CSNK2A1
gene geneOn this page
Also known as Cka1Cka2
Summary
CSNK2A1 (casein kinase 2 alpha 1, HGNC:2457) is a protein-coding gene on chromosome 20p13, encoding Casein kinase II subunit alpha (P68400). 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.
Casein kinase II 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 rhythm. The kinase exists as a tetramer and is composed of an alpha, an alpha-prime, and two beta subunits. The alpha subunits contain the catalytic activity while the beta subunits undergo autophosphorylation. The protein encoded by this gene represents the alpha subunit. Multiple transcript variants encoding different protein isoforms have been found for this gene.
Source: NCBI Gene 1457 — RefSeq curated summary.
At a glance
- Gene–disease (curated): syndromic intellectual disability (Definitive, ClinGen) — +1 more curated relationship
- GWAS associations: 5
- Clinical variants (ClinVar): 281 total — 35 pathogenic, 35 likely-pathogenic
- Druggable target: yes — 36 molecules with ChEMBL bioactivity
- Dosage sensitivity (ClinGen): haploinsufficiency little evidence, triplosensitivity no evidence
- MANE Select transcript:
NM_177559
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:2457 |
| Approved symbol | CSNK2A1 |
| Name | casein kinase 2 alpha 1 |
| Location | 20p13 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | Cka1, Cka2 |
| Ensembl gene | ENSG00000101266 |
| Ensembl biotype | protein_coding |
| OMIM | 115440 |
| Entrez | 1457 |
Gene structure
Transcript identifiers
Ensembl transcripts: 68 — 50 protein_coding, 14 retained_intron, 4 nonsense_mediated_decay
ENST00000217244, ENST00000349736, ENST00000400217, ENST00000400227, ENST00000460062, ENST00000608066, ENST00000608490, ENST00000609525, ENST00000609606, ENST00000619801, ENST00000642160, ENST00000642673, ENST00000642689, ENST00000643600, ENST00000643602, ENST00000643641, ENST00000643660, ENST00000643680, ENST00000643700, ENST00000643910, ENST00000643968, ENST00000643980, ENST00000644003, ENST00000644170, ENST00000644177, ENST00000644448, ENST00000644710, ENST00000644885, ENST00000645091, ENST00000645187, ENST00000645234, ENST00000645249, ENST00000645260, ENST00000645334, ENST00000645623, ENST00000645641, ENST00000645768, ENST00000645840, ENST00000645910, ENST00000646305, ENST00000646443, ENST00000646477, ENST00000646561, ENST00000646814, ENST00000646908, ENST00000647026, ENST00000647155, ENST00000647348, ENST00000858421, ENST00000858422, ENST00000858423, ENST00000858424, ENST00000858425, ENST00000858426, ENST00000858427, ENST00000858428, ENST00000858429, ENST00000858430, ENST00000922657, ENST00000922658, ENST00000922659, ENST00000922660, ENST00000922661, ENST00000922662, ENST00000948675, ENST00000948676, ENST00000948677, ENST00000948678
RefSeq mRNA: 5 — MANE Select: NM_177559
NM_001362770, NM_001362771, NM_001895, NM_177559, NM_177560
CCDS: CCDS13003, CCDS13004
Canonical transcript exons
ENST00000217244 — 14 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000655087 | 486376 | 486462 |
| ENSE00000655088 | 487427 | 487575 |
| ENSE00000655089 | 488678 | 488778 |
| ENSE00001387136 | 527933 | 528049 |
| ENSE00001709328 | 508451 | 508660 |
| ENSE00003461081 | 497721 | 497780 |
| ENSE00003493190 | 505118 | 505229 |
| ENSE00003533811 | 492254 | 492364 |
| ENSE00003598248 | 499833 | 499934 |
| ENSE00003601224 | 495719 | 495802 |
| ENSE00003670561 | 499255 | 499305 |
| ENSE00003676631 | 489780 | 489881 |
| ENSE00003819107 | 472498 | 484076 |
| ENSE00003829049 | 543672 | 543790 |
Expression profiles
Bgee: expression breadth ubiquitous, 301 present calls, max score 98.04.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 51.1882 / max 385.0800, expressed in 1821 samples.
FANTOM5 promoters (4 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 185975 | 26.9510 | 1811 |
| 185974 | 21.7593 | 1808 |
| 185976 | 1.9317 | 1074 |
| 185973 | 0.5462 | 302 |
Top tissues by expression
301 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| cortical plate | UBERON:0005343 | 98.04 | gold quality |
| ganglionic eminence | UBERON:0004023 | 97.88 | gold quality |
| ventricular zone | UBERON:0003053 | 97.58 | gold quality |
| colonic epithelium | UBERON:0000397 | 97.38 | gold quality |
| adrenal tissue | UBERON:0018303 | 97.06 | gold quality |
| embryo | UBERON:0000922 | 96.39 | gold quality |
| gingival epithelium | UBERON:0001949 | 96.04 | gold quality |
| calcaneal tendon | UBERON:0003701 | 95.96 | gold quality |
| islet of Langerhans | UBERON:0000006 | 95.88 | gold quality |
| rectum | UBERON:0001052 | 95.71 | gold quality |
| stromal cell of endometrium | CL:0002255 | 95.63 | gold quality |
| gastrocnemius | UBERON:0001388 | 95.46 | gold quality |
| muscle of leg | UBERON:0001383 | 95.45 | gold quality |
| amniotic fluid | UBERON:0000173 | 95.32 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 95.32 | gold quality |
| tonsil | UBERON:0002372 | 95.16 | gold quality |
| secondary oocyte | CL:0000655 | 95.08 | gold quality |
| monocyte | CL:0000576 | 94.90 | gold quality |
| gingiva | UBERON:0001828 | 94.74 | gold quality |
| mononuclear cell | CL:0000842 | 94.65 | gold quality |
| gall bladder | UBERON:0002110 | 94.56 | gold quality |
| leukocyte | CL:0000738 | 94.51 | gold quality |
| esophagus squamous epithelium | UBERON:0006920 | 94.11 | gold quality |
| bone marrow cell | CL:0002092 | 94.04 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 93.94 | gold quality |
| esophagus mucosa | UBERON:0002469 | 93.93 | gold quality |
| epithelium of esophagus | UBERON:0001976 | 93.87 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 93.86 | gold quality |
| penis | UBERON:0000989 | 93.84 | gold quality |
| right testis | UBERON:0004534 | 93.77 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 8.12 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): ETS1, FOS, HHEX, NFKB1, NFKB, PDX1, RELA, SP1, SP3, TAL1
miRNA regulators (miRDB)
105 targeting CSNK2A1, 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-188-3P | 100.00 | 68.76 | 1240 |
| HSA-MIR-5011-5P | 100.00 | 83.46 | 5820 |
| HSA-MIR-8485 | 100.00 | 77.57 | 4731 |
| HSA-MIR-190A-3P | 100.00 | 80.35 | 5520 |
| HSA-MIR-4682 | 100.00 | 68.89 | 1258 |
| HSA-MIR-1252-5P | 100.00 | 69.80 | 2774 |
| HSA-MIR-432-3P | 100.00 | 67.86 | 705 |
| HSA-MIR-3646 | 100.00 | 73.56 | 5283 |
| HSA-MIR-3667-3P | 99.99 | 67.17 | 1636 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-548N | 99.98 | 71.94 | 4170 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-548AA | 99.96 | 70.64 | 3753 |
| HSA-MIR-548AP-3P | 99.96 | 70.64 | 3753 |
| HSA-MIR-548T-3P | 99.96 | 70.64 | 3753 |
| HSA-MIR-590-3P | 99.96 | 74.34 | 6478 |
| HSA-MIR-3912-5P | 99.95 | 66.11 | 925 |
| HSA-MIR-4648 | 99.91 | 67.00 | 710 |
| HSA-MIR-1305 | 99.91 | 71.43 | 3443 |
| HSA-MIR-548E-5P | 99.89 | 72.73 | 4486 |
| HSA-MIR-6780A-5P | 99.88 | 66.69 | 2776 |
| HSA-MIR-6124 | 99.87 | 69.78 | 3551 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-4698 | 99.84 | 71.41 | 4303 |
| HSA-MIR-6785-5P | 99.82 | 68.68 | 4428 |
| HSA-MIR-1273H-5P | 99.77 | 66.32 | 2471 |
| HSA-MIR-3934-3P | 99.76 | 65.51 | 1351 |
| HSA-MIR-4319 | 99.76 | 69.83 | 2586 |
| HSA-MIR-3617-5P | 99.75 | 69.41 | 1968 |
| HSA-MIR-641 | 99.75 | 69.35 | 1975 |
Functional genomics
