CSNK1G2

Summary

CSNK1G2 (casein kinase 1 gamma 2, HGNC:2455) is a protein-coding gene on chromosome 19p13.3, encoding Casein kinase I isoform gamma-2 (P78368). Serine/threonine-protein kinase.

Enables protein serine/threonine kinase activity. Predicted to be involved in endocytosis; positive regulation of canonical Wnt signaling pathway; and signal transduction. Located in membrane.

Source: NCBI Gene 1455 — RefSeq curated summary.

At a glance

• GWAS associations: 8
• Clinical variants (ClinVar): 60 total
• Druggable target: yes — 22 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001319

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2455
Approved symbol	CSNK1G2
Name	casein kinase 1 gamma 2
Location	19p13.3
Locus type	gene with protein product
Status	Approved
Aliases	CK1g2
Ensembl gene	ENSG00000133275
Ensembl biotype	protein_coding
OMIM	602214
Entrez	1455

Gene structure

Transcript identifiers

Ensembl transcripts: 27 — 22 protein_coding, 3 retained_intron, 1 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000255641, ENST00000585957, ENST00000585959, ENST00000589350, ENST00000589385, ENST00000589861, ENST00000590106, ENST00000591002, ENST00000591752, ENST00000614707, ENST00000615564, ENST00000890345, ENST00000890346, ENST00000890347, ENST00000935016, ENST00000935017, ENST00000935018, ENST00000935019, ENST00000935020, ENST00000935021, ENST00000935022, ENST00000935023, ENST00000935024, ENST00000935025, ENST00000949202, ENST00000949203, ENST00000949204

RefSeq mRNA: 1 — MANE Select: NM_001319 NM_001319

CCDS: CCDS12077

Canonical transcript exons

ENST00000255641 — 12 exons

Exon	Start	End
ENSE00001375639	1980149	1981338
ENSE00001547251	1941172	1941418
ENSE00001685652	1978442	1978511
ENSE00002281299	1969508	1969959
ENSE00003504585	1978859	1979093
ENSE00003568837	1978602	1978750
ENSE00003578542	1979911	1980017
ENSE00003637916	1979163	1979248
ENSE00003675744	1979752	1979835
ENSE00003680258	1979495	1979643
ENSE00003790088	1979319	1979403
ENSE00003790624	1978305	1978345

Expression profiles

Bgee: expression breadth ubiquitous, 297 present calls, max score 98.59.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 44.1414 / max 877.9400, expressed in 1824 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
173019	42.8905	1823
173020	0.8437	499
173018	0.3053	102
173021	0.0861	29
173022	0.0159	3

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
left testis	UBERON:0004533	98.59	gold quality
right testis	UBERON:0004534	98.56	gold quality
endothelial cell	CL:0000115	98.23	gold quality
granulocyte	CL:0000094	98.06	gold quality
cervix squamous epithelium	UBERON:0006922	97.82	gold quality
testis	UBERON:0000473	96.83	gold quality
sural nerve	UBERON:0015488	96.59	gold quality
pancreatic ductal cell	CL:0002079	96.42	gold quality
blood	UBERON:0000178	96.36	gold quality
pylorus	UBERON:0001166	95.83	gold quality
right hemisphere of cerebellum	UBERON:0014890	95.82	gold quality
Brodmann (1909) area 10	UBERON:0013541	95.71	gold quality
periodontal ligament	UBERON:0008266	95.52	gold quality
spleen	UBERON:0002106	95.45	gold quality
cerebellar hemisphere	UBERON:0002245	95.32	gold quality
cerebellar cortex	UBERON:0002129	95.31	gold quality
lower esophagus mucosa	UBERON:0035834	95.24	gold quality
cerebellar vermis	UBERON:0004720	95.22	gold quality
monocyte	CL:0000576	95.15	gold quality
mononuclear cell	CL:0000842	95.08	gold quality
leukocyte	CL:0000738	95.07	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	94.99	gold quality
stromal cell of endometrium	CL:0002255	94.98	gold quality
cerebellum	UBERON:0002037	94.94	gold quality
adenohypophysis	UBERON:0002196	94.91	gold quality
metanephros cortex	UBERON:0010533	94.84	gold quality
pituitary gland	UBERON:0000007	94.50	gold quality
left adrenal gland cortex	UBERON:0035825	94.49	gold quality
right lung	UBERON:0002167	94.48	gold quality
right frontal lobe	UBERON:0002810	94.44	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	6.92
E-MTAB-6058	no	115.50

