CSNK1A1L

gene
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Also known as MGC33182

Summary

CSNK1A1L (casein kinase 1 alpha 1 like, HGNC:20289) is a protein-coding gene on chromosome 13q13.3, encoding Casein kinase I isoform alpha-like (Q8N752). Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates.

Predicted to enable protein serine/threonine kinase activity. Predicted to be involved in negative regulation of canonical Wnt signaling pathway and signal transduction. Predicted to be active in cytoplasm and nucleus.

Source: NCBI Gene 122011 — RefSeq curated summary.

At a glance

  • GWAS associations: 3
  • Clinical variants (ClinVar): 56 total — 1 pathogenic
  • Druggable target: yes — 7 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_145203

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:20289
Approved symbolCSNK1A1L
Namecasein kinase 1 alpha 1 like
Location13q13.3
Locus typegene with protein product
StatusApproved
AliasesMGC33182
Ensembl geneENSG00000180138
Ensembl biotypeprotein_coding
Entrez122011

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000379800

RefSeq mRNA: 1 — MANE Select: NM_145203 NM_145203

CCDS: CCDS9363

Canonical transcript exons

ENST00000379800 — 1 exons

ExonStartEnd
ENSE000014825413710325937105664

Expression profiles

Bgee: expression breadth broad, 17 present calls, max score 81.47.

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099181.47gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047374.13gold quality
bloodUBERON:000017866.11gold quality
right testisUBERON:000453459.50gold quality
testisUBERON:000047358.03gold quality
bone marrow cellCL:000209257.50silver quality
left testisUBERON:000453357.25gold quality
bone marrowUBERON:000237155.43gold quality
cortical plateUBERON:000534353.04gold quality
ventricular zoneUBERON:000305347.92silver quality
granulocyteCL:000009444.41silver quality
sural nerveUBERON:001548842.44gold quality
spleenUBERON:000210642.01silver quality
colonic epitheliumUBERON:000039741.30gold quality
vermiform appendixUBERON:000115440.07silver quality
skeletal muscle tissueUBERON:000113439.17gold quality
stromal cell of endometriumCL:000225538.94gold quality
right lungUBERON:000216738.80silver quality
gall bladderUBERON:000211038.63gold quality
apex of heartUBERON:000209837.58silver quality
muscle tissueUBERON:000238536.42gold quality
liverUBERON:000210736.31gold quality
urinary bladderUBERON:000125535.93gold quality
monocyteCL:000057635.65gold quality
placentaUBERON:000198734.32gold quality
lungUBERON:000204833.86silver quality
upper lobe of left lungUBERON:000895233.61silver quality
fundus of stomachUBERON:000116033.32gold quality
corpus callosumUBERON:000233632.93gold quality
endometriumUBERON:000129532.91gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

ExperimentMarker?Max mean expression
E-ANND-3no2.17

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

63 targeting CSNK1A1L, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-513A-5P100.0069.772465
HSA-MIR-223-3P99.9970.141140
HSA-MIR-371B-5P99.9975.344759
HSA-MIR-428299.9975.366408
HSA-MIR-513B-5P99.9969.962150
HSA-MIR-1213699.9872.815713
HSA-MIR-373-5P99.9875.364753
HSA-MIR-616-5P99.9875.584775
HSA-MIR-493-5P99.9672.472382
HSA-MIR-211099.9666.681930
HSA-MIR-391099.9571.132227
HSA-MIR-806399.9169.763146
HSA-MIR-7-1-3P99.9171.534384
HSA-MIR-7-2-3P99.9171.404394
HSA-MIR-652-5P99.9167.49505
HSA-MIR-6857-5P99.8765.32985
HSA-MIR-659-3P99.8570.691620
HSA-MIR-60999.8264.26505
HSA-MIR-3150A-3P99.7664.441640
HSA-MIR-6763-5P99.7664.681767
HSA-MIR-467999.7669.191229
HSA-MIR-5580-3P99.7069.412052
HSA-MIR-317599.6566.302031
HSA-MIR-6516-3P99.6568.571238
HSA-MIR-561-3P99.6470.903647
HSA-MIR-368599.6268.831621
HSA-MIR-3942-3P99.5769.032854
HSA-MIR-4708-3P99.5167.99870
HSA-MIR-4677-3P99.4967.911246