ClinGen dosage: haploinsufficiency 1 (little evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map
Literature-anchored findings (GeneRIF, showing 40)
- uPA-dependent VSMC adhesion is a function of selective Vn phosphorylation by the ectoprotein kinase CK2 (PMID:11756447)
- Generation of mutants of CK2alpha which are dependent on the beta-subunit for catalytic activity (PMID:11827164)
- HIV-1 Rev transactivator: a beta-subunit directed substrate and effector of protein kinase CK2 (PMID:11827166)
- Protein kinase CK2: signaling and tumorigenesis in the mammary gland. (PMID:11827167)
- Response of cancer cells to molecular interruption of the CK2 signal. (PMID:11827168)
- Functional specialization of CK2 isoforms and characterization of isoform-specific binding partners (PMID:11827170)
- Characterization of CK2 holoenzyme variants with regard to crystallization (PMID:11827171)
- Transcriptional coordination of the genes encoding catalytic (CK2alpha) and regulatory (CK2beta) subunits of human protein kinase CK2. (PMID:11827174)
- Consequences of CK2 signaling to the nuclear matrix. (PMID:11827176)
- Localization of individual subunits of protein kinase CK2 to the endoplasmic reticulum and to the Golgi apparatus (PMID:11827177)
- Interactions between protein kinase CK2 and Pin1. Evidence for phosphorylation-dependent interactions. (PMID:11940573)
- Unique activation mechanism of protein kinase CK2. The N-terminal segment is essential for constitutive activity of the catalytic subunit but not of the holoenzyme (PMID:11956194)
- 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 and 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)
- 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)
- This protein is associated with the COP9 signalosome. (PMID:12628923)
- HSF1 activation by heat is correlated with the thermal activation of nuclear CK2 and overexpression of CK2 activates HSF1 (PMID:12659875)
- results indicate that protein kinase CKII may control IkappaBalpha and p27Kip1 degradation and thereby G1/S phase transition through the phosphorylation of threonine 10 within CKBBP1 protein (PMID:12748192)
- Crystal structure of a C-terminal deletion mutant of human protein kinase CK2 catalytic subunit (PMID:12860116)
- Evaluation of different pathways involved in death signaling suggest that the regulation of a critical proapoptotic step in HuH-7 cells by CK2alpha" is mediated by a JNK signaling cascade. (PMID:14962846)
- structure activity relationship: the PA 382-384 mutant exhibits an increased thermal and proteolytic stability (PMID:15108354)
- might play an important role in vivo in regulating the function and transport activity of ABCA1 and possibly of other members of the ABCA subfamily (PMID:15218032)
- Utilizing a kinase-driven assay biochemical purification, the authors identified casein kinase II (CKII) from HeLa cell nuclear extract as a cellular phosphoprotein pp32 kinase. (PMID:15287743)
- CK2 acts as an inhibitor of Cdk5 in the brain (PMID:15342635)
- Involvement of ubiquitous protein kinase CK2 in angiogenesis. Naturally derived CK2 inhibitors may be useful for treatment of proliferative retinopathies. (PMID:15557471)
- CK2 regulates the DNA-binding ability of SSRP1 and that this regulation may be responsive to specific cell stresses. (PMID:15659405)
- Data demonstrate that CK2alpha possesses sophisticated structural adaptations in favour of dual-cosubstrate specificity. (PMID:15740749)
- constitutive phosphorylation by CK2 may be required for maximal activation of Akt/PKB (PMID:15818404)
- CK2 may have the capacity to differentially regulate U1 and U6 transcription even though SNAP(C) is universally utilized for human snRNA gene transcription (PMID:15955816)
- multiple kinases, including CK2 and GSK3beta, participate in PTEN phosphorylation and GSK3beta may provide feedback regulation of PTEN (PMID:16107342)
- Protein kinase CK2 is characterized by an extremely high stability that might be due to its association with other intracellular proteins, enhanced half-life or lower vulnerability towards proteolytic degradation. (PMID:16133877)
- protein kinase CK2 is inactive in CCVs because of the fact that it is bound to the clathrin-coated vesicle (CCV) membrane via an interaction between phosphatidylinositol 4,5-bisphosphate in the CCV membrane and the active site in CK2 (PMID:16157582)
- In vitro phosphorylation of eIF2beta also pointed to Ser2 as a preferred site for CK2 phosphorylation (PMID:16225457)
- CK2 may be involved in the regulation of cell cycle progression by associating with and phosphorylating a key molecule for translation initiation. (PMID:16227438)
- casein kinase 2 induces PACS-1 binding of nephrocystin and targeting to cilia (PMID:16308564)
- CK2 is potentially a highly plausible target for cancer therapy. (PMID:16342410)
- phosphorylation of the (T300) residue is dependent on CK2 and is a necessary and functional prerequisite for TSPY’s transport into the nucleus (PMID:16426576)
- Dynamics of nucleolar reformation is ATP/GTP-dependent, sensitive to temperature, and creatin kinase-2 driven. (PMID:16540521)
- CK2 regulates NKX3-1 in prostate cells. (PMID:16581776)
- Based on its retinal localization, CK2 may be considered a new immunohistochemical astrocytic marker, and combination of CK2 inhibitors and octreotide may be a promising future treatment for proliferative retinopathies. (PMID:16651637)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | csnk2a4 | ENSDARG00000091702 |
| mus_musculus | Csnk2a1 | ENSMUSG00000074698 |
| rattus_norvegicus | Csnk2a1 | ENSRNOG00000005276 |
| drosophila_melanogaster | CkIIalpha | FBGN0264492 |
| caenorhabditis_elegans | kin-3 | WBGENE00002191 |
Paralogs (2): CSNK2A2 (ENSG00000070770), CSNK2A3 (ENSG00000254598)
Protein
Protein identifiers
Casein kinase II subunit alpha — P68400 (reviewed: P68400)
All UniProt accessions (22): P68400, A0A087WY74, A0A2R8Y3W6, A0A2R8Y4D6, A0A2R8Y4H0, A0A2R8Y5A0, A0A2R8Y797, A0A2R8Y7T1, A0A2R8YCC9, A0A2R8YCK2, A0A2R8YD58, A0A2R8YDP2, A0A2R8YDY7, A0A2R8YEL7, A0A2R8YEW1, A0A2R8YF43, A0A2R8YF47, A0A2R8YFU2, E7EU96, V9GY80, V9GYA2, V9GYW6
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, MRE11, 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. Phosphorylates YY1, protecting YY1 from cleavage by CASP7 during apoptosis. 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, ATF4, SRF, MAX, JUN, FOS, MYC and MYB. Phosphorylates Hsp90 and its co-chaperones FKBP4 and CDC37, which is essential for chaperone function. Mediates sequential phosphorylation of FNIP1, promoting its gradual interaction with Hsp90, leading to activate both kinase and non-kinase client proteins of Hsp90. 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. Phosphorylates PML at ‘Ser-565’ and primes it for ubiquitin-mediated degradation. Plays an important role in the circadian clock function by phosphorylating BMAL1 at ‘Ser-90’ which is pivotal for its interaction with CLOCK and which controls CLOCK nuclear entry. Phosphorylates CCAR2 at ‘Thr-454’ in gastric carcinoma tissue. Phosphorylates FMR1, promoting FMR1-dependent formation of a membraneless compartment. 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 RNPS1. Interacts with SNAI1. Interacts with PML (isoform PML-12). Interacts with CCAR2. Interacts with HIRIP3.
Subcellular location. Nucleus.
