CSNK1G3
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Summary
CSNK1G3 (casein kinase 1 gamma 3, HGNC:2456) is a protein-coding gene on chromosome 5q23.2, encoding Casein kinase I isoform gamma-3 (Q9Y6M4). Serine/threonine-protein kinase.
This gene encodes a member of a family of serine/threonine protein kinases that phosphorylate caseins and other acidic proteins. A related protein in the African clawed frog participates in the transmission of Wnt/beta-catenin signaling. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene.
Source: NCBI Gene 1456 — RefSeq curated summary.
At a glance
- Gene–disease (curated): Tourette syndrome (Limited, GenCC)
- GWAS associations: 26
- Clinical variants (ClinVar): 56 total — 1 pathogenic
- Druggable target: yes — 16 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_001364140
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:2456 |
| Approved symbol | CSNK1G3 |
| Name | casein kinase 1 gamma 3 |
| Location | 5q23.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000151292 |
| Ensembl biotype | protein_coding |
| OMIM | 604253 |
| Entrez | 1456 |
Gene structure
Transcript identifiers
Ensembl transcripts: 51 — 49 protein_coding, 1 protein_coding_CDS_not_defined, 1 retained_intron
ENST00000345990, ENST00000360683, ENST00000361991, ENST00000508708, ENST00000510842, ENST00000511130, ENST00000512718, ENST00000514131, ENST00000515322, ENST00000521364, ENST00000696905, ENST00000895947, ENST00000895948, ENST00000895949, ENST00000895950, ENST00000895951, ENST00000895952, ENST00000895953, ENST00000895954, ENST00000895955, ENST00000895956, ENST00000895957, ENST00000895958, ENST00000895959, ENST00000895960, ENST00000895961, ENST00000895962, ENST00000895963, ENST00000895964, ENST00000895965, ENST00000895966, ENST00000895967, ENST00000895968, ENST00000895969, ENST00000895970, ENST00000895971, ENST00000895972, ENST00000895973, ENST00000895974, ENST00000895975, ENST00000926407, ENST00000926408, ENST00000926409, ENST00000962235, ENST00000962236, ENST00000962237, ENST00000962238, ENST00000962239, ENST00000962240, ENST00000962241, ENST00000962242
RefSeq mRNA: 16 — MANE Select: NM_001364140
NM_001031812, NM_001044723, NM_001270572, NM_001270573, NM_001270574, NM_001364140, NM_001364141, NM_001364143, NM_001364144, NM_001364145, NM_001364146, NM_001364147, NM_001364148, NM_001364149, NM_001364150, NM_004384
CCDS: CCDS34218, CCDS4135, CCDS43355, CCDS59491, CCDS59492, CCDS59493, CCDS93772
Canonical transcript exons
ENST00000696905 — 14 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000998768 | 123604724 | 123604830 |
| ENSE00000998775 | 123588427 | 123588511 |
| ENSE00000998778 | 123575729 | 123575963 |
| ENSE00001082724 | 123590410 | 123590558 |
| ENSE00001120965 | 123591319 | 123591414 |
| ENSE00001331321 | 123605339 | 123605362 |
| ENSE00001521677 | 123545417 | 123545841 |
| ENSE00001521680 | 123512177 | 123512570 |
| ENSE00001736478 | 123588068 | 123588153 |
| ENSE00003597406 | 123573393 | 123573541 |
| ENSE00003663267 | 123557495 | 123557564 |
| ENSE00003692293 | 123553107 | 123553147 |
| ENSE00003967641 | 123595039 | 123595134 |
| ENSE00003968849 | 123614342 | 123617049 |
Expression profiles
Bgee: expression breadth ubiquitous, 280 present calls, max score 95.71.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 33.2405 / max 234.2416, expressed in 1816 samples.
FANTOM5 promoters (8 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 58234 | 20.9142 | 1797 |
| 58233 | 6.2264 | 1670 |
| 58232 | 1.7460 | 1042 |
| 58231 | 1.6483 | 944 |
| 58237 | 1.2289 | 689 |
| 58235 | 0.7236 | 470 |
| 58238 | 0.5138 | 248 |
| 58236 | 0.2393 | 72 |
Top tissues by expression
287 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| calcaneal tendon | UBERON:0003701 | 95.71 | gold quality |
| buccal mucosa cell | CL:0002336 | 94.32 | gold quality |
| endothelial cell | CL:0000115 | 93.90 | silver quality |
| cartilage tissue | UBERON:0002418 | 93.73 | gold quality |
| trigeminal ganglion | UBERON:0001675 | 93.49 | gold quality |
| jejunal mucosa | UBERON:0000399 | 92.91 | gold quality |
| colonic epithelium | UBERON:0000397 | 92.83 | gold quality |
| pericardium | UBERON:0002407 | 92.72 | gold quality |
| dorsal root ganglion | UBERON:0000044 | 92.47 | gold quality |
| Brodmann (1909) area 23 | UBERON:0013554 | 92.32 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 92.15 | gold quality |
| adrenal tissue | UBERON:0018303 | 92.07 | gold quality |
| cortical plate | UBERON:0005343 | 91.15 | gold quality |
