NUAK2

gene
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Also known as SNARKFLJ90349

Summary

NUAK2 (NUAK family kinase 2, HGNC:29558) is a protein-coding gene on chromosome 1q32.1, encoding NUAK family SNF1-like kinase 2 (Q9H093). Stress-activated kinase involved in tolerance to glucose starvation.

Enables ATP binding activity; magnesium ion binding activity; and protein serine/threonine kinase activity. Involved in several processes, including cellular response to glucose starvation; protein phosphorylation; and regulation of hippo signaling. Located in nuclear speck. Implicated in anencephaly.

Source: NCBI Gene 81788 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): anencephaly 2 (Moderate, GenCC)
  • GWAS associations: 10
  • Clinical variants (ClinVar): 115 total — 1 pathogenic, 1 likely-pathogenic
  • Phenotypes (HPO): 9
  • Druggable target: yes — 34 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_030952

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:29558
Approved symbolNUAK2
NameNUAK family kinase 2
Location1q32.1
Locus typegene with protein product
StatusApproved
AliasesSNARK, FLJ90349
Ensembl geneENSG00000163545
Ensembl biotypeprotein_coding
OMIM608131
Entrez81788

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000367157

RefSeq mRNA: 1 — MANE Select: NM_030952 NM_030952

CCDS: CCDS1453

Canonical transcript exons

ENST00000367157 — 7 exons

ExonStartEnd
ENSE00001075851205311705205311825
ENSE00001075853205308165205308230
ENSE00001075855205305199205305331
ENSE00001075858205308581205308732
ENSE00001075861205306188205306307
ENSE00001443657205321398205321745
ENSE00001607276205302063205304513

Expression profiles

Bgee: expression breadth ubiquitous, 220 present calls, max score 95.26.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 18.1400 / max 452.8664, expressed in 1521 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter IDTPM avgSamples expressed
1697018.01891519
169680.121059

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
cervix squamous epitheliumUBERON:000692295.26gold quality
lower esophagus mucosaUBERON:003583494.78gold quality
bloodUBERON:000017892.37gold quality
ileal mucosaUBERON:000033192.09gold quality
oviduct epitheliumUBERON:000480491.72gold quality
tongue squamous epitheliumUBERON:000691991.43gold quality
metanephros cortexUBERON:001053391.26gold quality
gingival epitheliumUBERON:000194990.81gold quality
cervix epitheliumUBERON:000480190.33gold quality
gingivaUBERON:000182890.19gold quality
squamous epitheliumUBERON:000691489.87gold quality
esophagus mucosaUBERON:000246989.60gold quality
pharyngeal mucosaUBERON:000035589.00gold quality
granulocyteCL:000009488.80gold quality
epithelium of esophagusUBERON:000197687.89gold quality
palpebral conjunctivaUBERON:000181287.65gold quality
esophagus squamous epitheliumUBERON:000692087.53gold quality
renal medullaUBERON:000036286.43gold quality
mucosa of transverse colonUBERON:000499186.11gold quality
nephron tubuleUBERON:000123186.00gold quality
kidney epitheliumUBERON:000481985.83gold quality
metanephric glomerulusUBERON:000473685.61gold quality
jejunal mucosaUBERON:000039985.25gold quality
upper leg skinUBERON:000426284.68gold quality
renal glomerulusUBERON:000007484.67gold quality
oral cavityUBERON:000016784.17gold quality
vaginaUBERON:000099683.98gold quality
adult mammalian kidneyUBERON:000008283.74gold quality
cortex of kidneyUBERON:000122583.73gold quality
buccal mucosa cellCL:000233683.55gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3yes6.02