Tissue specificity. Expressed in gastric carcinoma tissue and the expression gradually increases with the progression of the carcinoma (at protein level).
Post-translational modifications. Phosphorylated at Thr-344, Thr-360, Ser-362 and Ser-370 by CDK1 in prophase and metaphase and dephosphorylated during anaphase. Phosphorylation does not directly affect casein kinase 2 activity, but may contribute to its regulation by forming binding sites for interacting proteins and/or targeting it to different compartments.
Disease relevance. Okur-Chung neurodevelopmental syndrome (OCNDS) [MIM:617062] An autosomal dominant neurodevelopmental disorder characterized by developmental delay, intellectual disability, behavioral problems, hypotonia, speech problems, microcephaly, pachygyria and variable dysmorphic features. The disease is caused by variants affecting the gene represented in this entry.
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. Casein kinase 2 has been found to be increased at protein level and up-regulated at the level of enzyme activity in the majority of cancers. However, elevated levels of casein kinase 2 are present in certain normal organs such as brain and testes.
Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family. CK2 subfamily.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P68400-1 | 1 | yes |
| P68400-2 | 2 |
RefSeq proteins (5): NP_001349699, NP_001349700, NP_001886, NP_808227, NP_808228 (=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 (60 total): helix 24, strand 11, turn 6, sequence variant 4, sequence conflict 4, modified residue 4, binding site 2, chain 1, domain 1, splice variant 1, region of interest 1, active site 1
Structure
Experimental structures (PDB)
320 structures, top 30 by resolution.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 3WAR | X-RAY DIFFRACTION | 1.04 |
| 5ZN1 | X-RAY DIFFRACTION | 1.05 |
| 8AEC | X-RAY DIFFRACTION | 1.09 |
| 7I7Y | X-RAY DIFFRACTION | 1.15 |
| 6YZH | X-RAY DIFFRACTION | 1.19 |
| 5ZN2 | X-RAY DIFFRACTION | 1.2 |
| 7I8G | X-RAY DIFFRACTION | 1.23 |
| 4KWP | X-RAY DIFFRACTION | 1.25 |
| 5CVG | X-RAY DIFFRACTION | 1.25 |
| 7I8P | X-RAY DIFFRACTION | 1.25 |
| 7I8N | X-RAY DIFFRACTION | 1.28 |
| 8AE7 | X-RAY DIFFRACTION | 1.28 |
| 3NSZ | X-RAY DIFFRACTION | 1.3 |
| 7I8M | X-RAY DIFFRACTION | 1.31 |
| 7I8O | X-RAY DIFFRACTION | 1.31 |
| 7ZWG | X-RAY DIFFRACTION | 1.31 |
| 7ZYK | X-RAY DIFFRACTION | 1.31 |
| 7I86 | X-RAY DIFFRACTION | 1.32 |
| 5OUL | X-RAY DIFFRACTION | 1.34 |
| 7B8H | X-RAY DIFFRACTION | 1.34 |
| 7I7Z | X-RAY DIFFRACTION | 1.35 |
| 5CU6 | X-RAY DIFFRACTION | 1.36 |
| 5CSV | X-RAY DIFFRACTION | 1.38 |
| 7I8K | X-RAY DIFFRACTION | 1.38 |
| 5MOH | X-RAY DIFFRACTION | 1.38 |
| 5OTQ | X-RAY DIFFRACTION | 1.38 |
| 7I8D | X-RAY DIFFRACTION | 1.38 |
| 7I8H | X-RAY DIFFRACTION | 1.39 |
| 9QY7 | X-RAY DIFFRACTION | 1.39 |
| 6EHK | X-RAY DIFFRACTION | 1.4 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P68400-F1 | 90.78 | 0.87 |
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): 156 (proton acceptor)
Ligand- & substrate-binding residues (2): 45–53; 68
Post-translational modifications (4): 344, 360, 362, 370
Function
Pathways and Gene Ontology
Reactome pathways
15 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-9931529 | Phosphorylation and nuclear translocation of BMAL1 (ARNTL) and CLOCK |
| R-HSA-9931530 | Phosphorylation and nuclear translocation of the CRY:PER:kinase complex |
MSigDB gene sets: 547 (showing top):
PID_BCR_5PATHWAY, GOBP_REGULATION_OF_DOUBLE_STRAND_BREAK_REPAIR, MODULE_52, GOBP_REGULATION_OF_DNA_RECOMBINATION, GOBP_REGULATION_OF_AUTOPHAGY, GOBP_NEGATIVE_REGULATION_OF_PROTEOLYSIS, GOBP_REGULATION_OF_PROTEASOMAL_UBIQUITIN_DEPENDENT_PROTEIN_CATABOLIC_PROCESS, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, GOBP_NEGATIVE_REGULATION_OF_DNA_REPAIR, GOBP_PEPTIDYL_SERINE_MODIFICATION, MATTIOLI_MGUS_VS_PCL, GOBP_NEGATIVE_REGULATION_OF_DNA_RECOMBINATION, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, GOBP_GROWTH
GO Biological Process (35): double-strand break repair (GO:0006302), protein folding (GO:0006457), apoptotic process (GO:0006915), DNA damage response (GO:0006974), signal transduction (GO:0007165), positive regulation of cell population proliferation (GO:0008284), Wnt signaling pathway (GO:0016055), negative regulation of translation (GO:0017148), positive regulation of Wnt signaling pathway (GO:0030177), positive regulation of cell growth (GO:0030307), negative regulation of proteasomal ubiquitin-dependent protein catabolic process (GO:0032435), positive regulation of protein catabolic process (GO:0045732), rhythmic process (GO:0048511), protein stabilization (GO:0050821), regulation of cell cycle (GO:0051726), symbiont-mediated disruption of host cell PML body (GO:0075342), negative regulation of signal transduction by p53 class mediator (GO:1901797), positive regulation of aggrephagy (GO:1905337), regulation of chromosome separation (GO:1905818), negative regulation of double-strand break repair via homologous recombination (GO:2000042), negative regulation of apoptotic signaling pathway (GO:2001234), DNA damage checkpoint signaling (GO:0000077), deadenylation-dependent decapping of nuclear-transcribed mRNA (GO:0000290), double-strand break repair via homologous recombination (GO:0000724), regulation of transcription by RNA polymerase II (GO:0006357), protein phosphorylation (GO:0006468), protein catabolic process (GO:0030163), aggrephagy (GO:0035973), regulation of protein catabolic process (GO:0042176), negative regulation of translational initiation (GO:0045947), protein targeting to vacuole involved in autophagy (GO:0071211), execution phase of apoptosis (GO:0097194), double-strand break repair via classical nonhomologous end joining (GO:0097680), membraneless organelle assembly (GO:0140694), protein localization to site of double-strand break (GO:1990166)
GO Molecular Function (10): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), kinase activity (GO:0016301), identical protein binding (GO:0042802), Hsp90 protein binding (GO:0051879), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), transferase activity (GO:0016740)
GO Cellular Component (8): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytosol (GO:0005829), plasma membrane (GO:0005886), protein kinase CK2 complex (GO:0005956), PML body (GO:0016605), Sin3-type complex (GO:0070822), PcG protein complex (GO:0031519)
Reactome top-level categories
Rollup of top-14 pathways:
| Category | Pathways |
|---|---|
| Circadian clock | 2 |
| 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 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular process | 2 |
| regulation of cellular process | 2 |
| positive regulation of cellular process | 2 |
| protein kinase activity | 2 |
| cellular anatomical structure | 2 |
| DNA repair | 1 |
| protein maturation | 1 |
| programmed cell death | 1 |
