CSNK2A2

Summary

CSNK2A2 (casein kinase 2 alpha 2, HGNC:2459) is a protein-coding gene on chromosome 16q21, encoding Casein kinase II subunit alpha’ (P19784). Catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated serine or threonine.

This gene encodes the alpha’, or alpha 2, catalytic subunit of the protein kinase enzyme, casein kinase 2 (CK2). Casein kinase 2 is a serine/threonine protein kinase that phosphorylates acidic proteins such as casein. It is involved in various cellular processes, including cell cycle control, apoptosis, and circadian rhythms. This heterotetrameric kinase includes two catalytic subunits, either alpha or alpha’, and two regulatory beta subunits. The closely related gene paralog encoding the alpha, or alpha 1 subunit (CSNK2A1, Gene ID: 1457) is found on chromosome 20. An intronic variant in this gene (alpha 2) may be associated with leukocyte telomere length in a South Asian population. A related transcribed pseudogene is found on chromosome 11.

Source: NCBI Gene 1459 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 59 total
• Phenotypes (HPO): 48
• Druggable target: yes — 70 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001896

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2459
Approved symbol	CSNK2A2
Name	casein kinase 2 alpha 2
Location	16q21
Locus type	gene with protein product
Status	Approved
Aliases	CSNK2A1, CK2alpha'
Ensembl gene	ENSG00000070770
Ensembl biotype	protein_coding
OMIM	115442
Entrez	1459

Gene structure

Transcript identifiers

Ensembl transcripts: 22 — 17 protein_coding, 4 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000262506, ENST00000562367, ENST00000563307, ENST00000565188, ENST00000566813, ENST00000567730, ENST00000676463, ENST00000677823, ENST00000867095, ENST00000931138, ENST00000931139, ENST00000931140, ENST00000931141, ENST00000931142, ENST00000931143, ENST00000931144, ENST00000931145, ENST00000952600, ENST00000952601, ENST00000952602, ENST00000952603, ENST00000952604

RefSeq mRNA: 1 — MANE Select: NM_001896 NM_001896

CCDS: CCDS10794

Canonical transcript exons

ENST00000262506 — 12 exons

Exon	Start	End
ENSE00000686599	58196733	58196844
ENSE00001141971	58157907	58158353
ENSE00002580532	58197633	58198106
ENSE00003500637	58168610	58168693
ENSE00003578235	58167207	58167308
ENSE00003613163	58166584	58166684
ENSE00003617109	58174451	58174510
ENSE00003626920	58165560	58165708
ENSE00003627731	58167685	58167795
ENSE00003631800	58184260	58184310
ENSE00003633561	58164054	58164147
ENSE00003691923	58186755	58186856

Expression profiles

Bgee: expression breadth ubiquitous, 287 present calls, max score 98.41.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 57.3179 / max 737.9465, expressed in 1826 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
157610	55.7423	1826
157611	1.2536	827
157607	0.3220	158

Top tissues by expression

293 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
secondary oocyte	CL:0000655	98.41	gold quality
left testis	UBERON:0004533	98.34	gold quality
right testis	UBERON:0004534	98.27	gold quality
oocyte	CL:0000023	98.18	gold quality
testis	UBERON:0000473	97.11	gold quality
skin of leg	UBERON:0001511	95.85	gold quality
sperm	CL:0000019	95.54	gold quality
upper leg skin	UBERON:0004262	95.49	gold quality
upper arm skin	UBERON:0004263	95.32	gold quality
skin of abdomen	UBERON:0001416	95.27	gold quality
zone of skin	UBERON:0000014	94.94	gold quality
male germ cell	CL:0000015	94.83	gold quality
adult organism	UBERON:0007023	94.12	gold quality
body of pancreas	UBERON:0001150	93.62	gold quality
ganglionic eminence	UBERON:0004023	93.56	gold quality
stromal cell of endometrium	CL:0002255	93.22	gold quality
cortical plate	UBERON:0005343	93.01	gold quality
muscle layer of sigmoid colon	UBERON:0035805	92.38	gold quality
hindlimb stylopod muscle	UBERON:0004252	92.13	gold quality
popliteal artery	UBERON:0002250	92.04	gold quality
tibial artery	UBERON:0007610	92.04	gold quality
lower esophagus muscularis layer	UBERON:0035833	92.03	gold quality
lower esophagus	UBERON:0013473	92.01	gold quality
pancreas	UBERON:0001264	91.75	gold quality
gastrocnemius	UBERON:0001388	91.73	gold quality
body of stomach	UBERON:0001161	91.64	gold quality
mammalian vulva	UBERON:0000997	91.61	gold quality
islet of Langerhans	UBERON:0000006	91.58	gold quality
left ovary	UBERON:0002119	91.56	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	91.53	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CTCF, ETS1, HHEX, IRF6, MAFB, PDX1, SP3, STAT1, TP53, ZNF236

miRNA regulators (miRDB)

46 targeting CSNK2A2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-23A-3P	99.95	74.24	3163
HSA-MIR-23B-3P	99.95	74.24	3163
HSA-MIR-23C	99.95	73.92	3192
HSA-MIR-95-5P	99.89	72.17	3973
HSA-MIR-6124	99.87	69.78	3551
HSA-MIR-659-3P	99.85	70.69	1620
HSA-MIR-5010-3P	99.83	70.60	2357
HSA-MIR-379-3P	99.69	69.60	1524
HSA-MIR-411-3P	99.69	69.63	1524
HSA-MIR-671-5P	99.52	67.11	1277
HSA-MIR-6727-3P	99.49	65.92	1333
HSA-MIR-4722-3P	99.35	65.22	1099
HSA-MIR-3160-5P	99.28	69.07	1938
HSA-MIR-6071	99.16	67.77	1780
HSA-MIR-4464	98.95	67.73	820
HSA-MIR-4748	98.95	67.53	810
HSA-MIR-1294	98.91	69.26	1030
HSA-MIR-9986	98.91	69.28	1024
HSA-MIR-6829-5P	98.86	65.12	1480
HSA-MIR-4272	98.76	68.74	1810
HSA-MIR-7114-5P	98.51	67.87	1349

Literature-anchored findings (GeneRIF, showing 37)