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

56 targeting CSNK1G2, 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-1252-5P	100.00	69.80	2774
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-4481	100.00	66.42	1669
HSA-MIR-103A-3P	99.98	69.14	1595
HSA-MIR-107	99.98	69.14	1595
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-6835-3P	99.93	70.49	2904
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-3686	99.90	70.53	2432
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-3919	99.87	69.45	2489
HSA-MIR-579-3P	99.86	71.66	3628
HSA-MIR-664B-3P	99.84	71.65	3590
HSA-MIR-4422	99.72	72.07	2908
HSA-MIR-3059-5P	99.70	69.93	2491
HSA-MIR-29B-2-5P	99.67	68.98	1726
HSA-MIR-3934-5P	99.67	64.04	846
HSA-MIR-6887-3P	99.66	67.83	1778
HSA-MIR-7157-5P	99.66	69.33	1829
HSA-MIR-6512-3P	99.65	66.07	1468
HSA-MIR-6720-5P	99.65	66.22	1459
HSA-MIR-4743-3P	99.62	68.12	2095
HSA-MIR-4516	99.61	67.78	3390
HSA-MIR-4310	99.59	68.84	2527
HSA-MIR-569	99.42	66.32	1009
HSA-MIR-135A-5P	99.36	71.85	1601
HSA-MIR-135B-5P	99.36	71.63	1613
HSA-MIR-155-5P	99.35	70.16	1509
HSA-MIR-4652-3P	99.33	70.02	2742

Literature-anchored findings (GeneRIF, showing 8)

• MTA1s interacts with CKI-gamma2, which can phosphorylate MTA1s in an antiestrogen-dependent manner.Estrogen stimulates CKI-gamma2. CKI-gamma2 phosphorylates and modulates the functions of MTA1s. (PMID:15077195)
• Data indicate that SNPs rs740423, rs2277737, rs1059684 of CSNK1G2 gene may contribute to familial febrile convulsions in children. (PMID:15300631)
• CK1epsilon and CK1gamma2 were found to bind to Per1 and to promote its degradation (PMID:15917222)
• Ligand-dependent ubiquitination of Smad3 is regulated by CK1g2, an inhibitor of TGF-beta signaling. (PMID:18794808)
• These results indicate that CKIgamma2 hyperphosphorylates the serine-repeat motif of CERT, thereby inactivating CERT and down-regulating the synthesis of sphingomyelin. (PMID:19005213)
• MicroRNA-155 regulates casein kinase 1 gamma 2: a potential pathogenetic role in chronic lymphocytic leukemia (PMID:28885613)
• IRS4, as a new substrate of CHIP, is negatively regulated by CK1gamma2 at the posttranslational level. (PMID:30026872)
• CSNK1G2 differently sensitizes tamoxifen-induced decrease in PI3K/AKT/mTOR/S6K and ERK signaling according to the estrogen receptor existence in breast cancer cells. (PMID:33861751)

Cross-species orthologs

67 orthologs

Organism	Symbol	Gene ID
danio_rerio	csnk1g2a	ENSDARG00000005458
danio_rerio	csnk1g2b	ENSDARG00000034056
mus_musculus	Csnk1g2	ENSMUSG00000003345
rattus_norvegicus	Csnk1g2	ENSRNOG00000018529
drosophila_melanogaster	gish	FBGN0250823
caenorhabditis_elegans		WBGENE00007049
caenorhabditis_elegans		WBGENE00007269
caenorhabditis_elegans		WBGENE00007305
caenorhabditis_elegans		WBGENE00007335
caenorhabditis_elegans		WBGENE00007448
caenorhabditis_elegans		WBGENE00007777
caenorhabditis_elegans		WBGENE00007791
caenorhabditis_elegans		WBGENE00008088
caenorhabditis_elegans		WBGENE00008423
caenorhabditis_elegans		WBGENE00008464
caenorhabditis_elegans	F10G8.2	WBGENE00008662
caenorhabditis_elegans		WBGENE00008883
caenorhabditis_elegans		WBGENE00009324
caenorhabditis_elegans		WBGENE00009402
caenorhabditis_elegans		WBGENE00010555
caenorhabditis_elegans		WBGENE00010692
caenorhabditis_elegans		WBGENE00010874
caenorhabditis_elegans		WBGENE00011283
caenorhabditis_elegans		WBGENE00012169
caenorhabditis_elegans		WBGENE00012637
caenorhabditis_elegans		WBGENE00012731
caenorhabditis_elegans		WBGENE00013868
caenorhabditis_elegans		WBGENE00014007
caenorhabditis_elegans		WBGENE00015893
caenorhabditis_elegans		WBGENE00016111
caenorhabditis_elegans	C34B2.3	WBGENE00016388
caenorhabditis_elegans		WBGENE00016513
caenorhabditis_elegans		WBGENE00016541
caenorhabditis_elegans		WBGENE00016673
caenorhabditis_elegans		WBGENE00016765
caenorhabditis_elegans	C55B7.10	WBGENE00016946
caenorhabditis_elegans		WBGENE00016963
caenorhabditis_elegans		WBGENE00017050
caenorhabditis_elegans		WBGENE00017714
caenorhabditis_elegans		WBGENE00017725
caenorhabditis_elegans		WBGENE00017803
caenorhabditis_elegans	F33D11.7	WBGENE00018004
caenorhabditis_elegans		WBGENE00018122
caenorhabditis_elegans		WBGENE00018123
caenorhabditis_elegans		WBGENE00018202
caenorhabditis_elegans		WBGENE00018203
caenorhabditis_elegans		WBGENE00018745
caenorhabditis_elegans		WBGENE00018839
caenorhabditis_elegans		WBGENE00019086
caenorhabditis_elegans		WBGENE00019119
caenorhabditis_elegans		WBGENE00019459
caenorhabditis_elegans		WBGENE00019556
caenorhabditis_elegans		WBGENE00019561
caenorhabditis_elegans		WBGENE00019562
caenorhabditis_elegans		WBGENE00019642
caenorhabditis_elegans	kin-35	WBGENE00019769
caenorhabditis_elegans		WBGENE00020071
caenorhabditis_elegans		WBGENE00020072
caenorhabditis_elegans		WBGENE00020223
caenorhabditis_elegans		WBGENE00020580
caenorhabditis_elegans	W09C3.1	WBGENE00021109
caenorhabditis_elegans	Y47G6A.13	WBGENE00021639
caenorhabditis_elegans	Y65B4A.9	WBGENE00022032
caenorhabditis_elegans		WBGENE00022102
caenorhabditis_elegans	Y71F9AL.2	WBGENE00022108
caenorhabditis_elegans		WBGENE00022705
caenorhabditis_elegans		WBGENE00022707