| apoptotic signaling pathway | 1 |
| execution phase of apoptosis | 1 |
| cellular response to stress | 1 |
| cell communication | 1 |
| signaling | 1 |
| cellular response to stimulus | 1 |
| cell population proliferation | 1 |
| regulation of cell population proliferation | 1 |
| cell surface receptor signaling pathway | 1 |
| translation | 1 |
| regulation of translation | 1 |
| negative regulation of gene expression | 1 |
| negative regulation of protein metabolic process | 1 |
| positive regulation of signal transduction | 1 |
| Wnt signaling pathway | 1 |
| regulation of Wnt signaling pathway | 1 |
| regulation of cell growth | 1 |
| cell growth | 1 |
| positive regulation of growth | 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 |
| positive regulation of catabolic process | 1 |
| protein catabolic process | 1 |
| regulation of protein catabolic process | 1 |
| positive regulation of protein metabolic process | 1 |
| biological_process | 1 |
| regulation of protein stability | 1 |
| cell cycle | 1 |
| symbiont-mediated disruption of host cellular anatomical structure | 1 |
| signal transduction by p53 class mediator | 1 |
Protein interactions and networks
STRING
0 interactions, top by confidence (×1000):
IntAct
743 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CSNK2A1 | CSNK2B | psi-mi:“MI:0407”(direct interaction) | 0.980 |
| CSNK2A1 | CSNK2B | psi-mi:“MI:0915”(physical association) | 0.980 |
| CSNK2B | CSNK2A1 | psi-mi:“MI:2364”(proximity) | 0.980 |
| CSNK2B | CSNK2A1 | psi-mi:“MI:0915”(physical association) | 0.980 |
| HEXIM1 | CCNT1 | psi-mi:“MI:0914”(association) | 0.930 |
| CSNK2A1 | CSNK2A2 | psi-mi:“MI:0914”(association) | 0.920 |
| PCGF5 | CSNK2A2 | psi-mi:“MI:0914”(association) | 0.880 |
| POLR2E | POLR3A | psi-mi:“MI:0914”(association) | 0.870 |
| CSNK2A1 | RNF111 | psi-mi:“MI:0915”(physical association) | 0.850 |
| RNF111 | CSNK2A1 | psi-mi:“MI:0915”(physical association) | 0.850 |
| RYBP | BMI1 | psi-mi:“MI:0914”(association) | 0.850 |
| CSNK2A2 | EIF3J | psi-mi:“MI:0914”(association) | 0.790 |
| NRP1 | CSNK2A2 | psi-mi:“MI:0914”(association) | 0.790 |
| CSNK2A1 | STAC3 | psi-mi:“MI:0915”(physical association) | 0.780 |
| THAP1 | CSNK2A1 | psi-mi:“MI:0915”(physical association) | 0.780 |
| STAC3 | CSNK2A1 | psi-mi:“MI:0915”(physical association) | 0.780 |
| CSNK2A1 | THAP1 | psi-mi:“MI:0915”(physical association) | 0.780 |
| SIRT1 | CSNK2A1 | psi-mi:“MI:0915”(physical association) | 0.770 |
| CSNK2A1 | CSNK2A1 | psi-mi:“MI:0217”(phosphorylation reaction) | 0.760 |
| HEXIM2 | AHCYL1 | psi-mi:“MI:0914”(association) | 0.740 |
| VSX1 | USP12 | psi-mi:“MI:0914”(association) | 0.730 |
| CSNK2A1 | NFYA | psi-mi:“MI:0915”(physical association) | 0.670 |
BioGRID (1570): AKT1 (Biochemical Activity), SGT1 (Biochemical Activity), SUGT1 (Biochemical Activity), MAGEA11 (Two-hybrid), NFYA (Two-hybrid), RNF111 (Two-hybrid), THAP1 (Two-hybrid), STAC3 (Two-hybrid), CSNK2A1 (Affinity Capture-Western), CSNK2A1 (Affinity Capture-MS), CSNK2A1 (Affinity Capture-MS), CSNK2A1 (Affinity Capture-MS), DAXX (Biochemical Activity), NOP58 (Biochemical Activity), RNF7 (Biochemical Activity)
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
200 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| CSNK2A1 | “up-regulates activity” | CAV2 | phosphorylation |
| CSNK2A1 | up-regulates | RNF7 | phosphorylation |
| CSNK2A1 | up-regulates | WAS | phosphorylation |
| CSNK2A1 | “up-regulates activity” | LIG1 | phosphorylation |
| CSNK2A1 | “down-regulates activity” | CDC34 | phosphorylation |
| CSNK2A1 | up-regulates | HDAC1 | phosphorylation |
| CSNK2A1 | up-regulates | STX1A | phosphorylation |
| CSNK2A1 | up-regulates | VAMP4 | phosphorylation |
| CSNK2A1 | up-regulates | PKD2 | phosphorylation |
| CSNK2A1 | up-regulates | PTGES3 | phosphorylation |
| CSNK2A1 | down-regulates | CDC25C | phosphorylation |
| CSNK2A1 | up-regulates | DEK | phosphorylation |
| CSNK2A1 | up-regulates | XRCC1 | phosphorylation |
| CSNK2A1 | up-regulates | TLE1 | phosphorylation |
| CSNK2A1 | down-regulates | GRIN2B | phosphorylation |
| CSNK2A1 | “down-regulates activity” | HNRNPC | phosphorylation |
| CSNK2A1 | up-regulates | LEF1 | phosphorylation |
| CSNK2A1 | up-regulates | CDK1 | phosphorylation |
| CSNK2A1 | up-regulates | AKT1 | phosphorylation |
| CSNK2A1 | up-regulates | CAPZA1 | phosphorylation |
| CSNK2A1 | down-regulates | ARNT | phosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 171 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 | 29.2× | 6e-10 |
| PTEN Regulation | 8 | 17.7× | 2e-06 |
| Transcriptional Regulation by E2F6 | 6 | 17.1× | 1e-04 |
| Regulation of PTEN gene transcription | 9 | 15.6× | 1e-06 |
| Oncogenic MAPK signaling | 5 | 12.1× | 3e-03 |
| Transcriptional regulation by RUNX1 | 6 | 8.5× | 3e-03 |
| Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells) | 6 | 8.5× | 3e-03 |
| Signaling by BRAF and RAF1 fusions | 5 | 8.3× | 9e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| negative regulation of proteasomal ubiquitin-dependent protein catabolic process | 5 | 13.3× | 6e-03 |
| mRNA splicing, via spliceosome | 9 | 5.5× | 6e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
281 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 35 |
| Likely pathogenic | 35 |
| Uncertain significance | 91 |
| Likely benign | 50 |
| Benign | 24 |
Top pathogenic / likely-pathogenic (30)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1033456 | NM_177559.3(CSNK2A1):c.376del (p.Gln126fs) | Pathogenic |
| 1329650 | NM_177559.3(CSNK2A1):c.838C>T (p.Arg280Ter) | Pathogenic |
| 1675245 | NM_177559.3(CSNK2A1):c.142G>A (p.Gly48Ser) | Pathogenic |
| 1690320 | NM_177559.3(CSNK2A1):c.832C>T (p.Arg278Ter) | Pathogenic |
| 1709571 | NM_177559.3(CSNK2A1):c.127C>T (p.Arg43Ter) | Pathogenic |
| 1801973 | NM_177559.3(CSNK2A1):c.61C>T (p.Arg21Ter) | Pathogenic |
| 224797 | NM_177559.3(CSNK2A1):c.824+2T>C | Pathogenic |
| 224799 | NM_177559.3(CSNK2A1):c.524A>G (p.Asp175Gly) | Pathogenic |
| 224800 | NM_177559.3(CSNK2A1):c.149A>C (p.Tyr50Ser) | Pathogenic |
| 2442654 | NM_177559.3(CSNK2A1):c.102-2A>G | Pathogenic |
| 2503390 | NM_177559.3(CSNK2A1):c.213+1G>T | Pathogenic |
| 2504560 | NM_177559.3(CSNK2A1):c.523G>A (p.Asp175Asn) | Pathogenic |
| 2663860 | NM_177559.3(CSNK2A1):c.572G>A (p.Arg191Gln) | Pathogenic |
| 280816 | NM_177559.3(CSNK2A1):c.139C>G (p.Arg47Gly) | Pathogenic |
| 3340574 | NM_177559.3(CSNK2A1):c.151A>C (p.Ser51Arg) | Pathogenic |
| 3370910 | NM_177559.3(CSNK2A1):c.920_921dup (p.Asp308fs) | Pathogenic |
| 3385354 | NM_177559.3(CSNK2A1):c.224dup (p.Lys76fs) | Pathogenic |
| 3391482 | NM_177559.3(CSNK2A1):c.524A>C (p.Asp175Ala) | Pathogenic |
| 3774820 | NM_177559.3(CSNK2A1):c.467A>G (p.Asp156Gly) | Pathogenic |
| 3777315 | NM_177559.3(CSNK2A1):c.214-1G>A | Pathogenic |
| 3899537 | NM_177559.3(CSNK2A1):c.589T>G (p.Phe197Val) | Pathogenic |
| 392940 | NM_177559.3(CSNK2A1):c.426+1G>T | Pathogenic |