• Functional specialization of CK2 isoforms and characterization of isoform-specific binding partners (PMID:11827170)
• Localization of individual subunits of protein kinase CK2 to the endoplasmic reticulum and to the Golgi apparatus (PMID:11827177)
• Association and regulation of casein kinase 2 activity by adenomatous polyposis coli protein (PMID:11972058)
• Protein kinase CK2 dependent phosphorylation of the E2 ubiquitin conjugating enzyme UBC3B induces its interaction with beta-TRCp and enhances beta-catenin degradation [UBC3B] (PMID:12037680)
• FGF-1 binds to both the catalytic alpha-subunit & to the regulatory beta-subunit of CK2. FGF-1 & CK2 alpha are shown to interact in vivo. A correlation between the mitogenic potential of FGF-1 mutants & their ability to bind to CK2 alpha was observed. (PMID:12145206)
• physiological control of G-protein regulation by phosducin-like protein seems to involve phosphorylation by CK2 and alternative splicing of the regulator (PMID:12466282)
• Data point to a particular role of the catalytic alpha and alpha’ subunits of protein kinase CK2, which may be different from their roles in the holoenzyme. (PMID:12568341)
• Ets motifs play, in cooperation with Sp motif clusters, a central role in regulating CK2alpha’ gene transcription. (PMID:16335532)
• Results identified the motor neuron protein KIF5C as a new binding partner for the protein kinase CK2alpha’. (PMID:19011756)
• The CK2 alpha’ phosphorylates APRIL and therefore is responsible for the regulation of the nucleocytoplasmic translocation of CD83 mRNA. (PMID:19130553)
• Data presented the crystal structures of CK2alpha in complex with CX-4945 and adenylyl phosphoramidate at 2.7 and 1.3 A, respectively. (PMID:21093442)
• A thorough investigation of CK2alpha identifies key energetic hot spots on the surface of CK2alpha and their thermostability and catalytic activity in comparison to the wild type subunit. (PMID:21142136)
• In hsCK2alpha’ an open conformation of the interdomain hinge/helix alphaD region that is critical for ATP-binding is found corresponding to an incomplete catalytic spine. In contrast hsCK2alpha often adopts the canonical, PKA-like version of the catalytic spine. (PMID:21739153)
• Lack of DNA-PKcs is accompanied by an increase in the protein level of one of the catalytic isozymes of protein kinase CK2, i.e., CK2alpha’ and a concomitant increase in CK2 activity. (PMID:21750982)
• CK2alpha’ exhibits a striking preference for caspase-3 phosphorylation in cells as compared to CK2alpha and that CK2beta exhibits the capacity to abolish caspase-3 phosphorylation (PMID:23599180)
• CSNK2A2 phosphorylates telomeric repeat binding factor 1 and plays an important role for regulation of telomere length. (PMID:24795349)
• Data suggest casein kinase II (CK2) inhibitors indeno[1,2-b]indole-9,10-dione, which also inhibited the breast cancer resistance protein ABCG2, might be a good therapeutic strategy to improve anticancer drug efficiency. (PMID:25272055)
• Over-expressed CK2alpha positively regulate Hh/Gli1 signaling in human mesothelioma. (PMID:25422081)
• we propose that Foxc2 is functionally maintained in the cytoplasm of normal epithelial cells by CK2alpha/alpha’-mediated phosphorylation at serine 124, which is dependent on proper targeting of the holoenzyme via the CK2b regulatory subunit. (PMID:25486430)
• CK2 is widely expressed in follicular, Burkitt and diffuse large B-cell lymphomas and may have role in malignant B-cell growth. (PMID:25788269)
• We conclude that this class of chimeric peptides, in addition to altering some properties of CK2 holoenzyme, affects several other cellular targets, causing profound perturbations of cell biology (PMID:25936516)
• results suggest that CK2alpha might play an oncogenic role in hepatocellular carcinoma (PMID:26430962)
• KLF4 acts as a tumor suppressor or oncogene to activate or repress target gene transcription depending on its acetylation status, which is regulated by p21 and CK2 interaction-mediated HDAC2 phosphorylation (PMID:26729194)
• we identify a therapeutically exploitable posttranslational mechanism by which CK2alpha-mediated degradation of BRMS1 promotes metastases in lung cancer (PMID:26980766)
• In this study, the disordered feature of Nopp140 and the effect of CK2alpha on the structure of Nopp140 were examined using single-molecule fluorescence resonance energy transfer (smFRET) and electron paramagnetic resonance (EPR). (PMID:27297113)
• this study shows that breakpoint cluster region protein regulates inflammation development via the alpha subunit of casein kinase II (PMID:27630163)
• These data support a role for casein kinase 2 in regulation of protein synthesis by downregulating stress granule formation through G3BP1. (PMID:27920254)
• CK2 is required to mediate FXR SUMOylation. (PMID:28201649)
• Multiple conformations of kinase II subunit alpha (CK2alpha) hinge region, located near the active site, were observed during the dynamics. (PMID:29243286)
• The influence of the combined treatment on apoptosis in leukemia cells, as well as on cell-cycle progression and the levels of TS, CK2alpha and P-Ser529-p65 were determined. (PMID:30061228)
• Okur-Chung neurodevelopmental syndrome-linked CK2alpha variants have reduced kinase activity. (PMID:33944995)
• CK2alpha causes stemness and chemotherapy resistance in liver cancer through the Hedgehog signaling pathway. (PMID:34548224)
• Casein Kinase 2alpha Augments Oxaliplatin Resistance in Colorectal Cancer Cells by Increasing ABCE1 Expression. (PMID:37247928)
• CSNK2A2 promotes hepatocellular carcinoma progression through activation of NF-kappaB pathway. (PMID:37268061)
• Cell cycle-dependent gene networks for cell proliferation activated by nuclear CK2alpha complexes. (PMID:37907238)
• Protein Kinase CK2alpha’, More than a Backup of CK2alpha. (PMID:38132153)
• Protein kinase CK2alpha is overexpressed in classical hodgkin lymphoma, regulates key signaling pathways, PD-L1 and may represent a new target for therapy. (PMID:38807597)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	csnk2a2a	ENSDARG00000012818
danio_rerio	csnk2a2b	ENSDARG00000013582
mus_musculus	Csnk2a2	ENSMUSG00000046707
rattus_norvegicus	Csnk2a2	ENSRNOG00000011933
drosophila_melanogaster	CkIIalpha	FBGN0264492
caenorhabditis_elegans	kin-3	WBGENE00002191

Paralogs (2): CSNK2A1 (ENSG00000101266), CSNK2A3 (ENSG00000254598)

Protein

Protein identifiers

Casein kinase II subunit alpha’ — P19784 (reviewed: P19784)

All UniProt accessions (3): P19784, H3BNI9, H3BSA1

UniProt curated annotations — full annotation on UniProt →

Function. Catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated serine or threonine. Regulates numerous cellular processes, such as cell cycle progression, apoptosis and transcription, as well as viral infection. May act as a regulatory node which integrates and coordinates numerous signals leading to an appropriate cellular response. During mitosis, functions as a component of the p53/TP53-dependent spindle assembly checkpoint (SAC) that maintains cyclin-B-CDK1 activity and G2 arrest in response to spindle damage. Also required for p53/TP53-mediated apoptosis, phosphorylating ‘Ser-392’ of p53/TP53 following UV irradiation. Phosphorylates a number of DNA repair proteins in response to DNA damage, such as MDC1, RAD9A, RAD51 and HTATSF1, promoting their recruitment to DNA damage sites. Can also negatively regulate apoptosis. Phosphorylates the caspases CASP9 and CASP2 and the apoptotic regulator NOL3. Phosphorylation protects CASP9 from cleavage and activation by CASP8, and inhibits the dimerization of CASP2 and activation of CASP8. Regulates transcription by direct phosphorylation of RNA polymerases I, II, III and IV. Also phosphorylates and regulates numerous transcription factors including NF-kappa-B, STAT1, CREB1, IRF1, IRF2, ATF1, SRF, MAX, JUN, FOS, MYC and MYB. Phosphorylates Hsp90 and its co-chaperones FKBP4 and CDC37, which is essential for chaperone function. Regulates Wnt signaling by phosphorylating CTNNB1 and the transcription factor LEF1. Acts as an ectokinase that phosphorylates several extracellular proteins. During viral infection, phosphorylates various proteins involved in the viral life cycles of EBV, HSV, HBV, HCV, HIV, CMV and HPV. May phosphorylate histone H2A on ‘Ser-1’.

