1; NAK
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Representative Drug(s) CX-4945 Drug Info IC50 = 35 nM [1]
Co-Target Name Death-associated protein kinase 3 (DAPK3) Literature-reported Target
UniProt ID DAPK3_HUMAN
Gene Name DAPK3
Synonyms
Zipper-interacting protein kinase; ZIPK; ZIP-kinase; MYPT1 kinase; DAP-like kinase; DAP kinase 3
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Representative Drug(s) CX-4945 Drug Info IC50 = 17 nM [1]
Co-Target Name CDC-like kinase 3 (CLK3) Literature-reported Target
UniProt ID CLK3_HUMAN
Gene Name CLK3
Synonyms
Dual specificity protein kinase CLK3
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Representative Drug(s) CX-4945 Drug Info IC50 = 41 nM [1]
Co-Target Name Casein kinase II alpha'/beta complex (CSNK2A2-CSNK2B) Co-Target
UniProt ID CSK22_HUMAN-CSK2B_HUMAN
Gene Name CSNK2A2-CSNK2B
Synonyms
CK II alpha'/beta
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Representative Drug(s) CX-4945 Drug Info Ki = 0.22 nM [6]
Co-Target Name Homeodomain-interacting protein kinase 3 (HIPK3) Co-Target
UniProt ID HIPK3_HUMAN
Gene Name HIPK3
Synonyms
Androgen receptor-interacting nuclear protein kinase; ANPK; Fas-interacting serine/threonine-protein kinase; FIST; Homolog of protein kinase YAK1
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Representative Drug(s) CX-4945 Drug Info IC50 = 45 nM [1]
Co-Target Name Cyclin dependent kinase 1-G2/mitotic specific cyclin B complex (CDK1-CCNB) Co-Target
UniProt ID CDK1_HUMAN-CCNB1_HUMAN/CCNB2_HUMAN/CCNB3_HUMAN
Gene Name CDK1-CCNB1/CCNB2/CCNB3
Representative Drug(s) CX-4945 Drug Info IC50 = 56 nM [1]
References  Top
REF 1 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. 2011 Jan 27;54(2):635-54.
REF 2 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. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92.
REF 3 Novel non-ATP competitive small molecules targeting the CK2 alpha/beta interface. Bioorg Med Chem. 2018 Jul 15;26(11):3016-20.
REF 4 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site. J Med Chem. 2019 Feb 28;62(4):1803-1816.
REF 5 Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors. Bioorg Med Chem. 2016 Mar 1;24(5):1136-41.
REF 6 Synthesis and SAR of inhibitors of protein kinase CK2: novel tricyclic quinoline analogs. Bioorg Med Chem Lett. 2012 Jan 1;22(1):45-8.

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