| 4082413 | NM_177559.3(CSNK2A1):c.581C>T (p.Ser194Phe) | Pathogenic |
| 421395 | NM_177559.3(CSNK2A1):c.468T>A (p.Asp156Glu) | Pathogenic |
| 4282412 | NM_177559.3(CSNK2A1):c.152G>T (p.Ser51Ile) | Pathogenic |
| 4531756 | NM_177559.3(CSNK2A1):c.538G>A (p.Glu180Lys) | Pathogenic |
| 4819102 | NM_177559.3(CSNK2A1):c.829_847del (p.Ser277fs) | Pathogenic |
| 4819106 | NM_177559.3(CSNK2A1):c.254del (p.Leu85fs) | Pathogenic |
| 4849518 | NM_177559.3(CSNK2A1):c.546T>G (p.Tyr182Ter) | Pathogenic |
| 521073 | NM_177559.3(CSNK2A1):c.783C>A (p.Tyr261Ter) | Pathogenic |
SpliceAI
2222 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 20:486371:CTGA:C | donor_loss | 1.0000 |
| 20:486372:TGA:T | donor_loss | 1.0000 |
| 20:486374:A:C | donor_loss | 1.0000 |
| 20:486459:GTGT:G | acceptor_gain | 1.0000 |
| 20:486463:C:CC | acceptor_gain | 1.0000 |
| 20:487421:ACTCA:A | donor_loss | 1.0000 |
| 20:487423:TCAC:T | donor_loss | 1.0000 |
| 20:487424:CACAG:C | donor_loss | 1.0000 |
| 20:487425:A:AC | donor_gain | 1.0000 |
| 20:487425:ACAG:A | donor_loss | 1.0000 |
| 20:487426:C:CA | donor_gain | 1.0000 |
| 20:487426:CAGAA:C | donor_gain | 1.0000 |
| 20:487442:C:CA | donor_gain | 1.0000 |
| 20:487447:G:A | donor_gain | 1.0000 |
| 20:487573:TGT:T | acceptor_gain | 1.0000 |
| 20:487573:TGTC:T | acceptor_loss | 1.0000 |
| 20:487574:GT:G | acceptor_gain | 1.0000 |
| 20:487574:GTC:G | acceptor_loss | 1.0000 |
| 20:487575:TC:T | acceptor_loss | 1.0000 |
| 20:487576:C:CC | acceptor_gain | 1.0000 |
| 20:487577:T:G | acceptor_loss | 1.0000 |
| 20:488671:GACTT:G | donor_loss | 1.0000 |
| 20:488672:ACTT:A | donor_loss | 1.0000 |
| 20:488673:CTT:C | donor_loss | 1.0000 |
| 20:488674:TTA:T | donor_loss | 1.0000 |
| 20:488675:T:TG | donor_loss | 1.0000 |
| 20:488676:A:AC | donor_gain | 1.0000 |
| 20:488676:ACCT:A | donor_loss | 1.0000 |
| 20:488677:C:CC | donor_gain | 1.0000 |
| 20:488677:CCTG:C | donor_gain | 1.0000 |
AlphaMissense
0 scored. Top likely-pathogenic:
dbSNP variants (sampled 300 via entrez): RS1000058052 (20:481617 T>C), RS1000083409 (20:519087 C>T), RS1000135942 (20:540815 T>C), RS1000147092 (20:474791 T>G), RS1000215208 (20:531689 T>C), RS1000226196 (20:494156 T>C), RS1000270290 (20:541178 G>A,C), RS1000356280 (20:512365 A>C), RS1000420069 (20:478184 T>C), RS1000469273 (20:542112 G>A), RS1000473767 (20:543571 C>T), RS1000478280 (20:506476 G>C), RS1000545073 (20:503050 C>A,T), RS1000549050 (20:496338 G>A), RS1000557067 (20:495916 T>C,G)
Disease associations
OMIM: gene MIM:115440 | disease phenotypes: MIM:617062, MIM:615895
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| Okur-Chung neurodevelopmental syndrome | Definitive | Autosomal dominant |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| syndromic intellectual disability | Definitive | AD |
Mondo (6): Okur-Chung neurodevelopmental syndrome (MONDO:0014893), intellectual disability (MONDO:0001071), neurodevelopmental disorder (MONDO:0700092), epilepsy (MONDO:0005027), polyglucosan body myopathy 1 with or without immunodeficiency (MONDO:0014389), autism spectrum disorder (MONDO:0005258)
Orphanet (5): Okur-Chung neurodevelopmental syndrome (Orphanet:689422), Autoinflammatory syndrome with pyogenic bacterial infection and amylopectinosis (Orphanet:329173), Polyglucosan body myopathy type 1 (Orphanet:397937), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658), NON RARE IN EUROPE: Autism (Orphanet:106)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
5 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST003542_11 | Night sleep phenotypes | 8.000000e-08 |
| GCST003542_24 | Night sleep phenotypes | 4.000000e-07 |
| GCST005024_26 | Pursuit maintenance gain | 8.000000e-06 |
| GCST012490_24 | Femur bone mineral density x serum urate levels interaction | 1.000000e-12 |
| GCST012490_353 | Femur bone mineral density x serum urate levels interaction | 4.000000e-13 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0008433 | pursuit maintenance gain measurement |
| EFO:0004531 | urate measurement |
MeSH disease descriptors (3)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D004827 | Epilepsy | C10.228.140.490 |
| D008607 | Intellectual Disability | C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539 |
| D065886 | Neurodevelopmental Disorders | F03.625 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (4): CHEMBL2095191 (PROTEIN COMPLEX GROUP), CHEMBL3038477 (PROTEIN COMPLEX), CHEMBL3629 (SINGLE PROTEIN), CHEMBL3832943 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
36 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 421,627 (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 |
|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL1789941 | RUXOLITINIB | 4 | 11,547 |
| CHEMBL189963 | PALBOCICLIB | 4 | 13,102 |
| CHEMBL2005186 | BELUMOSUDIL | 4 | 1,817 |
| CHEMBL3301610 | ABEMACICLIB | 4 | 7,045 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL608533 | MIDOSTAURIN | 4 | 7,259 |
| CHEMBL58 | MITOXANTRONE | 4 | 166,878 |
| CHEMBL50 | QUERCETIN | 3 | 74,559 |
| CHEMBL223360 | LINIFANIB | 3 | 3,925 |
| CHEMBL483158 | ALISERTIB | 3 | 2,305 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL91829 | RUBOXISTAURIN | 3 | 77 |
| CHEMBL3265032 | ENTOSPLETINIB | 3 | 1,628 |
| CHEMBL1230165 | SILMITASERTIB | 2 | 593 |
| CHEMBL31574 | FISETIN | 2 | 7,745 |
| CHEMBL6246 | ELLAGIC ACID | 2 | 23,148 |
| CHEMBL105442 | CI-1040 | 2 | 3,936 |
| CHEMBL1232461 | MOLIBRESIB | 2 | |
| CHEMBL1721885 | SU-014813 | 2 | |
| CHEMBL1738758 | ONVANSERTIB | 2 | |
| CHEMBL230011 | TG100-115 | 2 | |
| CHEMBL475251 | R-406 | 2 | |
| CHEMBL572878 | TOZASERTIB | 2 | |
| CHEMBL151 | LUTEOLIN | 2 | |
| CHEMBL8260 | BAICALEIN | 2 | |
| CHEMBL83628 | CHROMOCARB | 2 | |
| CHEMBL1084546 | PF-00562271 | 1 |
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 (4 total), top 4:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| silmitasertib | Inhibition | 9.0 | pIC50 |
| compound 1a [PMID: 24900749] | Inhibition | 8.0 | pIC50 |
| KDX1381 | Binding | 7.27 | pKd |
| compound 2c [PMID: 22115617] | Inhibition | 7.08 | pKi |
Binding affinities (BindingDB)
344 measured of 1578 human assays (1583 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 |
| 5-(4-chlorophenyl)benzo[c]2,6-naphthyridine-8-carboxylic acid (Compound 12) | IC50 | 0.5 nM | |
| 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 |
| CX-5279 | IC50 | 0.91 nM | |
| 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 |
| CX-4945 | IC50 | 1.5 nM | |
| 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 |
ChEMBL bioactivities
2359 potent at pChembl≥5 of 2534 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.89 | Kd | 0.01288 | nM | CHEMBL4089961 |
| 10.80 | Kd | 0.016 | nM | CHEMBL4089961 |
| 10.50 | Kd | 0.03162 | nM | CHEMBL4077554 |
| 10.43 | Kd | 0.037 | nM | CHEMBL4077554 |
| 10.32 | Kd | 0.0482 | nM | CHEMBL3103191 |
| 10.08 | Ki | 0.084 | nM | CHEMBL5419810 |