Subunit / interactions. Heterotetramer composed of two catalytic subunits (alpha chain and/or alpha’ chain) and two regulatory subunits (beta chains). The tetramer can exist as a combination of 2 alpha/2 beta, 2 alpha’/2 beta or 1 alpha/1 alpha’/2 beta subunits. Also part of a CK2-SPT16-SSRP1 complex composed of SSRP1, SUPT16H, CSNK2A1, CSNK2A2 and CSNK2B, which forms following UV irradiation. Interacts with CSNK2A2IP (via C-terminus). Interacts with SIRT6; preventing CSNK2A2 localization to the nucleus. Interacts with RNPS1. Interacts with HIRIP3.

Subcellular location. Nucleus. Cytoplasm.

Activity regulation. Constitutively active protein kinase whose activity is not directly affected by phosphorylation. Seems to be regulated by level of expression and localization.

Miscellaneous. Can use both ATP and GTP as phosphoryl donors. Phosphorylation by casein kinase 2 has been estimated to represent up to one quarter of the eukaryotic phosphoproteome.

Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family. CK2 subfamily.

RefSeq proteins (1): NP_001887* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR045216	CK2_alpha	Family

Pfam: PF00069

Enzyme classification (BRENDA):

• EC 2.7.11.1 — non-specific serine/threonine protein kinase (BRENDA: 71 organisms, 682 substrates, 228 inhibitors, 23 Km, 6 kcat entries)

Substrate kinetics (BRENDA)

8 substrates with measured Km, best-characterized 8. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.0007–0.64	11
KKRAARATSNVFA	0.013–0.045	3
PAH1 PHOSPHATIDATE PHOSPHATASE	0.0002	2
RRRLSSLRA	0.0036–0.0037	2
GTP	0.46	1
KKRAARASSNVFA	0.02	1
LYS-LYS-PHE-ASN-ARG-THR-LEU-SER-VAL-ALA	0.0093	1
MYELIN BASIC PROTEIN	0.145	1

Catalyzed reactions (Rhea), 2 shown:

• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)

UniProt features (49 total): helix 21, strand 10, turn 7, modified residue 5, binding site 2, chain 1, domain 1, sequence variant 1, active site 1

Structure

Experimental structures (PDB)

56 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
6TGU	X-RAY DIFFRACTION	0.83
9Q9D	X-RAY DIFFRACTION	0.89
9Q8C	X-RAY DIFFRACTION	0.9
6TE2	X-RAY DIFFRACTION	0.92
9Q9G	X-RAY DIFFRACTION	0.94
9QAB	X-RAY DIFFRACTION	0.95
6HMQ	X-RAY DIFFRACTION	0.97
7ATV	X-RAY DIFFRACTION	0.98
9Q8Q	X-RAY DIFFRACTION	0.98
9QAK	X-RAY DIFFRACTION	0.98
6HMD	X-RAY DIFFRACTION	1
7A22	X-RAY DIFFRACTION	1.01
7A2H	X-RAY DIFFRACTION	1.01
9QAG	X-RAY DIFFRACTION	1.01
9QB0	X-RAY DIFFRACTION	1.01
9R5D	X-RAY DIFFRACTION	1.02
7A1Z	X-RAY DIFFRACTION	1.02
6HMC	X-RAY DIFFRACTION	1.03
8QCD	X-RAY DIFFRACTION	1.03
9Q9A	X-RAY DIFFRACTION	1.03
6HMB	X-RAY DIFFRACTION	1.04
8QCG	X-RAY DIFFRACTION	1.04
9H96	X-RAY DIFFRACTION	1.04
9R5C	X-RAY DIFFRACTION	1.04
7AT9	X-RAY DIFFRACTION	1.05
9QB6	X-RAY DIFFRACTION	1.05
9IHG	X-RAY DIFFRACTION	1.08
6TEW	X-RAY DIFFRACTION	1.08
8QBU	X-RAY DIFFRACTION	1.09
9R5B	X-RAY DIFFRACTION	1.09

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P19784-F1	94.91	0.94

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 157 (proton acceptor)

Ligand- & substrate-binding residues (2): 46–54; 69

Post-translational modifications (5): 13, 18, 21, 97, 288

Function

Pathways and Gene Ontology

Reactome pathways

14 pathways

ID	Pathway
R-HSA-1483191	Synthesis of PC
R-HSA-201688	WNT mediated activation of DVL
R-HSA-2514853	Condensation of Prometaphase Chromosomes
R-HSA-445144	Signal transduction by L1
R-HSA-6804756	Regulation of TP53 Activity through Phosphorylation
R-HSA-6814122	Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding
R-HSA-8934903	Receptor Mediated Mitophagy
R-HSA-8939243	RUNX1 interacts with co-factors whose precise effect on RUNX1 targets is not known
R-HSA-8948751	Regulation of PTEN stability and activity
R-HSA-9755511	KEAP1-NFE2L2 pathway
R-HSA-9768727	Regulation of CDH1 posttranslational processing and trafficking to plasma membrane
R-HSA-9828806	Maturation of hRSV A proteins
R-HSA-9929491	SPOP-mediated proteasomal degradation of PD-L1(CD274)
R-HSA-9931530	Phosphorylation and nuclear translocation of the CRY:PER:kinase complex

MSigDB gene sets: 700 (showing top): PID_BCR_5PATHWAY, GOBP_REGULATION_OF_DOUBLE_STRAND_BREAK_REPAIR, MODULE_52, GOBP_REGULATION_OF_DNA_RECOMBINATION, GOBP_HEPATICOBILIARY_SYSTEM_DEVELOPMENT, GOBP_REGULATION_OF_AUTOPHAGY, GOBP_NEGATIVE_REGULATION_OF_PROTEOLYSIS, GOBP_REGULATION_OF_PROTEASOMAL_UBIQUITIN_DEPENDENT_PROTEIN_CATABOLIC_PROCESS, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, GCANCTGNY_MYOD_Q6, BHATI_G2M_ARREST_BY_2METHOXYESTRADIOL_DN, GOBP_NEGATIVE_REGULATION_OF_DNA_REPAIR, GOBP_PEPTIDYL_SERINE_MODIFICATION, MATTIOLI_MGUS_VS_PCL