| tendon | UBERON:0000043 | 91.03 | gold quality |
| rectum | UBERON:0001052 | 90.95 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 90.93 | gold quality |
| synovial joint | UBERON:0002217 | 90.92 | gold quality |
| corpus callosum | UBERON:0002336 | 90.59 | gold quality |
| colonic mucosa | UBERON:0000317 | 90.46 | gold quality |
| islet of Langerhans | UBERON:0000006 | 90.33 | gold quality |
| jejunum | UBERON:0002115 | 90.16 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 90.01 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 89.95 | gold quality |
| pons | UBERON:0000988 | 89.86 | gold quality |
| ventricular zone | UBERON:0003053 | 89.85 | gold quality |
| ganglionic eminence | UBERON:0004023 | 89.74 | gold quality |
| secondary oocyte | CL:0000655 | 89.49 | gold quality |
| superficial temporal artery | UBERON:0001614 | 89.47 | gold quality |
| oocyte | CL:0000023 | 89.45 | gold quality |
| oviduct epithelium | UBERON:0004804 | 89.24 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 4.92 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
218 targeting CSNK1G3, 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-200B-3P | 100.00 | 73.31 | 2693 |
| HSA-MIR-200C-3P | 100.00 | 73.35 | 2685 |
| HSA-MIR-429 | 100.00 | 73.44 | 2698 |
| HSA-MIR-3646 | 100.00 | 73.56 | 5283 |
| HSA-MIR-8485 | 100.00 | 77.57 | 4731 |
| HSA-MIR-3924 | 100.00 | 72.09 | 2394 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-186-5P | 99.99 | 70.83 | 3707 |
| HSA-MIR-3667-3P | 99.99 | 67.17 | 1636 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-513B-5P | 99.99 | 69.96 | 2150 |
| HSA-LET-7F-2-3P | 99.98 | 70.98 | 2588 |
| HSA-MIR-1185-1-3P | 99.98 | 71.04 | 2593 |
| HSA-MIR-1185-2-3P | 99.98 | 71.04 | 2593 |
| HSA-MIR-4803 | 99.98 | 71.99 | 3117 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-4789-5P | 99.98 | 70.76 | 2721 |
| HSA-MIR-6891-5P | 99.98 | 66.53 | 1372 |
| HSA-MIR-103A-3P | 99.98 | 69.14 | 1595 |
| HSA-MIR-107 | 99.98 | 69.14 | 1595 |
| HSA-MIR-9-3P | 99.96 | 70.88 | 2068 |
| HSA-MIR-548AT-5P | 99.96 | 70.83 | 2666 |
| HSA-MIR-1468-3P | 99.96 | 72.74 | 3797 |
| HSA-MIR-548AJ-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-548X-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-23A-3P | 99.95 | 74.24 | 3163 |
Literature-anchored findings (GeneRIF, showing 4)
- Intratumoral heterogeneity of CSNK1G3 mutations, a casein kinase 1, in colon cancers. (PMID:32241596)
- Protein proximity networks and functional evaluation of the casein kinase 1 gamma family reveal unique roles for CK1gamma3 in WNT signaling. (PMID:35487243)
- circCsnk1g3- and circAnkib1-regulated interferon responses in sarcoma promote tumorigenesis by shaping the immune microenvironment. (PMID:36433954)
- A novel nanoplatform-based circCSNK1G3 affects CBX7 protein and promotes glioma cell growth. (PMID:39033888)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Csnk1g3 | ENSMUSG00000073563 |
| rattus_norvegicus | Csnk1g3 | ENSRNOG00000016677 |
| drosophila_melanogaster | CG9962 | FBGN0031441 |
| caenorhabditis_elegans | csnk-1 | WBGENE00013709 |
Paralogs (12): VRK2 (ENSG00000028116), CDC7 (ENSG00000097046), VRK1 (ENSG00000100749), VRK3 (ENSG00000105053), CSNK1A1 (ENSG00000113712), TTBK2 (ENSG00000128881), CSNK1G2 (ENSG00000133275), CSNK1D (ENSG00000141551), TTBK1 (ENSG00000146216), CSNK1G1 (ENSG00000169118), CSNK1A1L (ENSG00000180138), CSNK1E (ENSG00000213923)
Protein
Protein identifiers
Casein kinase I isoform gamma-3 — Q9Y6M4 (reviewed: Q9Y6M4)
All UniProt accessions (3): Q9Y6M4, A0A8V8TKT3, H0YBN6
UniProt curated annotations — full annotation on UniProt →
Function. Serine/threonine-protein kinase. Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. It can phosphorylate a large number of proteins. Participates in Wnt signaling. Regulates fast synaptic transmission mediated by glutamate.
Subunit / interactions. Monomer.
Subcellular location. Cytoplasm.
Post-translational modifications. Autophosphorylated.
Activity regulation. Inhibited by triazolodiamine 1 (5-amino-3-([4-(aminosulfonyl)phenyl]amino)-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide), (S)-propane-1,2-diol, 2-({6-[(3-chlorophenyl)amino]-9-isopropyl-9H-purin-2-yl}amino)-3-methylbutan-1-ol, N2-[(1R,2S)-2-aminocyclohexyl]-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine and 4-amino-2-(3-chloroanilino)-1,3-thiazol-5-ylmethanone.
Similarity. Belongs to the protein kinase superfamily. CK1 Ser/Thr protein kinase family. Casein kinase I subfamily.