Paralogs (12): VRK2 (ENSG00000028116), CDC7 (ENSG00000097046), VRK1 (ENSG00000100749), VRK3 (ENSG00000105053), CSNK1A1 (ENSG00000113712), TTBK2 (ENSG00000128881), CSNK1D (ENSG00000141551), TTBK1 (ENSG00000146216), CSNK1G3 (ENSG00000151292), CSNK1G1 (ENSG00000169118), CSNK1A1L (ENSG00000180138), CSNK1E (ENSG00000213923)

Protein

Protein identifiers

Casein kinase I isoform gamma-2 — P78368 (reviewed: P78368)

All UniProt accessions (7): A0A087WWF5, A0A087WXD7, A0A087WZK4, P78368, K7EJC0, K7EP38, K7ESB6

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. Phosphorylates COL4A3BP/CERT, MTA1 and SMAD3. SMAD3 phosphorylation promotes its ligand-dependent ubiquitination and subsequent proteasome degradation, thus inhibiting SMAD3-mediated TGF-beta responses. Hyperphosphorylation of the serine-repeat motif of COL4A3BP/CERT leads to its inactivation by dissociation from the Golgi complex, thus down-regulating ER-to-Golgi transport of ceramide and sphingomyelin synthesis. Triggers PER1 proteasomal degradation probably through phosphorylation. Involved in brain development and vesicular trafficking and neurotransmitter releasing from small synaptic vesicles. Regulates fast synaptic transmission mediated by glutamate. Involved in regulation of reactive oxygen species (ROS) levels.

Subunit / interactions. Monomer. Interacts with MTA1 (short isoform) in the cytoplasm. Interacts with SMAD3. Interacts with DUOXA2.

Subcellular location. Cytoplasm. Cell cortex.

Tissue specificity. Testis.

Post-translational modifications. Autophosphorylated. Phosphorylated by aPKC which promotes dissociation from the cell cortex.

Activity regulation. Stimulated by estrogen. Repressed by 5-iodotubercidin (DB04604).

Domain organisation. The phospho-regulated basic and hydrophobic (PRBH) motif is sufficient and important for interaction with phospholipids permitting cortical localization. Phosphorylation of the PRBH motif by aPKC inhibits the association of the protein with the cortical membrane.

Similarity. Belongs to the protein kinase superfamily. CK1 Ser/Thr protein kinase family. Casein kinase I subfamily.

RefSeq proteins (1): NP_001310* (*=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 (49 total): helix 10, sequence variant 9, strand 9, turn 9, region of interest 3, compositionally biased region 3, binding site 2, chain 1, domain 1, sequence conflict 1, active site 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
2C47	X-RAY DIFFRACTION	2.4

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P78368-F1	80.30	0.70

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): 165 (proton acceptor)

Ligand- & substrate-binding residues (2): 75; 52–60

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
R-HSA-1660661	Sphingolipid de novo biosynthesis
R-HSA-4641262	Disassembly of the destruction complex and recruitment of AXIN to the membrane
R-HSA-1430728	Metabolism
R-HSA-162582	Signal Transduction
R-HSA-195721	Signaling by WNT
R-HSA-201681	TCF dependent signaling in response to WNT
R-HSA-428157	Sphingolipid metabolism
R-HSA-556833	Metabolism of lipids