Literature-anchored findings (GeneRIF, showing 1)

  • Casein kinase 1 controls the shuttling of epidermal growth factor receptor and estrogen receptor in endometrial carcinoma induced by breast cancer hormonal therapy: Relevance of GPER1/Src. (PMID:37257767)

Cross-species orthologs

69 orthologs

OrganismSymbolGene ID
danio_reriottbk2aENSDARG00000005670
danio_reriottbk2bENSDARG00000043026
danio_reriottbk1aENSDARG00000056019
danio_reriottbk1bENSDARG00000056659
drosophila_melanogasterballFBGN0027889
drosophila_melanogasterCG9962FBGN0031441
caenorhabditis_elegansWBGENE00007049
caenorhabditis_elegansWBGENE00007269
caenorhabditis_elegansWBGENE00007305
caenorhabditis_elegansWBGENE00007335
caenorhabditis_elegansWBGENE00007448
caenorhabditis_elegansWBGENE00007777
caenorhabditis_elegansWBGENE00007791
caenorhabditis_elegansWBGENE00008088
caenorhabditis_elegansWBGENE00008423
caenorhabditis_elegansWBGENE00008464
caenorhabditis_elegansF10G8.2WBGENE00008662
caenorhabditis_elegansWBGENE00008883
caenorhabditis_elegansWBGENE00009324
caenorhabditis_elegansWBGENE00009402
caenorhabditis_elegansWBGENE00010555
caenorhabditis_elegansWBGENE00010692
caenorhabditis_elegansWBGENE00010874
caenorhabditis_elegansWBGENE00011283
caenorhabditis_elegansWBGENE00012169
caenorhabditis_elegansWBGENE00012637
caenorhabditis_elegansWBGENE00012731
caenorhabditis_elegansWBGENE00013868
caenorhabditis_elegansWBGENE00014007
caenorhabditis_elegansWBGENE00015893
caenorhabditis_elegansWBGENE00016111
caenorhabditis_elegansC34B2.3WBGENE00016388
caenorhabditis_elegansWBGENE00016513
caenorhabditis_elegansWBGENE00016541
caenorhabditis_elegansWBGENE00016673
caenorhabditis_elegansWBGENE00016765
caenorhabditis_elegansC55B7.10WBGENE00016946
caenorhabditis_elegansWBGENE00016963
caenorhabditis_elegansWBGENE00017050
caenorhabditis_elegansWBGENE00017714
caenorhabditis_elegansWBGENE00017725
caenorhabditis_elegansWBGENE00017803
caenorhabditis_elegansWBGENE00017895
caenorhabditis_elegansF33D11.7WBGENE00018004
caenorhabditis_elegansWBGENE00018122
caenorhabditis_elegansWBGENE00018123
caenorhabditis_elegansWBGENE00018202
caenorhabditis_elegansWBGENE00018203
caenorhabditis_elegansWBGENE00018745
caenorhabditis_elegansWBGENE00018839
caenorhabditis_elegansWBGENE00019086
caenorhabditis_elegansWBGENE00019119
caenorhabditis_elegansWBGENE00019459
caenorhabditis_elegansWBGENE00019556
caenorhabditis_elegansWBGENE00019561
caenorhabditis_elegansWBGENE00019562
caenorhabditis_elegansWBGENE00019642
caenorhabditis_eleganskin-35WBGENE00019769
caenorhabditis_elegansWBGENE00020071
caenorhabditis_elegansWBGENE00020072
caenorhabditis_elegansWBGENE00020223
caenorhabditis_elegansWBGENE00020580
caenorhabditis_elegansW09C3.1WBGENE00021109
caenorhabditis_elegansY47G6A.13WBGENE00021639
caenorhabditis_elegansY65B4A.9WBGENE00022032
caenorhabditis_elegansWBGENE00022102
caenorhabditis_elegansY71F9AL.2WBGENE00022108
caenorhabditis_elegansWBGENE00022705
caenorhabditis_elegansWBGENE00022707

Paralogs (12): VRK2 (ENSG00000028116), CDC7 (ENSG00000097046), VRK1 (ENSG00000100749), VRK3 (ENSG00000105053), CSNK1A1 (ENSG00000113712), TTBK2 (ENSG00000128881), CSNK1G2 (ENSG00000133275), CSNK1D (ENSG00000141551), TTBK1 (ENSG00000146216), CSNK1G3 (ENSG00000151292), CSNK1G1 (ENSG00000169118), CSNK1E (ENSG00000213923)

Protein

Protein identifiers

Casein kinase I isoform alpha-likeQ8N752 (reviewed: Q8N752)

Alternative names: CK1

All UniProt accessions (1): Q8N752

UniProt curated annotations — full annotation on UniProt →

Function. 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.