Isoforms (6)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9Y6M4-1 | 1, 3 | yes |
| Q9Y6M4-2 | 2, 3L, CSNK1G3L | |
| Q9Y6M4-3 | 3 | |
| Q9Y6M4-4 | 4 | |
| Q9Y6M4-5 | 5 | |
| Q9Y6M4-6 | 6 |
RefSeq proteins (16): NP_001026982, NP_001038188, NP_001257501, NP_001257502, NP_001257503, NP_001351069, NP_001351070, NP_001351072, NP_001351073, NP_001351074, NP_001351075, NP_001351076, NP_001351077, NP_001351078, NP_001351079, NP_004375 (=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 |
| IPR022247 | Casein_kinase-1_gamma_C | Domain |
| IPR050235 | CK1_Ser-Thr_kinase-like | Family |
Pfam: PF00069, PF12605
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 (57 total): helix 11, strand 10, turn 9, modified residue 6, splice variant 5, sequence conflict 4, compositionally biased region 4, region of interest 3, binding site 2, chain 1, domain 1, active site 1
Structure
Experimental structures (PDB)
10 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 2IZR | X-RAY DIFFRACTION | 1.3 |
| 6GRO | X-RAY DIFFRACTION | 1.45 |
| 2IZU | X-RAY DIFFRACTION | 1.85 |
| 2CHL | X-RAY DIFFRACTION | 1.95 |
| 2IZS | X-RAY DIFFRACTION | 1.95 |
| 2IZT | X-RAY DIFFRACTION | 2 |
| 4G17 | X-RAY DIFFRACTION | 2.1 |
| 4G16 | X-RAY DIFFRACTION | 2.3 |
| 4HGL | X-RAY DIFFRACTION | 2.4 |
| 4HGS | X-RAY DIFFRACTION | 2.4 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9Y6M4-F1 | 77.08 | 0.65 |
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): 162 (proton acceptor)
Ligand- & substrate-binding residues (2): 49–57; 72
Post-translational modifications (6): 1, 413, 366, 367, 291, 254
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 219 (showing top):
RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, GGTGTGT_MIR329, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, KEGG_HEDGEHOG_SIGNALING_PATHWAY, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, GOBP_VESICLE_MEDIATED_TRANSPORT, GOBP_REGULATION_OF_WNT_SIGNALING_PATHWAY, FOXO4_01, FOXO1_01, FOXD3_01, AAACCAC_MIR140, MILI_PSEUDOPODIA_HAPTOTAXIS_UP, GOBP_CANONICAL_WNT_SIGNALING_PATHWAY, PID_FOXO_PATHWAY, ZHAN_MULTIPLE_MYELOMA_HP_UP
GO Biological Process (6): endocytosis (GO:0006897), signal transduction (GO:0007165), Wnt signaling pathway (GO:0016055), protein modification process (GO:0036211), positive regulation of canonical Wnt signaling pathway (GO:0090263), protein phosphorylation (GO:0006468)
GO Molecular Function (8): protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (3): nucleus (GO:0005634), cytoplasm (GO:0005737), plasma membrane (GO:0005886)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein kinase activity | 2 |
| vesicle budding from membrane | 1 |
| membrane invagination | 1 |
| vesicle-mediated transport | 1 |
| import into cell | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| cell surface receptor signaling pathway | 1 |
| protein metabolic process | 1 |
| macromolecule modification | 1 |
| positive regulation of Wnt signaling pathway | 1 |
| canonical Wnt signaling pathway | 1 |
| regulation of canonical Wnt signaling pathway | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| intracellular membrane-bounded organelle | 1 |
| intracellular anatomical structure | 1 |
| cellular anatomical structure | 1 |
| membrane | 1 |
| cell periphery | 1 |
Protein interactions and networks
STRING
1288 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CSNK1G3 | CTNNA2 | P26232 | 462 |
| CSNK1G3 | LRP8 | Q14114 | 430 |
| CSNK1G3 | LRP1B | Q9NZR2 | 410 |
| CSNK1G3 | EDAR | Q9UNE0 | 398 |
| CSNK1G3 | WNT2 | P09544 | 391 |
| CSNK1G3 | CSNK1G1 | Q9HCP0 | 390 |
| CSNK1G3 | PDIK1L | Q8N165 | 384 |
| CSNK1G3 | NEO1 | Q92859 | 381 |
| CSNK1G3 | UBAC2 | Q8NBM4 | 381 |
| CSNK1G3 | LRP6 | O75581 | 376 |
| CSNK1G3 | TMEM220 | Q6QAJ8 | 369 |
| CSNK1G3 | ZNF433 | Q8N7K0 | 358 |
| CSNK1G3 | ALB | P02768 | 351 |
| CSNK1G3 | SLC35A2 | P78381 | 336 |
| CSNK1G3 | N0E472 | N0E472 | 327 |
IntAct
79 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| MED21 | MED19 | psi-mi:“MI:0914”(association) | 0.880 |
| GPR156 | PLD2 | psi-mi:“MI:0914”(association) | 0.640 |
| CSNK1G3 | CSNK1G2 | psi-mi:“MI:0914”(association) | 0.640 |
| CSNK1G1 | CSNK1G3 | psi-mi:“MI:0915”(physical association) | 0.620 |
| SLC31A1 | C2orf72 | psi-mi:“MI:0914”(association) | 0.530 |
| GJB7 | PALM3 | psi-mi:“MI:0914”(association) | 0.530 |
| S1PR2 | PALM3 | psi-mi:“MI:0914”(association) | 0.530 |
| TPCN2 | AP3B1 | psi-mi:“MI:0914”(association) | 0.530 |
| MRAP2 | GOLIM4 | psi-mi:“MI:0914”(association) | 0.530 |
| CSNK1G2 | GINS1 | psi-mi:“MI:0914”(association) | 0.530 |
| CSNK1G2 | MAPK14 | psi-mi:“MI:0914”(association) | 0.530 |
| PNMA2 | CCDC85C | psi-mi:“MI:0914”(association) | 0.530 |
| NRAS | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.480 |
| CSNK1G3 | LRRK2 | psi-mi:“MI:0217”(phosphorylation reaction) | 0.440 |
| GPC1 | SNAP23 | psi-mi:“MI:0915”(physical association) | 0.400 |
| GPC1 | GANAB | psi-mi:“MI:0915”(physical association) | 0.400 |
| M2 | IPO5 | psi-mi:“MI:0914”(association) | 0.350 |
| SGK1 | psi-mi:“MI:0914”(association) | 0.350 | |
| TBKBP1 | psi-mi:“MI:0914”(association) | 0.350 | |