GO Biological Process (15): double-strand break repair (GO:0006302), apoptotic process (GO:0006915), DNA damage response (GO:0006974), spermatogenesis (GO:0007283), Wnt signaling pathway (GO:0016055), cerebral cortex development (GO:0021987), negative regulation of proteasomal ubiquitin-dependent protein catabolic process (GO:0032435), liver regeneration (GO:0097421), regulation of mitophagy (GO:1901524), obsolete positive regulation of protein targeting to mitochondrion (GO:1903955), regulation of chromosome separation (GO:1905818), negative regulation of apoptotic signaling pathway (GO:2001234), protein phosphorylation (GO:0006468), regulation of protein catabolic process (GO:0042176), regulation of cell cycle (GO:0051726)

GO Molecular Function (8): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (8): chromatin (GO:0000785), acrosomal vesicle (GO:0001669), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytosol (GO:0005829), protein kinase CK2 complex (GO:0005956), cytoplasm (GO:0005737), PcG protein complex (GO:0031519)

Reactome top-level categories

Rollup of top-14 pathways:

Category	Pathways
Glycerophospholipid biosynthesis	1
TCF dependent signaling in response to WNT	1
Mitotic Prometaphase	1
L1CAM interactions	1
Regulation of TP53 Activity	1
Chaperonin-mediated protein folding	1
Mitophagy	1
Transcriptional regulation by RUNX1	1
PTEN Regulation	1
Cellular response to chemical stress	1
Regulation of CDH1 Expression and Function	1
Respiratory syncytial virus (RSV) genome replication, transcription and translation	1
Regulation of PD-L1(CD274) Post-translational modification	1
Circadian clock	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
apoptotic signaling pathway	2
protein kinase activity	2
DNA repair	1
programmed cell death	1
execution phase of apoptosis	1
cellular response to stress	1
developmental process involved in reproduction	1
male gamete generation	1
cell surface receptor signaling pathway	1
pallium development	1
anatomical structure development	1
regulation of proteasomal ubiquitin-dependent protein catabolic process	1
proteasome-mediated ubiquitin-dependent protein catabolic process	1
negative regulation of proteasomal protein catabolic process	1
negative regulation of ubiquitin-dependent protein catabolic process	1
liver development	1
animal organ regeneration	1
mitophagy	1
regulation of macroautophagy	1
regulation of autophagy of mitochondrion	1
chromosome separation	1
regulation of chromosome segregation	1
negative regulation of signal transduction	1
negative regulation of apoptotic process	1
regulation of apoptotic signaling pathway	1
phosphorylation	1
protein modification process	1
regulation of catabolic process	1
protein catabolic process	1
regulation of protein metabolic process	1
cell cycle	1
regulation of cellular process	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1

Protein interactions and networks

STRING

3783 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CSNK2A2	PLEKHO1	Q53GL0	981
CSNK2A2	N0E472	N0E472	953
CSNK2A2	CSNK2B	P07312	953
CSNK2A2	KMT5B	Q4FZB7	849
CSNK2A2	GGA3	Q9NZ52	764
CSNK2A2	GGA1	Q9UJY5	763
CSNK2A2	KIF5C	O60282	755
CSNK2A2	AP1G2	O75843	752
CSNK2A2	GOPC	Q9HD26	714
CSNK2A2	MAPK1	P28482	710
CSNK2A2	TP53	P04637	702
CSNK2A2	GOLPH3	Q9H4A6	602
CSNK2A2	PACS2	Q86VP3	600
CSNK2A2	HSP90AA1	P07900	592
CSNK2A2	PACS1	Q6VY07	588

IntAct

333 interactions, top by confidence:

A	B	Type	Score
CSNK2B	CSNK2A2	psi-mi:“MI:0915”(physical association)	0.960
CSNK2A2	CSNK2B	psi-mi:“MI:0915”(physical association)	0.960
CSNK2B	CSNK2A2	psi-mi:“MI:0914”(association)	0.960
HEXIM1	CCNT1	psi-mi:“MI:0914”(association)	0.930
CSNK2A1	CSNK2A2	psi-mi:“MI:0914”(association)	0.920
CSNK2A2	CSNK2A1	psi-mi:“MI:0915”(physical association)	0.920
MED4	MED19	psi-mi:“MI:0914”(association)	0.900
RYBP	CSNK2A2	psi-mi:“MI:0914”(association)	0.900
PCGF5	CSNK2A2	psi-mi:“MI:0914”(association)	0.880
POLR2E	POLR3A	psi-mi:“MI:0914”(association)	0.870
MED20	MED19	psi-mi:“MI:0914”(association)	0.840
CSNK2A2	EIF3J	psi-mi:“MI:0914”(association)	0.790
NRP1	CSNK2A2	psi-mi:“MI:0914”(association)	0.790
CSNK2A2	TRIM41	psi-mi:“MI:0915”(physical association)	0.780
TRIM41	CSNK2A2	psi-mi:“MI:0915”(physical association)	0.780
HEXIM2	AHCYL1	psi-mi:“MI:0914”(association)	0.740
VSX1	USP12	psi-mi:“MI:0914”(association)	0.730
RING1	CBX4	psi-mi:“MI:0914”(association)	0.730
TP53	CSNK2A2	psi-mi:“MI:0914”(association)	0.730
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
CSNK2A2	ZNF670	psi-mi:“MI:0915”(physical association)	0.670

BioGRID (1139): TRIM41 (Two-hybrid), LAC1 (Biochemical Activity), Sirt1 (Biochemical Activity), CSNK2A2 (Affinity Capture-Western), CSNK2A2 (Affinity Capture-MS), KDM1A (Affinity Capture-Western), CSNK2A2 (Affinity Capture-Western), KDM1A (Reconstituted Complex), KDM1A (Biochemical Activity), CSNK2B (Two-hybrid), DEC1 (Two-hybrid), BHLHE41 (Two-hybrid), NR1D2 (Two-hybrid), CSNK2A2 (Affinity Capture-MS), CSNK2A2 (Affinity Capture-MS)

ESM2 similar proteins: A2YNT8, A2ZAB5, A9TF79, O54833, O64812, O76484, P0C5D6, P19784, P20427, P21869, P28523, P31748, P31749, P31750, P43291, P43292, P47196, P49136, P49137, P49138, P49139, P68399, P68400, Q01314, Q02066, Q0D4J7, Q16644, Q2QY53, Q39192, Q39193, Q3SYZ2, Q3UMW7, Q5N942, Q66H84, Q6P9R2, Q6ZI44, Q6ZLP5, Q75H77, Q75LR7, Q75V57

Diamond homologs: A0A194WDG1, A8WIP6, A8X5H5, B0Y4X4, B6F107, C4YGK0, G4N374, G4NH08, O04160, O08911, O13352, O23145, O42376, O54833, O61847, O64816, O64817, O76484, O94737, P00546, P08181, P14681, P15790, P18265, P18266, P18334, P19139, P19454, P19784, P20427, P21868, P21869, P23111, P24100, P28020, P28523, P28547, P29618, P29619, P33674

SIGNOR signaling

102 interactions.