MSigDB gene sets: 183 (showing top): KEGG_HEDGEHOG_SIGNALING_PATHWAY, AAGTCCA_MIR422B_MIR422A, GOBP_VESICLE_MEDIATED_TRANSPORT, GOBP_REGULATION_OF_WNT_SIGNALING_PATHWAY, CAGCTG_AP4_Q5, MORF_RAF1, GOBP_SPHINGOLIPID_METABOLIC_PROCESS, GOBP_CANONICAL_WNT_SIGNALING_PATHWAY, PID_FOXO_PATHWAY, GOBP_LIPID_METABOLIC_PROCESS, NRF2_Q4, GOBP_LIPID_BIOSYNTHETIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_CANONICAL_WNT_SIGNALING_PATHWAY, SPIELMAN_LYMPHOBLAST_EUROPEAN_VS_ASIAN_UP, REACTOME_SPHINGOLIPID_METABOLISM

GO Biological Process (6): protein phosphorylation (GO:0006468), endocytosis (GO:0006897), signal transduction (GO:0007165), Wnt signaling pathway (GO:0016055), sphingolipid biosynthetic process (GO:0030148), positive regulation of canonical Wnt signaling pathway (GO:0090263)

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

GO Cellular Component (6): nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), cell cortex (GO:0005938), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-6 pathways:

Category	Pathways
Sphingolipid metabolism	1
TCF dependent signaling in response to WNT	1
Signal Transduction	1
Signaling by WNT	1
Metabolism of lipids	1
Metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
protein kinase activity	2
cytoplasm	2
cell periphery	2
phosphorylation	1
protein modification process	1
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
sphingolipid metabolic process	1
lipid biosynthetic process	1
positive regulation of Wnt signaling pathway	1
canonical Wnt signaling pathway	1
regulation of canonical Wnt signaling pathway	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
intracellular membrane-bounded organelle	1
intracellular anatomical structure	1
membrane	1

Protein interactions and networks

STRING

1097 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CSNK1G2	NCK1	P16333	507
CSNK1G2	LRP6	O75581	467
CSNK1G2	AXIN1	O15169	440
CSNK1G2	LRP8	Q14114	432
CSNK1G2	VARS2	Q5ST30	413
CSNK1G2	WNT2	P09544	406
CSNK1G2	VARS1	P26640	405
CSNK1G2	SOD3	P08294	388
CSNK1G2	CSNK1G1	Q9HCP0	388
CSNK1G2	MGP	P08493	384
CSNK1G2	CERT1	Q9Y5P4	376
CSNK1G2	RPL14	P50914	335
CSNK1G2	ZMYND8	Q9ULU4	334
CSNK1G2	CTNNA2	P26232	319
CSNK1G2	NEO1	Q92859	305

IntAct

66 interactions, top by confidence:

A	B	Type	Score
CERT1	CSNK1G2	psi-mi:“MI:0915”(physical association)	0.800
CSNK1G2	CERT1	psi-mi:“MI:0915”(physical association)	0.800
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
CSNK1G2	CERT1	psi-mi:“MI:0915”(physical association)	0.670
CSNK1G1	CSNK1G2	psi-mi:“MI:0915”(physical association)	0.670
KCNJ2	KCNJ18	psi-mi:“MI:2364”(proximity)	0.660
CSNK1G3	CSNK1G2	psi-mi:“MI:0914”(association)	0.640
KRTAP10-7	CSNK1G2	psi-mi:“MI:0915”(physical association)	0.560
CSNK1G2	APPBP2	psi-mi:“MI:0915”(physical association)	0.560
CSNK1G2	RUNDC3B	psi-mi:“MI:0915”(physical association)	0.550
G3BP1	COX5A	psi-mi:“MI:0914”(association)	0.530
CSNK1G2	GINS1	psi-mi:“MI:0914”(association)	0.530
MRAP2	GOLIM4	psi-mi:“MI:0914”(association)	0.530
CSNK1G2	MAPK14	psi-mi:“MI:0914”(association)	0.530
LRRK2	CSNK1G2	psi-mi:“MI:0217”(phosphorylation reaction)	0.440
	CSNK1G2	psi-mi:“MI:0407”(direct interaction)	0.440
CSNK1G2	ERAP1	psi-mi:“MI:0915”(physical association)	0.400
CSNK1G1	CSNK1G2	psi-mi:“MI:0915”(physical association)	0.400
GPC1	SNAP23	psi-mi:“MI:0915”(physical association)	0.400
GPC1	GANAB	psi-mi:“MI:0915”(physical association)	0.400
WDCP	CSNK1G2	psi-mi:“MI:0915”(physical association)	0.370
CSNK1G2	RAP1GAP	psi-mi:“MI:0915”(physical association)	0.370
ATL2	ACRBP	psi-mi:“MI:0914”(association)	0.350

BioGRID (159): COL4A3BP (Two-hybrid), APPBP2 (Two-hybrid), KRTAP10-7 (Two-hybrid), CSNK1G2 (Affinity Capture-MS), CSNK1G2 (Affinity Capture-MS), CSNK1G2 (Affinity Capture-MS), CSNK1G2 (Affinity Capture-MS), CSNK1G2 (Affinity Capture-MS), COL4A3BP (Two-hybrid), CSNK1G2 (Affinity Capture-MS), CSNK1G2 (Affinity Capture-MS), CSNK1G2 (Affinity Capture-MS), CSNK1G2 (Affinity Capture-MS), CSNK1G3 (Affinity Capture-MS), CSNK1G2 (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

6 interactions.