| AHRR | psi-mi:“MI:0914”(association) | 0.350 | |
| PAK4 | psi-mi:“MI:0914”(association) | 0.350 | |
| ZDHHC5 | IGKV2D-24 | psi-mi:“MI:0914”(association) | 0.350 |
| CSNK1G2 | ZSWIM8 | psi-mi:“MI:0914”(association) | 0.350 |
| HASPIN | MYO1C | psi-mi:“MI:0914”(association) | 0.350 |
| CSNK1G3 | ACACB | psi-mi:“MI:0914”(association) | 0.350 |
| CSNK1G3 | YWHAG | psi-mi:“MI:0914”(association) | 0.350 |
| SAA1 | PLEKHG3 | psi-mi:“MI:0914”(association) | 0.350 |
| PROSER2 | VWA8 | psi-mi:“MI:0914”(association) | 0.350 |
| TSPAN10 | KLRG2 | psi-mi:“MI:0914”(association) | 0.350 |
| PTP4A3 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (182): CSNK1G3 (Biochemical Activity), CSNK1G3 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-Western), UBXN7 (Affinity Capture-Western), CSNK1G3 (Affinity Capture-MS), CSNK1G1 (Affinity Capture-MS), ANKRD13D (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS)
ESM2 similar proteins: A7E3X2, O74135, P29295, P35508, P40233, P40234, P40236, P42158, P48730, P49674, P51566, P78368, Q03141, Q06486, Q20471, Q39050, Q4R9A9, Q556Y4, Q5BP74, Q5PRD4, Q5R4V3, Q5RC72, Q5XF24, Q5ZJS0, Q5ZLL1, Q62761, Q62762, Q62763, Q6K9N1, Q6NRT0, Q6P3K7, Q6P647, Q7T2E3, Q8BTH8, Q8BVP5, Q8C4X2, Q8LPI7, Q8LPJ1, Q8VYK9, Q8WQ99
Diamond homologs: A7E3X2, B9VVJ6, O15726, O19175, O74135, O76324, O80888, P16912, P22517, P23291, P23292, P28327, P29295, P34516, P34633, P35507, P35508, P35509, P39962, P40230, P40233, P40234, P40235, P40236, P42158, P42168, P48729, P48730, P49615, P49674, P51166, P54367, P67827, P67828, P67829, P67962, P67963, P78368, P81123, P97633
SIGNOR signaling
3 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| CSNK1G3 | “up-regulates quantity by stabilization” | LYN | phosphorylation |
| CSNK1G3 | “up-regulates activity” | LRP6 | phosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 120 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 |
|---|---|---|---|
| Signaling by SCF-KIT | 5 | 16.6× | 8e-04 |
| Respiratory Syncytial Virus Infection Pathway | 5 | 13.1× | 2e-03 |
| RSV-host interactions | 6 | 12.5× | 7e-04 |
| Signaling by BRAF and RAF1 fusions | 5 | 11.4× | 2e-03 |
| Cytokine Signaling in Immune system | 8 | 4.3× | 6e-03 |
| Infectious disease | 11 | 3.6× | 3e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
56 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 1 |
| Likely pathogenic | 0 |
| Uncertain significance | 35 |
| Likely benign | 3 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 150374 | GRCh38/hg38 5q22.1-23.3(chr5:110687442-130103838)x1 | Pathogenic |
SpliceAI
1475 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 5:123545842:G:GA | donor_loss | 1.0000 |
| 5:123545842:G:GG | donor_gain | 1.0000 |
| 5:123545843:T:A | donor_loss | 1.0000 |
| 5:123554808:G:GT | donor_gain | 1.0000 |
| 5:123557489:A:AG | acceptor_gain | 1.0000 |
| 5:123557490:A:G | acceptor_gain | 1.0000 |
| 5:123573388:CCCA:C | acceptor_loss | 1.0000 |
| 5:123573390:CA:C | acceptor_loss | 1.0000 |
| 5:123573391:A:AG | acceptor_gain | 1.0000 |
| 5:123573391:AGAT:A | acceptor_gain | 1.0000 |
| 5:123573391:AGATG:A | acceptor_gain | 1.0000 |
| 5:123573392:G:A | acceptor_loss | 1.0000 |
| 5:123573392:G:GT | acceptor_gain | 1.0000 |
| 5:123573392:GA:G | acceptor_gain | 1.0000 |
| 5:123573392:GAT:G | acceptor_gain | 1.0000 |
| 5:123573392:GATG:G | acceptor_gain | 1.0000 |
| 5:123573392:GATGG:G | acceptor_gain | 1.0000 |
| 5:123573538:ACTG:A | donor_gain | 1.0000 |
| 5:123573541:GGTA:G | donor_loss | 1.0000 |
| 5:123573542:G:A | donor_loss | 1.0000 |
| 5:123573542:G:GG | donor_gain | 1.0000 |
| 5:123575721:A:AG | acceptor_gain | 1.0000 |
| 5:123588066:A:AG | acceptor_gain | 1.0000 |
| 5:123588067:G:GA | acceptor_gain | 1.0000 |
| 5:123588421:TTTTA:T | acceptor_loss | 1.0000 |
| 5:123588422:TTTA:T | acceptor_loss | 1.0000 |
| 5:123588423:TTA:T | acceptor_loss | 1.0000 |
| 5:123588424:TA:T | acceptor_loss | 1.0000 |
| 5:123588425:A:AG | acceptor_gain | 1.0000 |
| 5:123588426:G:GG | acceptor_gain | 1.0000 |
AlphaMissense
3000 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 5:123545779:T:A | V39D | 1.000 |
| 5:123545781:G:A | G40R | 1.000 |
| 5:123545781:G:C | G40R | 1.000 |
| 5:123545782:G:A | G40E | 1.000 |
| 5:123545782:G:T | G40V | 1.000 |
| 5:123545790:T:C | F43L | 1.000 |
| 5:123545791:T:C | F43S | 1.000 |
| 5:123545791:T:G | F43C | 1.000 |
| 5:123545792:T:A | F43L | 1.000 |
| 5:123545792:T:G | F43L | 1.000 |
| 5:123545797:T:A | V45D | 1.000 |
| 5:123545809:T:A | I49N | 1.000 |
| 5:123545811:G:A | G50R | 1.000 |
| 5:123545811:G:C | G50R | 1.000 |
| 5:123545812:G:A | G50E | 1.000 |
| 5:123545812:G:T | G50V | 1.000 |
| 5:123545817:G:A | G52S | 1.000 |
| 5:123545817:G:C | G52R | 1.000 |
| 5:123545817:G:T | G52C | 1.000 |
| 5:123545818:G:A | G52D | 1.000 |
| 5:123545818:G:C | G52A | 1.000 |
| 5:123545818:G:T | G52V | 1.000 |
| 5:123545822:T:A | N53K | 1.000 |
| 5:123545822:T:G | N53K | 1.000 |
| 5:123545823:T:A | F54I | 1.000 |
| 5:123545823:T:C | F54L | 1.000 |
| 5:123545823:T:G | F54V | 1.000 |
| 5:123545824:T:C | F54S | 1.000 |
| 5:123545824:T:G | F54C | 1.000 |