A	Effect	B	Mechanism
CSNK2A2	up-regulates	NKX3-1	phosphorylation
CSNK2A2	unknown	SMC3	phosphorylation
CSNK2A2	down-regulates	SET	phosphorylation
CSNK2A2	“down-regulates activity”	EIF4EBP1	phosphorylation
CSNK2A2	“up-regulates activity”	BID	phosphorylation
CSNK2A2	“down-regulates activity”	CTDP1	phosphorylation
CSNK2A2	“up-regulates activity”	EIF2B5	phosphorylation
CSNK2A2	“up-regulates activity”	HDAC1	phosphorylation
CSNK2A2	“up-regulates activity”	HDAC2	phosphorylation
CSNK2A2	unknown	MS4A1	phosphorylation
CSNK2A2	“up-regulates activity”	PTPRC	phosphorylation
CSNK2A2	“down-regulates quantity by destabilization”	SPIB	phosphorylation
CSNK2A2	“up-regulates activity”	UBE2R2	phosphorylation
CSNK2A2	“up-regulates activity”	WAS	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 198 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
RUNX1 interacts with co-factors whose precise effect on RUNX1 targets is not known	10	24.8×	3e-09
Transcriptional Regulation by E2F6	6	14.5×	4e-04
Negative epigenetic regulation of rRNA expression	6	12.9×	6e-04
Regulation of PTEN gene transcription	7	10.3×	5e-04
TP53 Regulates Transcription of DNA Repair Genes	6	9.0×	3e-03
Formation of the ternary complex, and subsequently, the 43S complex	5	8.9×	7e-03
Maturation of DENV proteins	5	8.7×	7e-03
Influenza Infection	6	8.7×	3e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

59 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	24
Likely benign	0
Benign	18

Top pathogenic / likely-pathogenic (0)

SpliceAI

2376 predictions. Top by Δscore:

Variant	Effect	Δscore
16:58163980:A:AC	donor_gain	1.0000
16:58164148:C:CC	acceptor_gain	1.0000
16:58165533:C:CA	donor_gain	1.0000
16:58165546:C:A	donor_gain	1.0000
16:58165554:ACT:A	donor_loss	1.0000
16:58165555:CTC:C	donor_loss	1.0000
16:58165556:TCAC:T	donor_loss	1.0000
16:58165557:CACAG:C	donor_loss	1.0000
16:58165558:A:AC	donor_gain	1.0000
16:58165558:A:C	donor_loss	1.0000
16:58165559:C:CA	donor_gain	1.0000
16:58165559:CA:C	donor_gain	1.0000
16:58165559:CAG:C	donor_gain	1.0000
16:58165559:CAGA:C	donor_gain	1.0000
16:58165559:CAGAA:C	donor_gain	1.0000
16:58165704:AATGT:A	acceptor_gain	1.0000
16:58165705:ATGT:A	acceptor_gain	1.0000
16:58165706:TGT:T	acceptor_gain	1.0000
16:58165707:GT:G	acceptor_gain	1.0000
16:58165708:TC:T	acceptor_loss	1.0000
16:58165709:C:CA	acceptor_loss	1.0000
16:58165709:C:CC	acceptor_gain	1.0000
16:58165710:T:A	acceptor_loss	1.0000
16:58166577:TACT:T	donor_loss	1.0000
16:58166578:A:AC	donor_gain	1.0000
16:58166579:C:CC	donor_gain	1.0000
16:58166579:CT:C	donor_loss	1.0000
16:58166579:CTTA:C	donor_gain	1.0000
16:58166580:TT:T	donor_loss	1.0000
16:58166581:TACTG:T	donor_loss	1.0000

AlphaMissense

2323 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
16:58165597:T:A	R313S	1.000
16:58165597:T:G	R313S	1.000
16:58165598:C:G	R313T	1.000
16:58167226:C:T	G236E	1.000
16:58167274:C:T	G220D	1.000
16:58167275:C:G	G220R	1.000
16:58167284:A:G	W217R	1.000
16:58167284:A:T	W217R	1.000
16:58167289:T:A	D215V	1.000
16:58167290:C:G	D215H	1.000
16:58167698:A:G	L204P	1.000
16:58167698:A:T	L204H	1.000
16:58167701:A:G	L203P	1.000
16:58167711:C:G	G200R	1.000
16:58167711:C:T	G200R	1.000
16:58167712:C:A	K199N	1.000
16:58167712:C:G	K199N	1.000
16:58167715:G:C	F198L	1.000
16:58167715:G:T	F198L	1.000
16:58167717:A:G	F198L	1.000
16:58167722:C:A	R196M	1.000
16:58167726:A:G	S195P	1.000
16:58167728:G:T	A194D	1.000
16:58167763:G:C	F182L	1.000
16:58167763:G:T	F182L	1.000
16:58167765:A:G	F182L	1.000
16:58167773:A:G	L179P	1.000
16:58167773:A:T	L179Q	1.000
16:58167777:C:A	G178C	1.000
16:58167777:C:G	G178R	1.000

dbSNP variants (sampled 300 via entrez): RS1000022059 (16:58196472 A>G), RS1000136006 (16:58158106 C>T), RS1000136449 (16:58196667 G>A), RS1000153042 (16:58187965 T>C), RS1000242697 (16:58160362 T>C), RS1000271824 (16:58194378 C>A), RS1000273027 (16:58189992 TA>T), RS1000304372 (16:58194750 T>C), RS1000408395 (16:58167008 T>C), RS1000417779 (16:58173360 A>G), RS1000484259 (16:58187557 T>C,G), RS1000530764 (16:58173051 C>A), RS1000547309 (16:58163705 T>C), RS1000614618 (16:58185317 A>C), RS1000666911 (16:58185073 C>A,T)

Disease associations

OMIM: gene MIM:115442 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

48 total (30 of 48 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000023	Inguinal hernia
HP:0000218	High palate
HP:0000219	Thin upper lip vermilion
HP:0000252	Microcephaly
HP:0000286	Epicanthus
HP:0000316	Hypertelorism
HP:0000347	Micrognathia
HP:0000369	Low-set ears
HP:0000378	Cupped ear
HP:0000396	Overfolded helix
HP:0000431	Wide nasal bridge
HP:0000463	Anteverted nares
HP:0000508	Ptosis
HP:0000537	Epicanthus inversus
HP:0000664	Synophrys
HP:0000750	Delayed speech and language development
HP:0000954	Single transverse palmar crease
HP:0001156	Brachydactyly
HP:0001249	Intellectual disability
HP:0001251	Ataxia
HP:0001252	Hypotonia
HP:0001263	Global developmental delay
HP:0001302	Pachygyria
HP:0001344	Absent speech
HP:0001382	Joint hypermobility
HP:0001508	Failure to thrive
HP:0001537	Umbilical hernia
HP:0001561	Polyhydramnios
HP:0001627	Abnormal heart morphology

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST002437_1	Telomere length	5.000000e-08
GCST004302_22	Primary biliary cholangitis	2.000000e-08
GCST005752_147	Systemic lupus erythematosus	3.000000e-06
GCST005752_34	Systemic lupus erythematosus	1.000000e-07
GCST005790_39	Rosacea symptom severity	2.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0009180	rosacea severity measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL2095191 (PROTEIN COMPLEX GROUP), CHEMBL3832943 (PROTEIN FAMILY), CHEMBL3883328 (PROTEIN COMPLEX), CHEMBL4070 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