A	Effect	B	Mechanism
CSNK1G2	down-regulates	PER1	phosphorylation
CSNK1G2	down-regulates	SMAD3	phosphorylation
CSNK1G2	down-regulates	CERT1	phosphorylation
CSNK1G2	“up-regulates quantity by stabilization”	LYN	phosphorylation
CSNK1G2	“down-regulates quantity by destabilization”	IRS4	phosphorylation
CSNK1G2	“up-regulates activity”	MTA1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 69 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.

GO biological processes:

GO term	Partners	Fold	FDR
endocytosis	6	9.8×	8e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	37
Likely benign	4
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

2220 predictions. Top by Δscore:

Variant	Effect	Δscore
19:1978303:A:AG	acceptor_gain	1.0000
19:1978304:G:GG	acceptor_gain	1.0000
19:1978437:CCCAG:C	acceptor_loss	1.0000
19:1978439:CA:C	acceptor_loss	1.0000
19:1978440:A:AG	acceptor_gain	1.0000
19:1978440:AG:A	acceptor_gain	1.0000
19:1978441:G:A	acceptor_loss	1.0000
19:1978441:G:GT	acceptor_gain	1.0000
19:1978441:GG:G	acceptor_gain	1.0000
19:1978441:GGA:G	acceptor_gain	1.0000
19:1978441:GGAGC:G	acceptor_gain	1.0000
19:1978513:T:A	donor_loss	1.0000
19:1978636:C:CA	acceptor_gain	1.0000
19:1978637:G:A	acceptor_gain	1.0000
19:1978747:GCTG:G	donor_gain	1.0000
19:1978751:G:GG	donor_gain	1.0000
19:1978751:GTGC:G	donor_loss	1.0000
19:1978752:T:G	donor_loss	1.0000
19:1978854:TGCA:T	acceptor_loss	1.0000
19:1978856:CAGAT:C	acceptor_loss	1.0000
19:1978857:A:AG	acceptor_gain	1.0000
19:1978857:AGAT:A	acceptor_loss	1.0000
19:1978858:G:GC	acceptor_gain	1.0000
19:1978858:GA:G	acceptor_gain	1.0000
19:1978858:GAT:G	acceptor_gain	1.0000
19:1978858:GATC:G	acceptor_gain	1.0000
19:1978858:GATCA:G	acceptor_gain	1.0000
19:1979092:GG:G	donor_gain	1.0000
19:1979093:GG:G	donor_gain	1.0000
19:1979402:AGGT:A	donor_loss	1.0000

AlphaMissense

2734 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:1969899:G:C	G43R	1.000
19:1969900:G:A	G43D	1.000
19:1969900:G:T	G43V	1.000
19:1969908:T:C	F46L	1.000
19:1969909:T:C	F46S	1.000
19:1969909:T:G	F46C	1.000
19:1969910:C:A	F46L	1.000
19:1969910:C:G	F46L	1.000
19:1969915:T:A	V48D	1.000
19:1969927:T:A	I52N	1.000
19:1969929:G:C	G53R	1.000
19:1969930:G:A	G53D	1.000
19:1969930:G:T	G53V	1.000
19:1969935:G:A	G55S	1.000
19:1969935:G:C	G55R	1.000
19:1969935:G:T	G55C	1.000
19:1969936:G:A	G55D	1.000
19:1969936:G:C	G55A	1.000
19:1969936:G:T	G55V	1.000
19:1969940:C:A	N56K	1.000
19:1969940:C:G	N56K	1.000
19:1969941:T:A	F57I	1.000
19:1969941:T:C	F57L	1.000
19:1969941:T:G	F57V	1.000
19:1969942:T:C	F57S	1.000
19:1969942:T:G	F57C	1.000
19:1969943:C:A	F57L	1.000
19:1969943:C:G	F57L	1.000
19:1969944:G:A	G58R	1.000
19:1969944:G:C	G58R	1.000

dbSNP variants (sampled 300 via entrez): RS1000019331 (19:1953753 C>G), RS1000085525 (19:1980937 C>A,T), RS1000107196 (19:1953597 G>A), RS1000117357 (19:1975069 G>A), RS1000145273 (19:1957052 C>A,T), RS1000164311 (19:1950156 A>G,T), RS1000188421 (19:1964732 T>C), RS1000199655 (19:1964842 C>T), RS1000262837 (19:1976705 C>G), RS1000313344 (19:1962736 A>C,G), RS1000329042 (19:1942775 G>A), RS1000344547 (19:1942599 G>A,C), RS1000345091 (19:1946481 C>G,T), RS1000362370 (19:1946797 C>A,G,T), RS1000377914 (19:1943158 T>G)