| 5:123545825:T:A | F54L | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000012535 (5:123516351 T>C), RS1000044655 (5:123552386 C>T), RS1000065318 (5:123612299 A>G), RS1000070508 (5:123545499 C>T), RS1000080910 (5:123538876 T>A,G), RS1000120943 (5:123571510 A>C,G,T), RS1000145525 (5:123530133 A>G), RS1000173273 (5:123534872 G>A), RS1000229382 (5:123527022 A>G), RS1000246965 (5:123579135 C>T), RS1000269927 (5:123608693 A>G), RS1000311731 (5:123568396 C>G,T), RS1000314618 (5:123608969 G>A,T), RS1000322808 (5:123586362 A>G), RS1000323256 (5:123546027 G>A)
Disease associations
OMIM: gene MIM:604253 | disease phenotypes:
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| Tourette syndrome | Limited | Unknown |
Mondo (1): Tourette syndrome (MONDO:0007661)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
26 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST000406_12 | Amyotrophic lateral sclerosis | 3.000000e-06 |
| GCST002221_16 | Cholesterol, total | 2.000000e-09 |
| GCST002222_57 | LDL cholesterol | 4.000000e-12 |
| GCST002928_27 | Nickel levels | 8.000000e-06 |
| GCST003833_6 | Adult asthma | 1.000000e-06 |
| GCST004233_13 | LDL cholesterol levels | 3.000000e-12 |
| GCST004235_45 | Total cholesterol levels | 2.000000e-09 |
| GCST005331_2 | CSF tryptophan concentration in tuberculous meningitis | 4.000000e-06 |
| GCST005348_171 | Total body bone mineral density | 8.000000e-12 |
| GCST005348_73 | Total body bone mineral density | 1.000000e-09 |
| GCST005559_11 | Virologic severity in Herpes simplex virus type 2 infection | 4.000000e-07 |
| GCST006230_1 | Pulse pressure | 9.000000e-07 |
| GCST006258_8 | Diastolic blood pressure | 2.000000e-11 |
| GCST006259_38 | Systolic blood pressure | 1.000000e-06 |
| GCST006288_216 | Heel bone mineral density | 3.000000e-10 |
| GCST006288_536 | Heel bone mineral density | 2.000000e-10 |
| GCST006612_23 | LDL cholesterol | 2.000000e-08 |
| GCST006979_117 | Heel bone mineral density | 3.000000e-30 |
| GCST007268_19 | Diastolic blood pressure | 1.000000e-11 |
| GCST007576_195 | Chronotype | 2.000000e-09 |
| GCST009391_595 | Metabolite levels | 1.000000e-08 |
| GCST010204_89 | Low density lipoprotein cholesterol levels | 2.000000e-19 |
| GCST010243_165 | Apolipoprotein B levels | 2.000000e-21 |
| GCST010245_147 | LDL cholesterol levels | 4.000000e-19 |
| GCST011772_2 | Rapid response to perioperative phenylephrine (change in systolic blood pressure) | 5.000000e-08 |
| GCST90002404_212 | Red cell distribution width | 8.000000e-12 |
EFO canonical traits (13, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004574 | total cholesterol measurement |
| EFO:0004611 | low density lipoprotein cholesterol measurement |
| EFO:0008534 | tryptophan measurement |
| EFO:0009010 | HSV2 virologic severity measurement |
| EFO:0005763 | pulse pressure measurement |
| EFO:0006336 | diastolic blood pressure |
| EFO:0006335 | systolic blood pressure |
| EFO:0009270 | heel bone mineral density |
| EFO:0008328 | chronotype measurement |
| EFO:0010502 | indoxyl sulfate measurement |
| EFO:0004615 | apolipoprotein B measurement |
| EFO:0006944 | systolic blood pressure change measurement |
| EFO:0009188 | Red cell distribution width |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D005879 | Tourette Syndrome | C10.228.140.079.898; C10.228.662.825.800; C10.574.500.850; C16.320.400.820; F03.625.992.850 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5084 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
16 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 101,368 (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 |
|---|---|---|---|
| CHEMBL180022 | NERATINIB | 4 | 9,404 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL14762 | SELICICLIB | 2 | 3,787 |
| CHEMBL1614713 | CC-401 | 2 | 389 |
| CHEMBL1721885 | SU-014813 | 2 | 363 |
| CHEMBL1967878 | CENISERTIB | 2 | 358 |
| CHEMBL230011 | TG100-115 | 2 | 1,504 |
| CHEMBL363648 | TAK-715 | 2 | 442 |
| CHEMBL513909 | BI-2536 | 2 | 895 |
| CHEMBL1908397 | KW-2449 | 1 | 622 |
| CHEMBL260933 | GS 6201 | 1 | 298 |
| CHEMBL3544966 | GSK-1059615 | 1 | 1,928 |
| CHEMBL3545083 | RGB-286638 | 1 | 551 |
| CHEMBL482967 | CYC-116 | 1 | 651 |
| CHEMBL571948 | Y-39983 | 1 | 705 |
| CHEMBL574738 | AST-487 | 1 | 451 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — Casein kinase 1 (CK1) family
Most potent curated ligand interactions (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| SGC-CK1γ-1 | Inhibition | 6.02 | pIC50 |
Binding affinities (BindingDB)
5 measured of 5 human assays (5 total across all organisms); most potent 5 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| (2R)-2-[[6-(benzylamino)-9-isopropyl-purin-2-yl]amino]butan-1-ol | KD | 260 nM |
| 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | KD | 1400 nM |
| 5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide | KD | 2600 nM |
| 1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b | KD | 3100 nM |
| N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | KD | 3500 nM |
ChEMBL bioactivities
201 potent at pChembl≥5 of 202 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.10 | Ki | 7.943 | nM | CHEMBL1999931 |