Subunit / interactions. Interacts with FAM83A, FAM83B, FAM83C, FAM83D, FAM83E, FAM83F, FAM83G and FAM83H (via DUF1669).

Subcellular location. Cytoplasm.

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

RefSeq proteins (1): NP_660204* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000719Prot_kinase_domDomain
IPR008271Ser/Thr_kinase_ASActive_site
IPR011009Kinase-like_dom_sfHomologous_superfamily
IPR017441Protein_kinase_ATP_BSBinding_site
IPR050235CK1_Ser-Thr_kinase-likeFamily

Pfam: PF00069

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 (19 total): sequence variant 9, compositionally biased region 2, binding site 2, chain 1, domain 1, sequence conflict 1, region of interest 1, active site 1, modified residue 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q8N752-F192.060.88

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): 136 (proton acceptor)

Ligand- & substrate-binding residues (2): 23–31; 46

Post-translational modifications (1): 8

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 61 (showing top): KEGG_HEDGEHOG_SIGNALING_PATHWAY, GOBP_REGULATION_OF_WNT_SIGNALING_PATHWAY, chr13q13, CATTTCA_MIR203, GOBP_CANONICAL_WNT_SIGNALING_PATHWAY, AACTTT_UNKNOWN, HNF1_01, ACEVEDO_METHYLATED_IN_LIVER_CANCER_DN, GOBP_NEGATIVE_REGULATION_OF_WNT_SIGNALING_PATHWAY, HOXA4_Q2, YNGTTNNNATT_UNKNOWN, CP2_01, GCCATNTTG_YY1_Q6, ATGTACA_MIR493, WGTTNNNNNAAA_UNKNOWN

GO Biological Process (4): signal transduction (GO:0007165), Wnt signaling pathway (GO:0016055), negative regulation of canonical Wnt signaling pathway (GO:0090090), protein phosphorylation (GO:0006468)

GO Molecular Function (7): 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), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (2): nucleus (GO:0005634), cytoplasm (GO:0005737)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
protein kinase activity2
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
cell surface receptor signaling pathway1
negative regulation of Wnt signaling pathway1
canonical Wnt signaling pathway1
regulation of canonical Wnt signaling pathway1
phosphorylation1
protein modification process1
adenyl ribonucleotide binding1
purine ribonucleoside triphosphate binding1
nucleoside phosphate binding1
heterocyclic compound binding1
kinase activity1
phosphotransferase activity, alcohol group as acceptor1
catalytic activity, acting on a protein1
transferase activity, transferring phosphorus-containing groups1
catalytic activity1
intracellular membrane-bounded organelle1
intracellular anatomical structure1
cellular anatomical structure1

Protein interactions and networks

STRING

550 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
CSNK1A1LAXIN2Q9Y2T1476
CSNK1A1LCSNK1A1P48729423
CSNK1A1LALPK3Q96L96380
CSNK1A1LNPIPB9F8W1W9377
CSNK1A1LGSK3BP49841375
CSNK1A1LPSKH2Q96QS6371
CSNK1A1LPROSER1Q86XN7365
CSNK1A1LUEVLDQ8IX04353
CSNK1A1LCCDC169A6NNP5348
CSNK1A1LMTRNR2L10P0CJ77348
CSNK1A1LAXIN1O15169341
CSNK1A1LFAM25AB3EWG3325
CSNK1A1LWNT8AQ9H1J5302
CSNK1A1LNHLRC3Q5JS37301
CSNK1A1LPSKH1P11801289

IntAct

34 interactions, top by confidence:

ABTypeScore
FAM83HCSNK1A1psi-mi:“MI:0914”(association)0.920
FAM83GCSNK1A1psi-mi:“MI:0914”(association)0.900
CSNK1A1FAM83Gpsi-mi:“MI:0914”(association)0.900
FAM83BCSNK1A1psi-mi:“MI:0914”(association)0.800
NCKIPSDGEMIN2psi-mi:“MI:0914”(association)0.640
FAM83CCSNK1A1psi-mi:“MI:0914”(association)0.610
FAM83DHMMRpsi-mi:“MI:0914”(association)0.560
FAM83ECSNK1A1psi-mi:“MI:0914”(association)0.540
FAM83FCSNK1A1psi-mi:“MI:0914”(association)0.540
VCAM1PSMD11psi-mi:“MI:0914”(association)0.530
FAM83ACSNK1A1psi-mi:“MI:0914”(association)0.430
Cbx1FLOT1psi-mi:“MI:0915”(physical association)0.400
CEBPECSNK1A1Lpsi-mi:“MI:0915”(physical association)0.370
JAM2CSNK1A1Lpsi-mi:“MI:0915”(physical association)0.370
JUNTPM3psi-mi:“MI:0914”(association)0.350
EGFRpsi-mi:“MI:0914”(association)0.350
SGK1psi-mi:“MI:0914”(association)0.350
HSCBRBP5psi-mi:“MI:0914”(association)0.350
ARRB2psi-mi:“MI:0914”(association)0.350
FAM170ANDC80psi-mi:“MI:0914”(association)0.350
PXNPIK3C2Apsi-mi:“MI:0914”(association)0.350
PRKD1psi-mi:“MI:0914”(association)0.350
CSNK1A1LPLEKHG3psi-mi:“MI:0914”(association)0.350

BioGRID (71): CSNK1A1L (Reconstituted Complex), TNFRSF1B (Biochemical Activity), CSNK1A1L (Biochemical Activity), TNFRSF1A (Biochemical Activity), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS), CSNK1A1L (Affinity Capture-MS)

ESM2 similar proteins: B9VVJ6, O15726, O76324, P35507, P35508, P40235, P40236, P42168, P48729, P48730, P49674, P54367, P67827, P67828, P67829, P67962, P67963, P78368, P97633, Q06486, Q39050, Q4R9A9, Q5BP74, Q5PRD4, Q5R4V3, Q5RC72, Q5ZLL1, Q62761, Q62762, Q62763, Q6P3K7, Q6P647, Q6QNL9, Q6QNM1, Q7RBX5, Q7T2E3, Q8BK63, Q8BVP5, Q8C4X2, Q8IHZ9

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

17 interactions.

AEffectBMechanism
CSNK1A1Lup-regulatesGLI2phosphorylation
CSNK1A1Lup-regulatesGLI3phosphorylation
PRKACAup-regulatesCSNK1A1Lphosphorylation
CSNK1A1Lup-regulatesGLIS2
CSNK1A1Lup-regulatesLRP6phosphorylation
FAM83G“up-regulates quantity”CSNK1A1Lbinding
FAM83B“up-regulates quantity”CSNK1A1Lbinding
FAM83H“up-regulates quantity”CSNK1A1Lbinding
FAM83A“up-regulates quantity”CSNK1A1Lbinding
FAM83D“up-regulates quantity”CSNK1A1Lbinding
FAM83E“up-regulates quantity”CSNK1A1Lbinding
FAM83F“up-regulates quantity”CSNK1A1Lbinding
FAM83C“up-regulates quantity”CSNK1A1Lbinding
CSNK1A1L“up-regulates activity”NFAT5phosphorylation
CSNK1A1Ldown-regulatesCTNNB1phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic1
Likely pathogenic0
Uncertain significance55
Likely benign0
Benign0

Top pathogenic / likely-pathogenic (1)

Variant IDHGVSClassification
1527765GRCh37/hg19 13q13.3(chr13:36064105-39230796)x1Pathogenic

SpliceAI

79 predictions. Top by Δscore:

VariantEffectΔscore
13:37105484:C:CTdonor_gain0.7900
13:37105485:C:CTdonor_gain0.7800
13:37105368:C:CTdonor_gain0.6800
13:37105369:C:CTdonor_gain0.6500
13:37105483:A:ACdonor_gain0.5900
13:37104782:C:CTacceptor_gain0.4500
13:37105388:G:GCdonor_gain0.4500
13:37105414:C:Adonor_gain0.4200
13:37105381:T:TAdonor_gain0.4100
13:37105382:C:Adonor_gain0.4100
13:37105406:AG:Adonor_gain0.3900
13:37105423:A:Tdonor_gain0.3900
13:37105489:T:TAdonor_gain0.3900
13:37105100:TG:Tdonor_gain0.3700
13:37105537:C:CCacceptor_gain0.3300
13:37104484:A:Cdonor_gain0.3200
13:37104502:AACCC:Adonor_gain0.3200
13:37105367:G:Cdonor_gain0.3200
13:37105412:ATC:Adonor_gain0.3200
13:37105592:CGG:Cdonor_gain0.3200
13:37104513:TAAA:Tdonor_gain0.3100
13:37104514:AAAA:Adonor_gain0.3100
13:37105585:C:CTdonor_gain0.3100
13:37105586:T:TTdonor_gain0.3100
13:37105384:CGGTG:Cdonor_gain0.3000
13:37105392:CAGGG:Cdonor_gain0.3000
13:37105486:A:AAdonor_gain0.3000
13:37104448:T:TAdonor_gain0.2900
13:37104838:T:Cdonor_gain0.2900
13:37105582:CCG:Cdonor_gain0.2900

AlphaMissense

2257 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
13:37104365:A:GW298R0.998
13:37104365:A:TW298R0.998
13:37104596:A:GW221R0.998
13:37104596:A:TW221R0.998
13:37104690:G:CS189R0.998
13:37104690:G:TS189R0.998
13:37104692:T:GS189R0.998
13:37104363:C:AW298C0.996
13:37104363:C:GW298C0.996
13:37104853:C:GR135P0.996
13:37105119:C:AK46N0.996
13:37105119:C:GK46N0.996
13:37104453:A:CF268L0.995
13:37104453:A:TF268L0.995
13:37104455:A:GF268L0.995
13:37104660:G:CS199R0.995
13:37104660:G:TS199R0.995
13:37104662:T:GS199R0.995
13:37104369:A:CF296L0.994
13:37104369:A:TF296L0.994
13:37104371:A:GF296L0.994
13:37104650:C:GD203H0.994
13:37104991:A:TV89D0.994
13:37105126:G:TA44E0.994
13:37105173:A:CF28L0.994
13:37105173:A:TF28L0.994
13:37105175:A:GF28L0.994
13:37104594:C:AW221C0.993
13:37104594:C:GW221C0.993
13:37104787:T:AD157V0.993

dbSNP variants (sampled 300 via entrez): RS1000227474 (13:37105554 G>A), RS1000326070 (13:37102964 A>G), RS1000378569 (13:37102807 A>C), RS1001649216 (13:37105064 T>C), RS1001680246 (13:37105326 C>A,G,T), RS1001992740 (13:37106102 A>G), RS1002023869 (13:37106526 A>C,G), RS1003380964 (13:37106657 G>A,T), RS1003737819 (13:37107055 A>G), RS1005342465 (13:37106321 C>A), RS1007189241 (13:37103308 C>G,T), RS1007537938 (13:37103657 T>C), RS1008599522 (13:37104829 A>G), RS1008891491 (13:37105689 A>C,T), RS1010136781 (13:37104528 G>A,C)

Disease associations

OMIM: gene `` | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

StudyTraitp-value
GCST001841_12Palmitoleic acid (16:1n-7) levels3.000000e-06
GCST002337_99Amyotrophic lateral sclerosis (sporadic)4.000000e-07
GCST004289_2Adiponectin levels in pregnancy5.000000e-06

EFO canonical traits (1, from GWAS)

EFO IDTrait name
EFO:0004502adiponectin measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5520 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

7 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 127,263 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL288441BOSUTINIB412,255
CHEMBL535SUNITINIB479,020
CHEMBL428690ALVOCIDIB327,781
CHEMBL603469LESTAURTINIB3
CHEMBL1721885SU-0148132363
CHEMBL230011TG100-11521,504
CHEMBL607707PELITINIB26,340