70 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 549,945 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL58	MITOXANTRONE	4	166,878
CHEMBL1078178	MOMELOTINIB	4	3,481
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1289926	AXITINIB	4	15,732
CHEMBL1614701	SELUMETINIB	4	10,221
CHEMBL1789941	RUXOLITINIB	4	11,547
CHEMBL189963	PALBOCICLIB	4	13,102
CHEMBL2035187	PACRITINIB	4	3,345
CHEMBL3301610	ABEMACICLIB	4	7,045
CHEMBL3301622	GILTERITINIB	4	2,395
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL941	IMATINIB	4	111,611
CHEMBL50	QUERCETIN	3	74,559
CHEMBL3265032	ENTOSPLETINIB	3	1,628
CHEMBL274654	ORANTINIB	3	3,596
CHEMBL3137331	DEFACTINIB	3	1,229
CHEMBL415049	BARASERTIB	3	2,371
CHEMBL428690	ALVOCIDIB	3	27,781
CHEMBL483158	ALISERTIB	3	2,305
CHEMBL522892	DOVITINIB	3
CHEMBL603469	LESTAURTINIB	3
CHEMBL91829	RUBOXISTAURIN	3
CHEMBL1230165	SILMITASERTIB	2
CHEMBL31574	FISETIN	2
CHEMBL6246	ELLAGIC ACID	2
CHEMBL105442	CI-1040	2
CHEMBL151	LUTEOLIN	2
CHEMBL1738758	ONVANSERTIB	2
CHEMBL8260	BAICALEIN	2

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Casein kinase 2 (CK2) family

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
silmitasertib	Inhibition	9.0	pIC50
compound 2c [PMID: 22115617]	Inhibition	7.68	pKi

Binding affinities (BindingDB)

110 measured of 110 human assays (111 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
5-[[4-[(1,5-dimethyl-1,2,4-triazol-3-yl)amino]-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]-1-methylindazole-3-carbonitrile	IC50	0.13 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl N-[(3S,4R)-1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-fluoropiperidin-4-yl]carbamate	IC50	0.14 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[(3-cyano-1-methylindazol-5-yl)amino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.15 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-(hydroxymethyl)anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.16 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-(3-hydroxypyrrolidin-1-yl)anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.17 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[3-(3-methoxypyrrolidin-1-yl)azetidin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.21 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[3-(1-acetylpiperidin-4-yl)-2-chloro-5-cyanoanilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.21 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[4-[(1,1-dioxothiolan-3-yl)amino]piperidin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.22 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[[3-cyano-1-[1-[(2R)-2-hydroxypropyl]piperidin-4-yl]indazol-5-yl]amino]-4-(ethylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.22 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-(morpholin-4-ylamino)anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.23 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-(2-chloro-5-cyano-3-ethenylanilino)-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.23 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[3-(3-methylsulfonylpyrrolidin-1-yl)azetidin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.24 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl N-[(3S,4R)-1-[1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]azetidin-3-yl]-4-methylpyrrolidin-3-yl]carbamate	IC50	0.27 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl N-[(3R,4R)-1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-phosphonooxypiperidin-4-yl]carbamate	IC50	0.27 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[[3-cyano-1-[1-[(2S)-2-hydroxypropyl]piperidin-4-yl]indazol-5-yl]amino]-4-(ethylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.27 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[3-[1-(1-acetylazetidin-3-yl)piperidin-4-yl]-2-chloro-5-cyanoanilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.28 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[4-(oxolan-3-yl)piperazin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.29 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
4-chloro-3-[[4-(cyclopropylamino)-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]-5-[6-fluoro-4-(oxetan-3-yl)-1,4-diazepan-1-yl]benzonitrile	IC50	0.29 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[4-[(2R)-2-hydroxypropyl]piperazin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.3 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[4-[(3-hydroxycyclobutyl)amino]piperidin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.3 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[3-(3-hydroxyazetidin-1-yl)azetidin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.3 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	0.31 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
3-[[4-(cyclopropylamino)-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]-4-fluoro-5-[3-(4-methylpiperazin-1-yl)azetidin-1-yl]benzonitrile	IC50	0.39 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl N-[(3R,4R)-1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-hydroxypiperidin-4-yl]carbamate	IC50	0.41 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl N-[(3S,4S)-1-[2-chloro-5-cyano-3-[[4-(ethylamino)-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-hydroxypiperidin-4-yl]carbamate	IC50	0.52 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl N-[(3S,4S)-1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-hydroxypiperidin-4-yl]carbamate	IC50	0.72 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl N-[(3S,4S)-1-[1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-4-yl]-4-methylpyrrolidin-3-yl]carbamate	IC50	1.31 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[[1-(oxetan-3-yl)piperidin-4-yl]amino]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.32 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
4-chloro-3-[[4-(ethylamino)-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]-5-[4-[[(2R)-2-hydroxypropyl]amino]piperidin-1-yl]benzonitrile	IC50	1.33 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[3-[1-[3,3-bis(hydroxymethyl)cyclobutyl]piperidin-4-yl]-2-chloro-5-cyanoanilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.34 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl 4-[4-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperazin-1-yl]piperidine-1-carboxylate	IC50	1.35 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
oxetan-3-yl 4-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidine-1-carboxylate	IC50	1.35 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
oxetan-3-yl N-[(3R,4R)-1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-hydroxypiperidin-4-yl]carbamate	IC50	1.36 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
4-chloro-3-[[4-(cyclopropylamino)-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]-5-[4-[(3,3-difluorocyclobutyl)amino]piperidin-1-yl]benzonitrile	IC50	1.37 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
N-[(3R,4R)-1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-hydroxypiperidin-4-yl]-2-(4-methylpiperazin-1-yl)acetamide	IC50	1.37 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[3-[(4aR,8aR)-1-(oxetan-3-yl)-3,4a,5,7,8,8a-hexahydro-2H-pyrido[3,4-b][1,4]oxazin-6-yl]-2-chloro-5-cyanoanilino]-4-(ethylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.37 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[4-(oxetan-3-yl)piperazin-1-yl]anilino]-4-(ethylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.39 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[4-(2,2-difluoroethyl)piperazin-1-yl]anilino]-4-(ethylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.39 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-(6-methyl-2,6-diazaspiro[3.3]heptan-2-yl)anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.4 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
4-chloro-3-[[4-(cyclopropylamino)-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]-5-[3-(morpholine-4-carbonyl)-4-(oxetan-3-yl)piperazin-1-yl]benzonitrile	IC50	1.4 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-(difluoromethyl)-3-[4-(3-methyloxetan-3-yl)piperazin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.42 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
4-chloro-3-[[4-(ethylamino)-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]-5-piperidin-4-ylbenzonitrile	IC50	1.42 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[4-(2-methylsulfonylethyl)piperazin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.44 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[[3-cyano-1-[1-(oxetan-3-yl)piperidin-4-yl]indazol-5-yl]amino]-4-(ethylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.44 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-(difluoromethyl)-3-[4-(1-methylazetidin-3-yl)piperazin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.5 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-methoxyethyl N-[(3R,4R)-1-[2-chloro-5-cyano-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-hydroxypiperidin-4-yl]carbamate	IC50	1.53 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
2-[2-chloro-5-cyano-3-[4-[(3-cyanocyclobutyl)amino]piperidin-1-yl]anilino]-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile	IC50	1.56 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
Staurosporine	KD	1.7 nM
methyl N-[(3S,4R)-1-[2-chloro-3-[[7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl]amino]-5-(difluoromethyl)phenyl]-4-methoxypyrrolidin-3-yl]carbamate	IC50	3.83 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors
methyl N-[(3R,4R)-1-[2-chloro-5-cyano-3-[[4-(ethylamino)-7-isocyanoimidazo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]-3-hydroxypiperidin-4-yl]carbamate	IC50	4.71 nM	US-8940736: Imidazotriazinecarbonitriles useful as kinase inhibitors