| 10.03 | Kd | 0.094 | nM | CHEMBL4099729 |
| 10.03 | Kd | 0.09333 | nM | CHEMBL4099729 |
| 9.89 | IC50 | 0.13 | nM | CHEMBL3699289 |
| 9.85 | IC50 | 0.14 | nM | CHEMBL3699277 |
| 9.82 | IC50 | 0.15 | nM | CHEMBL3699234 |
| 9.80 | IC50 | 0.16 | nM | CHEMBL3699295 |
| 9.79 | Kd | 0.1622 | nM | CHEMBL4075338 |
| 9.77 | IC50 | 0.17 | nM | CHEMBL3699235 |
| 9.77 | Kd | 0.17 | nM | CHEMBL4075338 |
| 9.68 | IC50 | 0.21 | nM | CHEMBL3699253 |
| 9.68 | IC50 | 0.21 | nM | CHEMBL3699266 |
| 9.66 | IC50 | 0.22 | nM | CHEMBL3699292 |
| 9.66 | IC50 | 0.22 | nM | CHEMBL3699244 |
| 9.64 | IC50 | 0.23 | nM | CHEMBL3699294 |
| 9.64 | IC50 | 0.23 | nM | CHEMBL3699237 |
| 9.64 | IC50 | 0.23 | nM | CHEMBL4848224 |
| 9.62 | IC50 | 0.24 | nM | CHEMBL3699252 |
| 9.59 | Ki | 0.26 | nM | CHEMBL398149 |
| 9.57 | IC50 | 0.27 | nM | CHEMBL3699291 |
| 9.57 | IC50 | 0.27 | nM | CHEMBL3699254 |
| 9.57 | IC50 | 0.27 | nM | CHEMBL3699276 |
| 9.55 | IC50 | 0.28 | nM | CHEMBL3699280 |
| 9.54 | IC50 | 0.29 | nM | CHEMBL3699238 |
| 9.54 | IC50 | 0.29 | nM | CHEMBL3699278 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL3699255 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL3699250 |
| 9.52 | IC50 | 0.3 | nM | CHEMBL3699239 |
| 9.51 | IC50 | 0.31 | nM | CHEMBL3699262 |
| 9.47 | Kd | 0.34 | nM | CHEMBL4162173 |
| 9.46 | Ki | 0.35 | nM | CHEMBL230354 |
| 9.42 | Ki | 0.38 | nM | SILMITASERTIB |
| 9.42 | Kd | 0.38 | nM | SILMITASERTIB |
| 9.41 | IC50 | 0.39 | nM | CHEMBL3699287 |
| 9.40 | Kd | 0.4 | nM | CHEMBL4075701 |
| 9.40 | Kd | 0.4 | nM | CHEMBL4169451 |
| 9.39 | IC50 | 0.41 | nM | CHEMBL3699256 |
| 9.38 | Kd | 0.42 | nM | CHEMBL4069112 |
| 9.38 | Kd | 0.4169 | nM | CHEMBL4069112 |
| 9.38 | Ki | 0.42 | nM | CHEMBL4846181 |
| 9.38 | Ki | 0.42 | nM | CHEMBL1682283 |
| 9.34 | IC50 | 0.46 | nM | CHEMBL4862003 |
| 9.30 | Kd | 0.5 | nM | CHEMBL4061407 |
| 9.30 | IC50 | 0.5 | nM | SILMITASERTIB |
| 9.28 | IC50 | 0.52 | nM | CHEMBL3699282 |
PubChem BioAssay actives
1178 with measured affinity, of 4321 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 |
|---|---|---|---|---|
| 2-[(E,3E)-3-[2-[4-[[(5S)-5-carboxy-5-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[9-(8-carboxybenzo[c][2,6]naphthyridin-5-yl)oxynonanoylamino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]pentyl]amino]-4-oxobutyl]-1-ethyl-2-methyl-6-sulfoindol-3-ylidene]prop-1-enyl]-1-ethyl-3,3-dimethylindol-1-ium-5-sulfonate | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | <0.0001 | uM |
| 5-[9-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(1S)-5-amino-1-carboxypentyl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-9-oxononoxy]benzo[c][2,6]naphthyridine-8-carboxylic acid | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | <0.0001 | uM |
| N-[2-[2-aminoethyl(methyl)amino]-5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]acetamide | 1301603: Binding affinity to His-tagged recombinant human CK2alpha (6 to 335 residues) after 50 to 116.7 mins by surface plasmon resonance assay | kd | <0.0001 | uM |
| N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-methylphenyl]acetamide | 1301603: Binding affinity to His-tagged recombinant human CK2alpha (6 to 335 residues) after 50 to 116.7 mins by surface plasmon resonance assay | kd | <0.0001 | uM |
| N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-[2-(dimethylamino)ethyl-methylamino]phenyl]acetamide | 1301603: Binding affinity to His-tagged recombinant human CK2alpha (6 to 335 residues) after 50 to 116.7 mins by surface plasmon resonance assay | kd | <0.0001 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[9-(8-carboxybenzo[c][2,6]naphthyridin-5-yl)oxynonanoylamino]hexanoyl]amino]-3-carboxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-carboxypropanoyl]amino]butanedioic acid | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0001 | uM |
| (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 |
| (2S)-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[9-[(8-carboxybenzo[c][2,6]naphthyridin-5-yl)amino]nonanoylamino]propanoyl]amino]propanoyl]amino]butanedioic acid | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0002 | 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 |
| 4-[2-[[4-[[6-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(1R)-5-amino-1-carboxypentyl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-6-oxohexyl]amino]-4-oxobutanoyl]amino]-1,3-selenazol-5-yl]benzoic acid | 1362772: Displacement of ARC-1504/ARC-1513-5O from CK2alpha (unknown origin) (1 to 335 residues) after 15 to 60 mins by luminescence assay | kd | 0.0003 | uM |
| N-[3-[(4-anilino-8-cyanopyrazolo[1,5-a][1,3,5]triazin-2-yl)amino]phenyl]acetamide | 291056: Inhibition of human CK2 alpha | ki | 0.0003 | uM |
| N-[3-[[8-cyano-4-(cyclopropylamino)pyrazolo[1,5-a][1,3,5]triazin-2-yl]amino]phenyl]acetamide | 291056: Inhibition of human CK2 alpha | ki | 0.0003 | uM |
| (2S)-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[9-(8-carboxybenzo[c][2,6]naphthyridin-5-yl)oxynonanoylamino]propanoyl]amino]propanoyl]amino]butanedioic acid | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0004 | uM |
| 2-[(1E,3E,5E)-5-[2-[4-[[(5S)-5-carboxy-5-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[8-(4,5,6,7-tetrabromobenzimidazol-1-yl)octanoylamino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]pentyl]amino]-4-oxobutyl]-1-ethyl-2-methyl-6-sulfoindol-3-ylidene]penta-1,3-dienyl]-1-ethyl-3,3-dimethylindol-1-ium-5-sulfonate | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0004 | uM |
| 5-[[(5R)-5-carboxy-5-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[6-[[4-[[5-(4-carboxyphenyl)-1,3-thiazol-2-yl]amino]-4-oxobutanoyl]amino]hexanoylamino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]pentyl]carbamoyl]-2-[3-(dimethylamino)-6-dimethylazaniumylidenexanthen-9-yl]benzoate | 1362772: Displacement of ARC-1504/ARC-1513-5O from CK2alpha (unknown origin) (1 to 335 residues) after 15 to 60 mins by luminescence assay | kd | 0.0004 | uM |
| 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid | 1294144: Inhibition of recombinant human CK2 holoenzyme using RRRDDDSDDD as substrate measured after 20 mins at 30 degC by radiometric kinase assay in presence of [gamma-32P]ATP | ki | 0.0004 | uM |
| 5-(3-cyanoanilino)pyrimido[4,5-c]quinoline-8-carboxylic acid | 1750468: Inhibition of CK2 (unknown origin) | ki | 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 |
| (2S)-6-amino-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[8-(4,5,6,7-tetrabromobenzimidazol-1-yl)octanoylamino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]hexanoic acid | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0005 | uM |
| 2-[(1E,3E,5E)-5-[2-[4-[[(5S)-5-[9-(8-carboxybenzo[c][2,6]naphthyridin-5-yl)oxynonanoylamino]-6-[[(2S)-3-carboxy-1-[[(2S)-3-carboxy-1-[[(2S)-3-carboxy-1-[[(1S)-1,2-dicarboxyethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-oxohexyl]amino]-4-oxobutyl]-1-ethyl-2-methyl-6-sulfoindol-3-ylidene]penta-1,3-dienyl]-1-ethyl-3,3-dimethylindol-1-ium-5-sulfonate | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0005 | uM |