| 8.00 | Ki | 10 | nM | CHEMBL1965660 |
| 7.70 | Ki | 19.95 | nM | CHEMBL1969588 |
| 7.70 | Ki | 19.95 | nM | CHEMBL2003638 |
| 7.50 | Ki | 31.62 | nM | CHEMBL1981079 |
| 7.50 | Ki | 31.62 | nM | CHEMBL2006439 |
| 7.50 | Ki | 31.62 | nM | CHEMBL1990288 |
| 7.43 | Kd | 37 | nM | CHEMBL5434183 |
| 7.40 | Ki | 39.81 | nM | CHEMBL1996066 |
| 7.30 | Ki | 50.12 | nM | CHEMBL1966628 |
| 7.10 | Ki | 79.43 | nM | CHEMBL1964290 |
| 7.10 | Ki | 79.43 | nM | CHEMBL1998159 |
| 7.10 | Ki | 79.43 | nM | CHEMBL1991078 |
| 7.01 | Kd | 97 | nM | CC-401 |
| 7.01 | Kd | 97 | nM | AST-487 |
| 7.00 | Kd | 100 | nM | CHEMBL1349996 |
| 7.00 | Ki | 100 | nM | CHEMBL1989646 |
| 7.00 | Ki | 100 | nM | CHEMBL1970903 |
| 7.00 | Ki | 100 | nM | CHEMBL1994830 |
| 6.90 | Ki | 125.9 | nM | CHEMBL1975900 |
| 6.90 | Ki | 125.9 | nM | CHEMBL1982361 |
| 6.82 | Kd | 150 | nM | CHEMBL5414359 |
| 6.80 | Ki | 158.5 | nM | CHEMBL1980489 |
| 6.80 | Ki | 158.5 | nM | CHEMBL225519 |
| 6.80 | Ki | 158.5 | nM | CHEMBL1978448 |
| 6.80 | Ki | 158.5 | nM | CHEMBL1969843 |
| 6.80 | Ki | 158.5 | nM | CHEMBL396523 |
| 6.80 | Ki | 158.5 | nM | CHEMBL1991063 |
| 6.70 | Ki | 199.5 | nM | CHEMBL1990288 |
| 6.62 | Kd | 240 | nM | SUNITINIB |
| 6.60 | Ki | 251.2 | nM | CHEMBL1995813 |
| 6.60 | Ki | 251.2 | nM | CHEMBL1971186 |
| 6.60 | Ki | 251.2 | nM | CHEMBL1994864 |
| 6.60 | Ki | 251.2 | nM | CHEMBL1974870 |
| 6.60 | Ki | 251.2 | nM | CHEMBL243088 |
| 6.54 | Kd | 290 | nM | CHEMBL5416758 |
| 6.54 | Kd | 290 | nM | CHEMBL408982 |
| 6.50 | Ki | 316.2 | nM | CHEMBL1988173 |
| 6.50 | Ki | 316.2 | nM | CHEMBL1986781 |
| 6.40 | Ki | 398.1 | nM | CHEMBL244378 |
| 6.37 | Kd | 427 | nM | CHEMBL3688339 |
| 6.34 | IC50 | 460 | nM | CHEMBL4101902 |
| 6.30 | Ki | 501.2 | nM | CHEMBL2005936 |
| 6.30 | Ki | 501.2 | nM | CHEMBL1972158 |
| 6.30 | Ki | 501.2 | nM | CHEMBL1965836 |
| 6.30 | Ki | 501.2 | nM | CHEMBL1986186 |
| 6.30 | Ki | 501.2 | nM | CHEMBL1979252 |
| 6.30 | Ki | 501.2 | nM | CHEMBL1988153 |
| 6.30 | Ki | 501.2 | nM | CHEMBL1990885 |
| 6.30 | Ki | 501.2 | nM | CHEMBL1998414 |
PubChem BioAssay actives
37 with measured affinity, of 1586 total; 29 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 |
|---|---|---|---|---|
| 5-[(5S)-5-(4-chlorophenyl)-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazol-3-yl]-3-methyl-2H-indazole | 2030650: Binding affinity to CSNK1G3 (unknown origin) assessed as dissociation constant by competitive binding assay | kd | 0.0370 | uM |
| 3-[3-(2-piperidin-1-ylethoxy)phenyl]-5-(1H-1,2,4-triazol-5-yl)-1H-indazole | 1424966: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0970 | uM |
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 435905: Binding constant for full-length CSNK1G3 | kd | 0.0970 | uM |
| (1E)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one | 1722615: Binding affinity to CSNK1G3 (unknown origin) | kd | 0.1000 | uM |
| 5-[4-[(4-chlorophenyl)methyl]-5-methyl-1,2,4-triazol-3-yl]-3-methyl-2H-indazole | 2030650: Binding affinity to CSNK1G3 (unknown origin) assessed as dissociation constant by competitive binding assay | kd | 0.1500 | uM |
| Sunitinib | 435905: Binding constant for full-length CSNK1G3 | kd | 0.2400 | uM |
| 5-[(5S)-5-(4-chlorophenyl)-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazol-3-yl]-3-methyl-2H-pyrazolo[4,3-b]pyridine | 2030650: Binding affinity to CSNK1G3 (unknown origin) assessed as dissociation constant by competitive binding assay | kd | 0.2900 | uM |
| (1Z)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one | 445574: Binding affinity to CSNK1G3 assessed as dissociation constant | kd | 0.2900 | uM |
| 1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone | 1424966: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.4270 | uM |
| 4-[3-amino-6-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-yl]-2-fluorobenzamide | 1434404: Inhibition of full length GST-tagged recombinant human CSNK1G3 expressed in baculovirus expression system | ic50 | 0.4600 | uM |
| 5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | 435905: Binding constant for full-length CSNK1G3 | kd | 0.5700 | uM |
| 5-[(5S)-5-(4-chlorophenyl)-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazol-3-yl]-3-methyl-2H-pyrazolo[3,4-b]pyridine | 2030650: Binding affinity to CSNK1G3 (unknown origin) assessed as dissociation constant by competitive binding assay | kd | 0.6700 | uM |
| 4-[(1R)-1-aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide | 1424966: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.7820 | uM |
| N-(2,2-difluoro-5H-[1,3]dioxolo[4,5-f]benzimidazol-6-yl)-3-methoxybenzamide | 1162642: Inhibition of GST-tagged human CK1gamma3 expressed in Escherichia coli using using alpha casein substrate by SDS-PAGE based autoradiography | ic50 | 0.8000 | uM |
| N-(2,2-difluoro-5H-[1,3]dioxolo[4,5-f]benzimidazol-6-yl)-2-[[2-(trifluoromethoxy)benzoyl]amino]-1,3-thiazole-4-carboxamide | 1162642: Inhibition of GST-tagged human CK1gamma3 expressed in Escherichia coli using using alpha casein substrate by SDS-PAGE based autoradiography | ic50 | 0.8100 | uM |