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

Binding affinities (BindingDB)

4 measured of 4 human assays (4 total across all organisms); most potent 4 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
StaurosporineKD1.7 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-carboxamideKD2600 nM
(E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-ethoxy-6-quinolyl]-4-(dimethylamino)but-2-enamideKD3500 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-carboxamideKD3500 nM

ChEMBL bioactivities

27 potent at pChembl≥5 of 27 total, top 22 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
6.60Kd250nMSTAUROSPORINE
6.28IC50520nMCHEMBL5303449
6.26Kd550nMSUNITINIB
6.00IC501000nMTP-030-1
6.00IC501000nMTP-030-2
6.00IC501000nMTP-030n
6.00Kd1000nMPELITINIB
5.90IC501270nMSTAUROSPORINE
5.82Kd1500nMSU-014813
5.77Kd1700nMCHEMBL280317
5.77IC501690nMSTAUROSPORINE
5.77Kd1700nMSB-203580
5.72Kd1900nMSB-202190
5.72Kd1900nMTG100-115
5.70Kd2000nMCHEMBL1241674
5.62IC502410nMSTAUROSPORINE
5.62Kd2400nMALVOCIDIB
5.58Kd2600nMBOSUTINIB
5.34Kd4600nMCHEMBL379218
5.28Kd5200nMTAE-684
5.23Kd5900nMSB-431542
5.15Kd7100nMLESTAURTINIB

PubChem BioAssay actives

22 with measured affinity, of 191 total; 15 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
(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-one435281: Binding constant for full-length CSNK1A1Lkd0.2500uM
Sunitinib435281: Binding constant for full-length CSNK1A1Lkd0.5500uM
(E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide435281: Binding constant for full-length CSNK1A1Lkd1.0000uM
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-carboxamide435281: Binding constant for full-length CSNK1A1Lkd1.5000uM
4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine435281: Binding constant for full-length CSNK1A1Lkd1.7000uM
4-[4-(4-fluorophenyl)-2-(4-methylsulfonylphenyl)-1H-imidazol-5-yl]pyridine1899314: Binding affinity to CK1a1L (unknown origin)kd1.7000uM
3-[2,4-diamino-7-(3-hydroxyphenyl)pteridin-6-yl]phenol624723: Binding constant for CSNK1A1L kinase domainkd1.9000uM
4-[4-(4-fluorophenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]phenol435281: Binding constant for full-length CSNK1A1Lkd1.9000uM
2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol624723: Binding constant for CSNK1A1L kinase domainkd2.0000uM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one624723: Binding constant for CSNK1A1L kinase domainkd2.4000uM
Bosutinib624723: Binding constant for CSNK1A1L kinase domainkd2.6000uM
(2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine624723: Binding constant for CSNK1A1L kinase domainkd4.6000uM
5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine624723: Binding constant for CSNK1A1L kinase domainkd5.2000uM
4-[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide435281: Binding constant for full-length CSNK1A1Lkd5.9000uM
(15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one624723: Binding constant for CSNK1A1L kinase domainkd7.1000uM

CTD chemical–gene interactions

14 total (human), top 14 by PubMed support.

ChemicalActions (top 5)PubMed papers
Aflatoxin B1decreases methylation, increases methylation2
bisphenol Adecreases methylation1
pyrogallol 1,3-dimethyl etheraffects cotreatment, affects localization, increases expression1
tris(1,3-dichloro-2-propyl)phosphateincreases expression1
sodium arseniteaffects expression1
CGP 52608affects binding, increases reaction1
Air Pollutantsincreases abundance, increases expression1
Benzo(a)pyreneincreases methylation1
Coalincreases abundance, increases expression1
Furaldehydeaffects cotreatment, affects localization, decreases expression1
Smokeincreases abundance, increases expression1
Sodium Chlorideaffects cotreatment, affects localization, decreases expression, increases expression1
Urethaneincreases expression1
Copper Sulfateincreases expression1

ChEMBL screening assays

93 unique, capped per target: 93 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1033256BindingInhibition of CSNK1A1L at 3 uMDiscovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. — J Med Chem

Clinical trials (associated diseases)

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

  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): sporadic amyotrophic lateral sclerosis