Disease associations

OMIM: gene MIM:602214 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

8 associations (top):

Study	Trait	p-value
GCST002783_448	Body mass index	1.000000e-07
GCST002783_485	Body mass index	3.000000e-07
GCST002783_9	Body mass index	2.000000e-06
GCST004621_204	Red cell distribution width	2.000000e-09
GCST005194_63	Coronary artery disease	8.000000e-06
GCST012245_2	Periodontitis (stage III/IV grade C)	2.000000e-06
GCST90002404_550	Red cell distribution width	1.000000e-15
GCST90026413_10	Severe insulin-deficient type 2 diabetes	9.000000e-06

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004340	body mass index
EFO:0009188	Red cell distribution width

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2111458 (PROTEIN FAMILY), CHEMBL2543 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

22 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 126,530 (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
CHEMBL1738797	ALECTINIB	4	6,731
CHEMBL180022	NERATINIB	4	9,404
CHEMBL2105759	BARICITINIB	4	6,741
CHEMBL535	SUNITINIB	4	79,020
CHEMBL223360	LINIFANIB	3	3,925
CHEMBL31965	CANERTINIB	3	8,083
CHEMBL1230165	SILMITASERTIB	2	593
CHEMBL14762	SELICICLIB	2	3,787
CHEMBL1614713	CC-401	2	389
CHEMBL1721885	SU-014813	2	363
CHEMBL1967878	CENISERTIB	2	358
CHEMBL1980297	ILORASERTIB	2	581
CHEMBL230011	TG100-115	2	1,504
CHEMBL363648	TAK-715	2	442
CHEMBL4462530	ZEMIRCICLIB	2	429
CHEMBL513909	BI-2536	2	895
CHEMBL1084546	PF-00562271	1	399
CHEMBL1908397	KW-2449	1	622
CHEMBL3544966	GSK-1059615	1	1,928
CHEMBL482767	SNS-314	1	336
CHEMBL482967	CYC-116	1
CHEMBL574738	AST-487	1

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 (2 total), top 2:

Ligand	Action	Affinity	Parameter
compound 14 [PMID: 24900428]	Inhibition	8.52	pIC50
SGC-CK1γ-1	Inhibition	6.74	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
Staurosporine	KD	1.7 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

320 potent at pChembl≥5 of 331 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.52	IC50	3	nM	CHEMBL2203564
8.52	IC50	3	nM	CHEMBL2203562
8.40	IC50	4	nM	CHEMBL2203565
8.40	IC50	4	nM	SILMITASERTIB
8.40	Ki	3.981	nM	CHEMBL1997129
8.40	Ki	3.981	nM	CHEMBL2003638
8.30	IC50	5	nM	CHEMBL2203563
8.30	IC50	5	nM	CHEMBL2203561
8.20	Ki	6.31	nM	CHEMBL1991078
8.20	Ki	6.31	nM	CHEMBL1969588
8.10	IC50	8	nM	CHEMBL2203556
8.10	IC50	8	nM	CHEMBL2203552
8.10	Ki	7.943	nM	CHEMBL1999931
7.77	IC50	17	nM	CHEMBL2203554
7.70	Ki	19.95	nM	CHEMBL1977223
7.62	IC50	24	nM	CHEMBL2203559
7.60	Ki	25.12	nM	CHEMBL1965660
7.60	Ki	25.12	nM	CHEMBL1996066
7.58	IC50	26	nM	CHEMBL2203560
7.50	Ki	31.62	nM	CHEMBL1989646
7.50	Ki	31.62	nM	CHEMBL1965631
7.48	IC50	33	nM	CHEMBL2203555
7.46	IC50	35	nM	HYMENIALDISINE
7.40	Ki	39.81	nM	CHEMBL1981079
7.40	Ki	39.81	nM	CHEMBL2006439
7.40	Ki	39.81	nM	CHEMBL1994830
7.36	IC50	44	nM	CHEMBL2203565
7.34	Kd	46	nM	CHEMBL3688339
7.30	IC50	50	nM	CHEMBL2203553
7.30	Ki	50.12	nM	CHEMBL396523
7.30	Ki	50.12	nM	CHEMBL1992937
7.20	Ki	63.1	nM	CHEMBL1964290
7.20	Ki	63.1	nM	CHEMBL1986263
7.20	Ki	63.1	nM	CHEMBL225519
7.20	Ki	63.1	nM	CHEMBL1969523
7.10	IC50	80	nM	CHEMBL2203557
7.10	Ki	79.43	nM	CHEMBL1974870
7.10	Ki	79.43	nM	CHEMBL243088
7.06	IC50	87	nM	CHEMBL2203565
7.06	Kd	86.66	nM	CHEMBL3752910
7.00	Kd	100	nM	CHEMBL1349996
7.00	ED50	99	nM	CHEMBL3752910
7.00	Ki	100	nM	CHEMBL244378
7.00	Ki	100	nM	CHEMBL1969843
6.98	Kd	105	nM	CC-401
6.96	Kd	110	nM	SUNITINIB
6.90	Ki	125.9	nM	CHEMBL1975128
6.90	Ki	125.9	nM	CHEMBL1991063
6.80	Ki	158.5	nM	CHEMBL1966628
6.80	Ki	158.5	nM	CHEMBL1998159