| 3-methyl-5-[5-methyl-4-[[4-(trifluoromethyl)phenyl]methyl]-1,2,4-triazol-3-yl]-2H-indazole | 2030650: Binding affinity to CSNK1G3 (unknown origin) assessed as dissociation constant by competitive binding assay | kd | 0.8600 | uM |
| (2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine | 624949: Binding constant for CSNK1G3 kinase domain | kd | 0.9100 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624949: Binding constant for CSNK1G3 kinase domain | kd | 1.2000 | uM |
| (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | 1715393: Inhibition of human CK1gamma3 using KRRRAL[pS]VASLPGL as substrate by [gamma-33P]-ATP assay | ic50 | 1.9800 | uM |
| 4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2148162: Binding affinity to human CSNK1G3 incubated for 45 mins by Kinobead based pull down assay | kd | 2.1730 | uM |
| 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | 624949: Binding constant for CSNK1G3 kinase domain | kd | 2.4000 | uM |
| 2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol | 624949: Binding constant for CSNK1G3 kinase domain | kd | 2.6000 | uM |
| (5Z)-5-[(4-pyridin-4-ylquinolin-6-yl)methylidene]-1,3-thiazolidine-2,4-dione | 1424966: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 2.8610 | uM |
| (2R)-2-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol | 435905: Binding constant for full-length CSNK1G3 | kd | 2.9000 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2148162: Binding affinity to human CSNK1G3 incubated for 45 mins by Kinobead based pull down assay | kd | 6.1372 | uM |
| 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine | 1424966: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 7.5360 | uM |
| Neratinib | 624949: Binding constant for CSNK1G3 kinase domain | kd | 7.8000 | uM |
| 4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 435905: Binding constant for full-length CSNK1G3 | kd | 7.9000 | uM |
| 3-[2,4-diamino-7-(3-hydroxyphenyl)pteridin-6-yl]phenol | 624949: Binding constant for CSNK1G3 kinase domain | kd | 8.7000 | uM |
CTD chemical–gene interactions
41 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| 7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide | decreases expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| GSK-J4 | increases expression | 1 |
| FR900359 | increases phosphorylation | 1 |
| ginger extract | affects cotreatment, affects expression, increases abundance | 1 |
| dicrotophos | decreases expression | 1 |
| alpha-pinene | affects cotreatment, increases expression, increases abundance | 1 |
| bisphenol A | affects cotreatment, affects expression, increases abundance | 1 |
| arsenite | affects binding, decreases reaction | 1 |
| mono-(2-ethylhexyl)phthalate | increases abundance, increases methylation | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | increases expression | 1 |
| sodium arsenite | affects cotreatment, increases abundance, increases expression | 1 |
| 2-bromopalmitate | decreases reaction, increases abundance, increases palmitoylation | 1 |
| manganese chloride | increases abundance, increases expression, affects cotreatment | 1 |
| methacrylaldehyde | affects cotreatment, increases expression, increases abundance | 1 |
| beta-methylcholine | affects expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| CGP 52608 | increases reaction, affects binding | 1 |
| jinfukang | decreases expression | 1 |
| Resveratrol | affects cotreatment, increases expression | 1 |
| Leflunomide | increases expression | 1 |
| Acrolein | increases abundance, affects cotreatment, increases expression | 1 |
| Air Pollutants | increases abundance, increases expression, affects cotreatment | 1 |
| Arsenic | affects cotreatment, increases abundance, increases expression | 1 |
| Cadmium | decreases reaction, increases abundance, increases palmitoylation | 1 |
| Caffeine | decreases phosphorylation | 1 |
| Coumestrol | decreases expression | 1 |
| Diethylhexyl Phthalate | increases abundance, increases methylation | 1 |
| Doxorubicin | decreases expression | 1 |
| Manganese | increases abundance, increases expression, affects cotreatment | 1 |
ChEMBL screening assays
216 unique, capped per target: 215 binding, 1 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1034090 | Binding | Inhibition of CSNK1G3 at 3 uM | Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. — J Med Chem |
| CHEMBL1964116 | Functional | PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: CSNK1G3 | PubChem BioAssay data set |
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_D7N0 | Ubigene A-549 CSNK1G3 KO | Cancer cell line | Male |
| CVCL_D8JH | Ubigene HCT 116 CSNK1G3 KO | Cancer cell line | Male |
| CVCL_D9CI | Ubigene HEK293 CSNK1G3 KO | Transformed cell line | Female |
| CVCL_E0B7 | Ubigene HeLa CSNK1G3 KO | Cancer cell line | Female |
| CVCL_SJ89 | HAP1 CSNK1G3 (-) 1 | Cancer cell line | Male |
| CVCL_SJ90 | HAP1 CSNK1G3 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
183 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00152750 | PHASE4 | UNKNOWN | Study of Clonidine on Sleep Architecture in Children With Tourette’s Syndrome (TS) and Comorbid ADHD |