ChEMBL bioactivities

1086 potent at pChembl≥5 of 1186 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.52	IC50	0.03	nM	CHEMBL3699289
10.15	IC50	0.07	nM	CHEMBL3699235
10.08	Ki	0.084	nM	CHEMBL5419810
10.05	IC50	0.09	nM	CHEMBL3699276
10.05	IC50	0.09	nM	CHEMBL3699234
9.96	IC50	0.11	nM	CHEMBL3699295
9.96	IC50	0.11	nM	CHEMBL3699252
9.96	IC50	0.11	nM	CHEMBL3699237
9.89	IC50	0.13	nM	CHEMBL3699282
9.82	IC50	0.15	nM	CHEMBL3699244
9.80	IC50	0.16	nM	CHEMBL3699294
9.80	IC50	0.16	nM	CHEMBL3699266
9.70	IC50	0.2	nM	CHEMBL3699238
9.68	IC50	0.21	nM	CHEMBL3699278
9.68	IC50	0.21	nM	CHEMBL3699292
9.66	Ki	0.22	nM	SILMITASERTIB
9.64	IC50	0.23	nM	CHEMBL3699296
9.64	IC50	0.23	nM	CHEMBL3699262
9.64	IC50	0.23	nM	CHEMBL4848224
9.60	IC50	0.25	nM	CHEMBL3699280
9.59	IC50	0.26	nM	CHEMBL3699259
9.57	IC50	0.27	nM	CHEMBL3699291
9.57	IC50	0.27	nM	CHEMBL3699255
9.57	IC50	0.27	nM	CHEMBL3699256
9.57	IC50	0.27	nM	CHEMBL3699267
9.55	IC50	0.28	nM	CHEMBL3699239
9.52	IC50	0.3	nM	SILMITASERTIB
9.51	IC50	0.31	nM	CHEMBL3699253
9.46	IC50	0.35	nM	CHEMBL3699257
9.42	Ki	0.38	nM	SILMITASERTIB
9.40	IC50	0.4	nM	CHEMBL1934184
9.38	Ki	0.42	nM	CHEMBL4846181
9.38	Ki	0.42	nM	CHEMBL1682283
9.35	IC50	0.45	nM	CHEMBL3699277
9.34	IC50	0.46	nM	CHEMBL4862003
9.33	IC50	0.47	nM	CHEMBL3699269
9.31	IC50	0.49	nM	CHEMBL3699254
9.31	IC50	0.49	nM	CHEMBL3699258
9.30	IC50	0.5	nM	CHEMBL1934172
9.30	IC50	0.5	nM	CHEMBL1934181
9.30	IC50	0.5	nM	CHEMBL1934182
9.28	IC50	0.52	nM	CHEMBL3699286
9.27	IC50	0.54	nM	CHEMBL3699250
9.22	IC50	0.6	nM	CHEMBL4872225
9.22	IC50	0.6	nM	CHEMBL1934180
9.21	IC50	0.61	nM	CHEMBL3699285
9.21	IC50	0.61	nM	CHEMBL3699287
9.21	IC50	0.61	nM	CHEMBL4875513
9.19	IC50	0.64	nM	CHEMBL3699260
9.18	IC50	0.66	nM	CHEMBL4860630