PubChem BioAssay actives

82 with measured affinity, of 1207 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-[2-[(4-fluoro-2-methylphenoxy)methyl]-5-methoxy-4-pyridinyl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0030	uM
2-[2-[(2,4-difluorophenoxy)methyl]-5-methoxy-4-pyridinyl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0030	uM
5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid	1831537: Inhibition of CK1 (unknown origin)	ic50	0.0040	uM
2-[2-[(4,5-difluoro-2-methylphenoxy)methyl]-5-methoxy-4-pyridinyl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0040	uM
2-[2-[(3,4-difluorophenoxy)methyl]-5-methoxy-4-pyridinyl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0050	uM
2-[2-[(4-fluorophenoxy)methyl]-5-methoxy-4-pyridinyl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0050	uM
2-(5-methoxy-2-quinolin-3-ylpyrimidin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0080	uM
2-(2-anilino-5-methoxypyrimidin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0080	uM
2-[2-[2-(4-fluorophenyl)ethyl]-5-methoxypyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0170	uM
2-[2-[(4-fluorophenoxy)methyl]-5-methoxypyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0240	uM
2-[2-[2-(4-fluorophenyl)ethyl]-5-methoxy-4-pyridinyl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0260	uM
2-[2-(benzylamino)-5-methoxypyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0330	uM
(4Z)-4-(2-amino-5-oxo-1H-imidazol-4-ylidene)-2-bromo-1,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one	1924344: Inhibition of CK1 (unknown origin)	ic50	0.0350	uM
1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone	1424965: 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	0.0460	uM
2-[2-[(E)-2-(4-fluorophenyl)ethenyl]-5-methoxypyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0500	uM
2-[2-[(4-fluorophenyl)methoxy]-5-methoxypyrimidin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.0800	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148161: Binding affinity to human CSNK1G2 incubated for 45 mins by Kinobead based pull down assay	kd	0.0867	uM
(1E)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one	1722614: Binding affinity to CSNK1G2 (unknown origin)	kd	0.1000	uM
3-[3-(2-piperidin-1-ylethoxy)phenyl]-5-(1H-1,2,4-triazol-5-yl)-1H-indazole	1424965: 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	0.1050	uM
Sunitinib	435282: Binding constant for full-length CSNK1G2	kd	0.1100	uM
N-[3-chloro-4-(4-methylpiperazin-1-yl)phenyl]-2-[4-(5,7-dimethoxy-4-oxo-3H-quinazolin-2-yl)phenoxy]acetamide	1831537: Inhibition of CK1 (unknown origin)	ic50	0.2300	uM
Baricitinib	1424965: 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	0.2650	uM
(1Z)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one	445573: Binding affinity to CSNK1G2 assessed as dissociation constant	kd	0.2700	uM
4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide	1539768: Inhibition of human CK1 in presence of [gamma33P]-ATP	ic50	0.3000	uM
(2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine	624833: Binding constant for CSNK1G2 kinase domain	kd	0.3800	uM
Alectinib	1424965: 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	0.5140	uM
4-[[5-amino-1-(3-methylthiophene-2-carbonyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide	240570: Inhibition of casein kinase-1	ic50	0.5700	uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone	624833: Binding constant for CSNK1G2 kinase domain	kd	0.5800	uM
2-[4-(2-hydroxypropan-2-yl)anilino]-3H-benzimidazole-5-carbonitrile	678165: Inhibition of CK1gamma2 expressed in HEK293 cells assessed as inhibition of LRP6 Thr1479 phosphorylation by immunoblotting	ic50	0.7000	uM
4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide	435282: Binding constant for full-length CSNK1G2	kd	0.7400	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	435282: Binding constant for full-length CSNK1G2	kd	0.7800	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	435282: Binding constant for full-length CSNK1G2	kd	0.7900	uM
2-(5-methoxy-2-phenoxypyrimidin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one	712793: Inhibition of CK1-gamma 2 using biotin[long chain]-KKRRRAL{pS}VATLPGL substrate in presence of 32 uM ATP	ic50	0.8530	uM
1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea	435282: Binding constant for full-length CSNK1G2	kd	0.9500	uM
(5Z)-5-[(4-pyridin-4-ylquinolin-6-yl)methylidene]-1,3-thiazolidine-2,4-dione	1424965: 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	0.9680	uM
3-(2-aminopyrimidin-4-yl)-6-bromo-1H-indol-4-ol	49209: Inhibition of Casein kinase I (CK1)	ic50	1.0000	uM
2-[4-(2-fluoro-3-pyridinyl)anilino]-3H-benzimidazole-5-carbonitrile	678165: Inhibition of CK1gamma2 expressed in HEK293 cells assessed as inhibition of LRP6 Thr1479 phosphorylation by immunoblotting	ic50	1.1700	uM
(2R)-2-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol	256634: Average Binding Constant for CSNK1G2; NA=Not Active at 10 uM	kd	1.4000	uM
2-[4-(1-methylpyrazol-4-yl)anilino]-3H-benzimidazole-5-carbonitrile	678165: Inhibition of CK1gamma2 expressed in HEK293 cells assessed as inhibition of LRP6 Thr1479 phosphorylation by immunoblotting	ic50	1.4500	uM
2-(4-tert-butylanilino)-3H-benzimidazole-5-carbonitrile	678165: Inhibition of CK1gamma2 expressed in HEK293 cells assessed as inhibition of LRP6 Thr1479 phosphorylation by immunoblotting	ic50	1.5100	uM
N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]methanesulfonamide	1424965: 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	1.7110	uM
N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide	1424965: 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	1.8620	uM
N-(4-tert-butylphenyl)-6-nitro-1H-benzimidazol-2-amine	678165: Inhibition of CK1gamma2 expressed in HEK293 cells assessed as inhibition of LRP6 Thr1479 phosphorylation by immunoblotting	ic50	2.3400	uM
3-[2,4-diamino-7-(3-hydroxyphenyl)pteridin-6-yl]phenol	624833: Binding constant for CSNK1G2 kinase domain	kd	2.4000	uM
5-amino-N-(2,6-difluorophenyl)-3-(4-sulfamoylanilino)-1,2,4-triazole-1-carbothioamide	240570: Inhibition of casein kinase-1	ic50	2.8000	uM
2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol	624833: Binding constant for CSNK1G2 kinase domain	kd	3.0000	uM
3-[[4-[4-(3-chloroanilino)-1,3,5-triazin-2-yl]-2-pyridinyl]amino]propan-1-ol	240612: Inhibition of Casein kinase I	ic50	3.0500	uM
2-(4-tert-butylanilino)-1,3-benzothiazole-6-carbonitrile	678165: Inhibition of CK1gamma2 expressed in HEK293 cells assessed as inhibition of LRP6 Thr1479 phosphorylation by immunoblotting	ic50	3.8300	uM
N-[3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl]propane-1-sulfonamide	624833: Binding constant for CSNK1G2 kinase domain	kd	4.1000	uM
(5Z)-5-(2-bromo-8-oxo-1,5,6,7-tetrahydropyrrolo[2,3-c]azepin-4-ylidene)imidazolidine-2,4-dione	1924344: Inhibition of CK1 (unknown origin)	ic50	4.5000	uM