| NCT00226824 | PHASE4 | TERMINATED | Safety Study of Galantamine in Tic Disorders |
| NCT00241176 | PHASE4 | COMPLETED | Open Label Trial of Aripiprazole in Children and Adolescents With Tourette’s Disorder |
| NCT00370838 | PHASE4 | COMPLETED | Comparison of Keppra and Clonidine in the Treatment of Tics |
| NCT01018056 | PHASE4 | COMPLETED | Developing New Treatments for Tourette Syndrome: Therapeutic Trials With Modulators of Glutamatergic Neurotransmission |
| NCT01547000 | PHASE4 | COMPLETED | Guanfacine in Children With Tic Disorders |
| NCT03239210 | PHASE4 | COMPLETED | Effects of Ondansetron in Obsessive-compulsive and Tic Disorders |
| NCT00004376 | PHASE3 | COMPLETED | Phase III Randomized, Double-Blind, Placebo-Controlled Study of Guanfacine for Tourette Syndrome and Attention Deficit Hyperactivity Disorder |
| NCT00206323 | PHASE3 | COMPLETED | A Randomized, Placebo-controlled, Tourette Syndrome Study. |
| NCT00206336 | PHASE3 | COMPLETED | An Open-label Study to Determine the Efficacy and Safety of Topiramate in the Treatment of Tourette Syndrome. |
| NCT00478842 | PHASE3 | COMPLETED | Pallidal Stimulation and Gilles de la Tourette Syndrome |
| NCT00681863 | PHASE3 | TERMINATED | Open-label Extension Study of Pramipexole in the Treatment of Children and Adolescents With Tourette Syndrome |
| NCT01501695 | PHASE3 | COMPLETED | Phase III Study of 5LGr to Treat Tic Disorder |
| NCT03087201 | PHASE3 | COMPLETED | CANNAbinoids in the Treatment of TICS (CANNA-TICS) |
| NCT03487783 | PHASE3 | COMPLETED | Aripiprazole Oral Solution in the Treatment of Children and Adolescents With Tourette’s Syndrome |
| NCT03567291 | PHASE3 | TERMINATED | Evaluation of Safety and Tolerability of Long-term TEV-50717 (Deutetrabenazine) for Treatment of Tourette Syndrome in Children and Adolescents |
| NCT03571256 | PHASE3 | COMPLETED | A Study to Test if TEV-50717 is Effective in Relieving Tics Associated With Tourette Syndrome (TS) |
| NCT06021522 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate Long-term Safety of Ecopipam Tablets in Children, Adolescents and Adults With Tourette’s Disorder |
| NCT00004393 | PHASE2 | COMPLETED | Phase II Double Blind Placebo Controlled Trial of Risperidone in Tourette Syndrome |
| NCT00004652 | PHASE2 | COMPLETED | Phase II Pilot Controlled Study of Short Vs Longer Term Pimozide (Orap) Therapy in Tourette Syndrome |
| NCT00231985 | PHASE2 | COMPLETED | Effectiveness of Behavior Therapy and Psychosocial Therapy for the Treatment of Tourette Syndrome and Chronic Tic Disorder |
| NCT00311909 | PHASE2 | COMPLETED | Thalamic Deep Brain Stimulation for Tourette Syndrome |
| NCT00529308 | PHASE2 | COMPLETED | Transcranial Magnetic Stimulation (TMS) for Individuals With Tourette’s Syndrome |
| NCT00558467 | PHASE2 | COMPLETED | Pramipexole Pilot Phase II Study in Children and Adolescents With Tourette Disorder According to DSM-IV Criteria |
| NCT01043549 | PHASE2 | TERMINATED | Repetitive Transcranial Magnetic Stimulation of the Posterior Parietal Cortex in Patients Suffering From Gilles de la Tourette Syndrome |
| NCT01133353 | PHASE2 | WITHDRAWN | A Study of the Effectiveness and Safety of Tetrabenazine MR in Pediatric Subjects With Tourette’s Syndrome |
| NCT01475383 | PHASE2 | WITHDRAWN | Study Evaluating The Safety And Efficacy Of PF-03654746 In Adult Subjects With Tourette’s Syndrome |
| NCT01647269 | PHASE2 | COMPLETED | A Trial of Bilateral Deep Brain Stimulation to the Globus Pallidus Internum in Tourette Syndrome |
| NCT01904773 | PHASE2 | COMPLETED | Safety, Tolerability, Pharmacokinetic, and Efficacy Study of AZD5213 in Adolescents With Tourette’s Disorder |
| NCT02102698 | PHASE2 | COMPLETED | Ecopipam Treatment of Tourette’s Syndrome in Subjects 7-17 Years |
| NCT02217007 | PHASE2 | WITHDRAWN | A Trial Evaluating the Efficacy, Safety, and Pharmacokinetics of SNC-102 in Subjects With Tourette Syndrome |
| NCT02247206 | PHASE2 | COMPLETED | VoIP Delivered Behavior Therapy for Tourette Syndrome |
| NCT02581865 | PHASE2 | COMPLETED | Safety and Efficacy Study of NBI-98854 in Adults With Tourette Syndrome |
| NCT02619084 | PHASE2 | COMPLETED | Subthalamic Stimulation in Tourette’s Syndrome |
| NCT02679079 | PHASE2 | COMPLETED | Safety and Efficacy Study of NBI-98854 in Children and Adolescents With Tourette Syndrome |
| NCT02879578 | PHASE2 | COMPLETED | Safety and Tolerability Study of NBI-98854 for the Treatment of Subjects With Tourette Syndrome |
| NCT03066193 | PHASE2 | COMPLETED | Efficacy of a Therapeutic Combination of Dronabinol and PEA for Tourette Syndrome |
| NCT03247244 | PHASE2 | TERMINATED | Safety and Efficacy of Cannabis in Tourette Syndrome |
| NCT03325010 | PHASE2 | COMPLETED | Safety, Tolerability, and Efficacy of NBI-98854 for the Treatment of Pediatric Subjects With Tourette Syndrome |
| NCT03444038 | PHASE2 | COMPLETED | Open-Label Safety and Tolerability Study of NBI-98854 for the Treatment of Pediatric Subjects With Tourette Syndrome |
Related Atlas pages
- Associated diseases: Tourette syndrome
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): Tourette syndrome