| 5-(4-chlorophenyl)benzo[c][2,6]naphthyridine-8-carboxylic acid | 1801077: Molecular Docking from Article 10.1111/cbdd.12372: “Structural basis for low-affinity binding of non-R2 carboxylate-substituted tricyclic quinoline analogs to CK2a: comparative molecular dynamics simulation studies.” | 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 |
| 4-[2-[[4-[[6-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(1R)-5-amino-1-carboxypentyl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-6-oxohexyl]amino]-4-oxobutanoyl]amino]-1,3-thiazol-5-yl]benzoic acid | 1362772: Displacement of ARC-1504/ARC-1513-5O from CK2alpha (unknown origin) (1 to 335 residues) after 15 to 60 mins by luminescence assay | kd | 0.0006 | 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 |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[9-(8-carboxy-5-oxobenzo[c][2,6]naphthyridin-6-yl)nonanoylamino]hexanoyl]amino]-3-carboxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-carboxypropanoyl]amino]butanedioic acid | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0007 | 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-[[(5R)-5-carboxy-5-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[[(2R)-3-carboxy-2-[6-[[4-[[5-(4-carboxyphenyl)-1,3-selenazol-2-yl]amino]-4-oxobutanoyl]amino]hexanoylamino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]pentyl]carbamoyl]-2-[3-(dimethylamino)-6-dimethylazaniumylidenexanthen-9-yl]benzoate | 1362772: Displacement of ARC-1504/ARC-1513-5O from CK2alpha (unknown origin) (1 to 335 residues) after 15 to 60 mins by luminescence assay | kd | 0.0008 | 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 |
| 3-(cyclopropylamino)-5-[3-(trifluoromethyl)anilino]pyrimido[4,5-c]quinoline-8-carboxylate | 1799832: Phosphorylation Assay from Article 10.1021/bi2008382: “Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.” | 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-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylate | 1799832: Phosphorylation Assay from Article 10.1021/bi2008382: “Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.” | ic50 | 0.0015 | uM |
| (2S)-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[7-(8-carboxybenzo[c][2,6]naphthyridin-5-yl)oxyheptanoylamino]propanoyl]amino]propanoyl]amino]butanedioic acid | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0016 | 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 |
| 5-[4-[2-aminoethyl(ethyl)amino]-3-(1,2,4-triazol-4-yl)anilino]-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile | 2066662: Inhibition of CSNK2A1 (unknown origin) in presence of ATP by Eurofins radiometric enzymatic 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-[3-[[8-cyano-4-(cyclobutylamino)pyrazolo[1,5-a][1,3,5]triazin-2-yl]amino]phenyl]acetamide | 291056: Inhibition of human CK2 alpha | ki | 0.0019 | uM |
| N-(3-ethynylphenyl)-6-(1H-1,2,4-triazol-5-yl)thieno[3,2-c]quinolin-4-amine | 657060: Inhibition of human recombinant CK2 (alphaalpha-betabeta) holoenzyme using RRRDDDSDDD as substrate and 15 uM ATP by radiometric assay | ic50 | 0.0020 | uM |
| 5-(3-ethynylanilino)pyrimido[4,5-c]quinoline-8-carboxylate | 1799832: Phosphorylation Assay from Article 10.1021/bi2008382: “Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.” | ic50 | 0.0021 | uM |
| (2S)-2-[[(2S)-3-carboxy-2-[[(2S)-3-carboxy-2-[9-(8-carboxy-5-oxobenzo[c][2,6]naphthyridin-6-yl)nonanoylamino]propanoyl]amino]propanoyl]amino]butanedioic acid | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0024 | uM |
| 2-[(1E,3E,5E)-5-[2-[4-[[(5S)-6-[[(2S)-3-carboxy-1-[[(2S)-3-carboxy-1-[[(2S)-3-carboxy-1-[[(1S)-1,2-dicarboxyethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-[9-(8-carboxy-5-oxobenzo[c][2,6]naphthyridin-6-yl)nonanoylamino]-6-oxohexyl]amino]-4-oxobutyl]-1-ethyl-2-methyl-6-sulfoindol-3-ylidene]penta-1,3-dienyl]-1-ethyl-3,3-dimethylindol-1-ium-5-sulfonate | 1481164: Inhibition of ARC-1504 binding to CK2alpha (unknown origin) (1 to 335 residues) measured after 15 mins by fluorescence anisotropic method | kd | 0.0024 | 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 |
| N-[2-[(3S)-3-aminopiperidin-1-yl]-5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]acetamide | 1301597: Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay | ic50 | 0.0030 | uM |
| N-[2-[[(2R)-2-aminopropyl]-methylamino]-5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]acetamide | 1301597: Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay | ic50 | 0.0030 | uM |
| N-[2-[[(2S)-2-aminopropyl]-methylamino]-5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]acetamide | 1301597: Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay | ic50 | 0.0030 | uM |
| N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-[methyl(2-morpholin-4-ylethyl)amino]phenyl]acetamide | 1301597: Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay | ic50 | 0.0030 | uM |
| N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-(3-hydroxypropylamino)phenyl]acetamide | 1301597: Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay | ic50 | 0.0030 | uM |
| N-[2-[2-aminoethyl(ethyl)amino]-5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]phenyl]acetamide | 1301597: Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay | ic50 | 0.0030 | uM |
CTD chemical–gene interactions
81 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects expression, decreases methylation, increases expression, affects cotreatment, decreases expression | 5 |
| Cyclosporine | increases expression | 3 |
| Cadmium Chloride | increases expression, decreases expression | 3 |
| bisphenol A | affects expression, increases expression | 2 |
| sodium arsenite | increases expression | 2 |
| silmitasertib | affects phosphorylation, affects reaction, affects binding, decreases reaction, decreases activity | 2 |
| Air Pollutants | affects cotreatment, increases abundance, increases oxidation, affects expression | 2 |
| Formaldehyde | affects localization, affects phosphorylation, decreases expression, affects reaction | 2 |
| Ozone | affects expression, affects cotreatment, increases oxidation, increases abundance | 2 |
| Quercetin | affects binding, decreases activity | 2 |
| Rotenone | increases cleavage, increases expression, increases lipidation, affects reaction, decreases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| multi-kinase inhibitor 108600 | affects folding, affects binding, decreases reaction, decreases activity | 1 |
| geldanamycin | increases expression | 1 |
| bufotalin | increases expression | 1 |
| alternariol | decreases activity | 1 |
| triphenyl phosphate | affects expression | 1 |
| alpha-pinene | affects cotreatment, increases oxidation, increases abundance | 1 |
| pyrithione | affects binding, affects cotreatment, decreases reaction, increases reaction | 1 |