CTD chemical–gene interactions

29 total (human), top 29 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
methylmercuric chloride	increases expression, affects cotreatment	3
sodium arsenite	decreases expression, increases expression	2
Hydrogen Peroxide	affects expression, decreases expression	2
FR900359	increases phosphorylation	1
bisphenol F	increases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases methylation	1
methylparaben	increases expression	1
benzo(e)pyrene	decreases methylation	1
4-hydroxy-2-nonenal	decreases expression	1
aflatoxin B2	decreases methylation	1
cupric chloride	increases expression	1
di-n-butylphosphoric acid	affects expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
dorsomorphin	affects cotreatment, increases expression	1
Resveratrol	increases expression, affects cotreatment	1
Sunitinib	increases expression	1
Air Pollutants	affects expression, increases abundance	1
Arsenic	affects methylation	1
Benzo(a)pyrene	increases methylation	1
Doxorubicin	decreases expression	1
Lipopolysaccharides	affects expression, affects response to substance	1
Methapyrilene	decreases methylation	1
Ozone	affects expression, increases abundance	1
Plant Extracts	increases expression, affects cotreatment	1
Smoke	decreases expression	1
Thiram	decreases expression	1
Valproic Acid	increases methylation	1
Vitamin E	decreases expression	1

ChEMBL screening assays

316 unique, capped per target: 315 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1051274	Binding	Percent residual CK1 activity in the presence of 10uM inhibitor	Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). — Biochem J
CHEMBL1963686	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: CSNK1G2	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_D7MZ	Ubigene A-549 CSNK1G2 KO	Cancer cell line	Male
CVCL_D8JG	Ubigene HCT 116 CSNK1G2 KO	Cancer cell line	Male
CVCL_D9CH	Ubigene HEK293 CSNK1G2 KO	Transformed cell line	Female
CVCL_E0B6	Ubigene HeLa CSNK1G2 KO	Cancer cell line	Female
CVCL_SJ87	HAP1 CSNK1G2 (-) 1	Cancer cell line	Male
CVCL_SJ88	HAP1 CSNK1G2 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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