PubChem BioAssay actives

864 with measured affinity, of 3049 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(2S)-6-amino-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2R)-3-carboxy-2-[8-(4,5,6,7-tetraiodobenzimidazol-1-yl)octanoylamino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]hexanoic acid	2028056: Binding affinity to CK2 (unknown origin) assessed as inhibition constant	ki	0.0001	uM
2-fluoroethyl 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylate	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0002	uM
5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ki	0.0002	uM
5-(3-cyanoanilino)pyrimido[4,5-c]quinoline-8-carboxylic acid	1750468: Inhibition of CK2 (unknown origin)	ki	0.0004	uM
5-(5-chlorothiophen-2-yl)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0004	uM
5-(3-ethynylanilino)pyrimido[4,5-c]quinoline-8-carboxylic acid	2028056: Binding affinity to CK2 (unknown origin) assessed as inhibition constant	ki	0.0004	uM
5-thiophen-3-ylbenzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0005	uM
5-(4-chlorophenyl)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0005	uM
5-(4-chlorophenyl)-3-(ethylamino)pyrimido[4,5-c]quinoline-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0005	uM
5-(3-chloroanilino)-N-(2-morpholin-4-ylethyl)benzo[c][2,6]naphthyridine-8-carboxamide	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0005	uM
2,2-difluoroethyl 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylate	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0006	uM
2-hydroxyethyl 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylate	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0006	uM
3-(cyclopropylamino)-5-phenylpyrimido[4,5-c]quinoline-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0006	uM
5-(3-chloroanilino)-N-(2-hydroxyethyl)benzo[c][2,6]naphthyridine-8-carboxamide	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0007	uM
5-[4-[2-aminoethyl(ethyl)amino]-3-(1,2,4-triazol-4-yl)anilino]-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile	2066663: Inhibition of CSNK2A2 (unknown origin) in presence of ATP by Eurofins radiometric enzymatic assay	ic50	0.0007	uM
2-iodoethyl 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylate	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0008	uM
methyl 3-[[5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carbonyl]amino]propanoate	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0008	uM
N-(2-aminoethyl)-5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxamide	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0009	uM
5-(4-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid	566117: Inhibition of human recombinant CK2 assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay	ic50	0.0010	uM
5-(3-hydroxyphenyl)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0010	uM
5-(3-chlorophenyl)sulfanylbenzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0010	uM
N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-[2-(dimethylamino)ethyl-methylamino]phenyl]acetamide	1301598: Inhibition of CK2 in human DLD1 HA-myr-AKT1 cells assessed as suppression of AKTser129 phosphorylation after 3 to 24 hrs by Western blot analysis	ic50	0.0010	uM
5-phenylbenzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0011	uM
5-(4-fluorophenyl)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0012	uM
5-(3-fluorophenyl)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0013	uM
5-[[8-(hydroxyamino)-8-oxooctyl]amino]benzo[c][2,6]naphthyridine-8-carboxylic acid;2,2,2-trifluoroacetic acid	1652189: Inhibition of human recombinant CK2 using RRRDDDSDDD peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0017	uM
N-(2-bromoethyl)-5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxamide	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0018	uM
N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-methylphenyl]acetamide	1301598: Inhibition of CK2 in human DLD1 HA-myr-AKT1 cells assessed as suppression of AKTser129 phosphorylation after 3 to 24 hrs by Western blot analysis	ic50	0.0020	uM
5-[(3-chlorophenyl)methyl]benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0021	uM
4-(6,8-dibromo-3-hydroxy-4-oxochromen-2-yl)benzoic acid	2028061: Inhibition of human recombinant CK2 using RRRDDDSDDD peptide as substrate incubated for 20 mins in presence of [gamma-32p]-ATP and ATP by beta-counter analysis	ki	0.0025	uM
5-(3-aminophenyl)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0027	uM
2-N-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-4-N-(1-methylimidazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine	1067929: Inhibition of human CK2alpha2	ic50	0.0027	uM
5-(3-chlorophenyl)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0029	uM
5-(2-phenylethylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid	566117: Inhibition of human recombinant CK2 assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay	ic50	0.0030	uM
5-(3-cyanoanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid	566117: Inhibition of human recombinant CK2 assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay	ic50	0.0030	uM
7-(cyclopropylamino)-5-[2-fluoro-5-(1,2,4-triazol-4-yl)anilino]pyrazolo[1,5-a]pyrimidine-3-carbonitrile	2066608: Inhibition of NLuc-fused CSNK2A2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NanoBRET assay	ic50	0.0032	uM
(2Z)-7-bromo-2-[(3-bromo-4-hydroxyphenyl)methylidene]-1-benzofuran-3-one	1934407: Inhibition of recombinant human CK2 using RRRDDDSDDD as substrate in presence of [gamma-33P-ATP] incubated for 20 mins by beta-counter analysis	ic50	0.0033	uM
3,3-dichloropropyl 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylate	1750390: Inhibition of human CK2 incubated for 2 hrs	ic50	0.0034	uM
5-[[6-(hydroxyamino)-6-oxohexyl]amino]benzo[c][2,6]naphthyridine-8-carboxylic acid;2,2,2-trifluoroacetic acid	1652189: Inhibition of human recombinant CK2 using RRRDDDSDDD peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0035	uM
5-(3-carbamoylphenyl)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0035	uM
5-(3-hydroxyphenyl)pyrimido[4,5-c]quinoline-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0035	uM
5-(3-chlorophenoxy)benzo[c][2,6]naphthyridine-8-carboxylic acid	637248: Inhibition of human recombinant CK2alpha/CK2beta using RRRDDDSDDD peptide as substrate by radiometric assay	ic50	0.0037	uM
N-[2-[[(2R)-2-aminopropyl]-methylamino]-5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]acetamide	1301598: Inhibition of CK2 in human DLD1 HA-myr-AKT1 cells assessed as suppression of AKTser129 phosphorylation after 3 to 24 hrs by Western blot analysis	ic50	0.0040	uM
N-[2-[[(2S)-2-aminopropyl]-methylamino]-5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]acetamide	1301598: Inhibition of CK2 in human DLD1 HA-myr-AKT1 cells assessed as suppression of AKTser129 phosphorylation after 3 to 24 hrs by Western blot analysis	ic50	0.0040	uM
6,8-dibromo-2-(4-hydroxy-3-methoxyphenyl)chromen-4-one	779046: Inhibition of recombinant human CK2 using RRRDDDSDDD as substrate after 20 mins by beta counting analysis in presence of [gamma-labeled 32P]ATP	ic50	0.0040	uM
7-(cyclopropylamino)-5-[3-(1,2,4-triazol-4-yl)anilino]pyrazolo[1,5-a]pyrimidine-3-carbonitrile	2066608: Inhibition of NLuc-fused CSNK2A2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NanoBRET assay	ic50	0.0040	uM
3-[(6-methyl-5-phenylthieno[2,3-d]pyrimidin-4-yl)amino]benzoic acid	1294149: Competitive inhibition of recombinant human CK2 holoenzyme by Lineweaver-Burk plot analysis	ki	0.0040	uM
5-(3-methoxyanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid	566117: Inhibition of human recombinant CK2 assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay	ic50	0.0040	uM
5-(3-chloro-4-fluoroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid	566117: Inhibition of human recombinant CK2 assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay	ic50	0.0040	uM
5-(4-phenoxyanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid	566117: Inhibition of human recombinant CK2 assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay	ic50	0.0040	uM

CTD chemical–gene interactions

65 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects expression, decreases expression	3
sodium arsenite	affects binding, increases reaction, increases expression	3
trichostatin A	affects cotreatment, decreases expression	2
cobaltous chloride	increases expression	2
Valproic Acid	affects expression, increases expression	2
aristolochic acid I	decreases expression, increases expression	1
GSK-J4	increases expression	1
bisphenol F	increases expression	1
TAK-243	increases sumoylation	1
multi-kinase inhibitor 108600	affects binding, affects folding, decreases reaction, decreases activity	1
triphenyl phosphate	affects expression	1
nobiletin	decreases expression, decreases reaction	1
sodium arsenate	decreases expression, decreases reaction	1
VX-agent	increases expression	1
quercitrin	affects expression	1
tetrabromobisphenol A	decreases expression	1
potassium chromate(VI)	affects cotreatment, increases expression	1
beta-methylcholine	affects expression	1
epigallocatechin gallate	affects cotreatment, increases expression	1
perfluorooctane sulfonic acid	increases expression	1
U 0126	affects expression, affects reaction	1
K 7174	increases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
Resveratrol	increases expression	1
Decitabine	increases expression	1
Sunitinib	increases expression	1

ChEMBL screening assays

793 unique, capped per target: 648 binding, 145 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1020723	Binding	Inhibition of human CK2 at 10 umol/L	Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). — J Med Chem
CHEMBL620984	Functional	Inhibition of CK-II-mediated 60S acidic ribosomal P protein activity at 10 uM	Casein kinase II inhibitors isolated from two Brazilian plants Hymenaea parvifolia and Wulffia baccata. — Bioorg Med Chem Lett

Cellosaurus cell lines

6 cell lines: 5 cancer cell line, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_D7N1	Ubigene A-549 CSNK2A2 KO	Cancer cell line	Male
CVCL_D8JI	Ubigene HCT 116 CSNK2A2 KO	Cancer cell line	Male
CVCL_D9CJ	Ubigene HEK293 CSNK2A2 KO	Transformed cell line	Female
CVCL_E0B8	Ubigene HeLa CSNK2A2 KO	Cancer cell line	Female
CVCL_SJ93	HAP1 CSNK2A2 (-) 1	Cancer cell line	Male
CVCL_SJ94	HAP1 CSNK2A2 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.