| salinomycin | decreases expression | 1 |
| decabromobiphenyl ether | decreases expression | 1 |
| quercitrin | affects expression | 1 |
| beta-lapachone | increases expression | 1 |
| arsenite | affects expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | increases expression | 1 |
| tetrabromobisphenol A | decreases expression | 1 |
| 3,4,5,3’,4’-pentachlorobiphenyl | affects expression | 1 |
| ochratoxin A | decreases expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| 2,2’,3’,4,4’,5-hexachlorobiphenyl | affects expression | 1 |
ChEMBL screening assays
1085 unique, capped per target: 937 binding, 146 functional, 2 admet
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 |
| CHEMBL4407590 | ADMET | Inhibition of recombinant human full-length His-tagged CSNK2A1 expressed in baculovirus expression system at 25 uM using FRET-labeled Ser/Thr 11 peptide as substrate measured after 1 hr by Z’-lyte assay relative to control | Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase. — J Med Chem |
Cellosaurus cell lines
476 cell lines: 476 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_0006 | THP-1 | Cancer cell line | Male |
| CVCL_0R21 | THP-1/DC-SIGN | Cancer cell line | Male |
| CVCL_0R25 | THP-1(NCI) | Cancer cell line | Male |
| CVCL_0R26 | THP-1(NCI)/DC-SIGN | Cancer cell line | Male |
| CVCL_3426 | THP-1h | Cancer cell line | Male |
| CVCL_3427 | THP-1l | Cancer cell line | Male |
| CVCL_4V22 | THP-1/ara-C | Cancer cell line | Male |
| CVCL_5115 | A-THP-1 | Cancer cell line | Male |
| CVCL_5I76 | THP1-defCASP1 | Cancer cell line | Male |
| CVCL_5I77 | THP1-NLRC4 | Cancer cell line | Male |
Clinical trials (associated diseases)
298 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT05657860 | PHASE4 | COMPLETED | Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome |
| NCT05744479 | PHASE4 | RECRUITING | Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability |
| NCT06107829 | PHASE4 | WITHDRAWN | Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities |
| NCT06997198 | PHASE4 | NOT_YET_RECRUITING | Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities |
| NCT04586348 | PHASE4 | UNKNOWN | Prenatal Iodine Supplementation and Early Childhood Neurodevelopment |
| NCT04873115 | PHASE4 | UNKNOWN | Double-blind, Placebo-controlled, Randomized Clinical Trial Comparing the Efficacy and Safety of Sialanar Plus orAl rehabiLitation Against Placebo Plus Oral Rehabilitation for chIldren and Adolescents With seVere Sialorrhoea and Neurodisabilties, |
| NCT02270736 | PHASE3 | COMPLETED | Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability |
| NCT02559102 | PHASE3 | COMPLETED | Dexmedetomidine Sedation Versus General Anaesthesia for Inguinal Hernia Surgery in Infants |
| NCT02757079 | PHASE3 | COMPLETED | Study of the Efficacy and Safety of NPC-15 for Sleep Disorders of Children With Neurodevelopmental Disorders |
| NCT06915480 | PHASE3 | RECRUITING | Reducing Missed Appointments |
| NCT07377032 | PHASE3 | RECRUITING | TAP-GRIN: Interventional Study on Patients With GRIN-related Neurodevelopmental Disorders |
| NCT02304302 | PHASE2 | COMPLETED | Down Syndrome Memantine Follow-up Study |
| NCT03862950 | PHASE2 | COMPLETED | A Trial of Metformin in Individuals With Fragile X Syndrome (Met) |
| NCT04529226 | PHASE2 | UNKNOWN | Study to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis |
| NCT04821856 | PHASE2 | COMPLETED | Evaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability |
| NCT02909959 | PHASE2 | COMPLETED | Sulforaphane for the Treatment of Young Men With Autism Spectrum Disorder |
| NCT06081348 | PHASE2 | RECRUITING | Sertraline vs. Placebo in the Treatment of Anxiety in Children and AdoLescents With NeurodevelopMental Disorders |
| NCT06352372 | PHASE2 | COMPLETED | Safety and Efficacy of tPBM for Epileptiform Activity in Autism |
| NCT05273320 | PHASE1 | COMPLETED | Clinical Trial of Nabilone for Aggression in Adults With Intellectual and Developmental Disabilities |
| NCT05301361 | PHASE1 | ENROLLING_BY_INVITATION | Sensitivity of the NIH Toolbox to Stimulant Treatment in Intellectual Disabilities |
| NCT06016764 | PHASE1 | COMPLETED | Use of MRI and cTBS for Catatonia in Autism |
| NCT06586827 | PHASE1 | COMPLETED | Impact of Competency-Based Training and Technical Assistance Employment Outcomes of Individuals With ID/DD |
| NCT07531940 | PHASE1 | NOT_YET_RECRUITING | Escalating Doses of Memantine in Down Syndrome (MEDS-123) |
| NCT00503191 | PHASE1 | COMPLETED | NeuroModulation Technique Treatment of Autism |
| NCT04475848 | PHASE1 | COMPLETED | A Study to Investigate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Food Effect of RO6953958 in Healthy Participants |
| NCT06300398 | PHASE1 | COMPLETED | IAMA-6 Oral Dose Study in Healthy Adults |
| NCT03479476 | PHASE2/PHASE3 | COMPLETED | A Trial of Metformin in Individuals With Fragile X Syndrome |
| NCT02616796 | PHASE1/PHASE2 | COMPLETED | Effects of Social Gaze Training on Brain and Behavior in Fragile X Syndrome |
| NCT06860672 | EARLY_PHASE1 | RECRUITING | Clinical Trial of the Dual Vector Base Editor for the Treatment of the CHD3-R1025W Mutation |
| NCT00597948 | Not specified | COMPLETED | Healthy Lifestyles for People With Intellectual Disabilities |
| NCT01087320 | Not specified | RECRUITING | Genome Medical Sequencing for Gene Discovery |
| NCT01652963 | Not specified | UNKNOWN | Picture-based Computerised Assessment and Training of Cognitive Behaviour Therapy Skills |
| NCT01695395 | Not specified | COMPLETED | Mental Health Care Provision for Adults With Intellectual Disability and a Mental Disorder |
| NCT01867554 | Not specified | COMPLETED | Research and Characterization of New Genes Involved in Intellectual Disability |
| NCT01915381 | Not specified | COMPLETED | Improving Adherence Healthy Lifestyle With a Smartphone Application Based on Adults With Intellectual Disabilities |
| NCT01988623 | Not specified | COMPLETED | Pivotal Response Treatment for Individuals With Intellectual Disabilities |
| NCT02099773 | Not specified | COMPLETED | Support Staff-client Interactions With Augmentative and Alternative Communication |
| NCT02136849 | Not specified | COMPLETED | Inter-regional Project of the Great Western Exploration Approach for Exome Molecular Causes Severe Intellectual Disability Isolated or Syndromic |
| NCT02225041 | Not specified | COMPLETED | Sedation Strategy and Cognitive Outcome After Critical Illness in Early Childhood |
| NCT02414438 | Not specified | COMPLETED | Establishing the Clinical Utility of First StepDx PLUS and NextStepDx PLUS Study |
Related Atlas pages
- Associated diseases: Okur-Chung neurodevelopmental syndrome, syndromic intellectual disability
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): Okur-Chung neurodevelopmental syndrome, polyglucosan body myopathy 1 with or without immunodeficiency