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

100 targeting NUAK2, 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-5692A100.0074.406850
HSA-MIR-6867-5P100.0082.213464
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-574-5P100.0066.01989
HSA-MIR-371B-5P99.9975.344759
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-6870-5P99.9968.552115
HSA-MIR-548AW99.9972.573559
HSA-MIR-373-5P99.9875.364753
HSA-MIR-616-5P99.9875.584775
HSA-MIR-480399.9871.993117
HSA-MIR-4723-5P99.9768.702034
HSA-MIR-569899.9768.492029
HSA-MIR-7111-5P99.9768.482062
HSA-MIR-23A-3P99.9574.243163
HSA-MIR-23B-3P99.9574.243163
HSA-MIR-23C99.9573.923192
HSA-MIR-497-5P99.9271.832674
HSA-MIR-15A-5P99.9072.802787
HSA-MIR-15B-5P99.9072.782798
HSA-MIR-16-5P99.9072.802780
HSA-MIR-195-5P99.9072.812805
HSA-MIR-449399.9066.48977
HSA-MIR-4753-3P99.9071.033786
HSA-MIR-6838-5P99.8971.942690
HSA-MIR-424-5P99.8971.902641
HSA-MIR-7162-3P99.8968.161682
HSA-MIR-124-3P99.8973.743043
HSA-MIR-506-3P99.8973.553057
HSA-MIR-6780A-5P99.8866.692776

Literature-anchored findings (GeneRIF, showing 23)

  • This study describes the cloning and characterization of the rat SNARK homolog, mapping of the human SNARK gene to 1q32, and a potential functional role as mediator of the cellular response to metabolic stress. (PMID:11284715)
  • SNARK is an NF-kappaB-regulated anti-apoptotic gene that contributes to the tumor-promoting activity of CD95 in apoptosis-resistant tumor cells (PMID:15345718)
  • These data suggests different phosphorylation and regulation of MYPT1 activity by NUAK2. (PMID:18023418)
  • EBV LMP1 upregulated the expression of SNARK; SNARK expression increased drug resistance in response to doxorubicin increased of cancer cell survival (PMID:18452098)
  • The nuclear localizing SNARK altered transcriptome profiles and a considerable part of these alterations were canceled by the mutation of NLS, suggesting the ability of SNARK to modulate gene expression dependent on its nuclear localization. (PMID:18992219)
  • Skeletal muscle SNARK expression is increased in human obesity, and in response to metabolic stressors, but not type 2 diabetes. Partial SNARK depletion failed to modify either glucose or lipid metabolism. (PMID:19652946)
  • Data show that SNARK is activated by muscle contraction and is a unique mediator of contraction-stimulated glucose transport in skeletal muscle. (PMID:20713714)
  • MLCP (myosin light chain phosphatase) activation is counteracted by a previously unrecognized association between MRIP (myosin phosphatase Rho-interacting protein) and the inducible kinase NUAK2 (PMID:21242312)
  • This study further supports the importance of NUAK2 in cancer development and tumor progression, while AMPK has antioncogenic properties. (PMID:21460252)
  • Considers possible roles of NUAK2 in tumorigenesis in general and suggest that NUAK2 has pivotal roles in acral melanomagenesis. (PMID:21911917)
  • Activation of AMP-activated protein kinase protects the integrity of the blood-brain barrier by suppressing the induction of NADPH oxidase-derived superoxide anions. (PMID:22796592)
  • The AMPK-related kinase SNARK regulates hepatitis C virus replication and pathogenesis through enhancement of TGF-beta signaling. (PMID:23831117)
  • Sucrose non-fermenting AMPK related kinase/Pentraxin 3 combined role in immunometabolic signaling and DNA damage response is proposed to accelerate cardiovascular complications in systemic lupus erythematosus patients (PMID:25732129)
  • NUAK2 silencing and inactivation of the PI3K pathway efficiently controlled CDK2 expression, whereas CDK2 inactivation specifically abrogated the growth of NUAK2-amplified and PTEN-deficient melanoma cells. (PMID:25832654)
  • miR143 inhibited the proliferation, migration and invasion of the glioblastoma cells by degrading NUAK2 in glioblastoma. (PMID:27081712)
  • Data (including data from studies in knockout and transgenic mice) suggest that NUAK2/SNARK is involved in both adipose inflammation and energy metabolism in adipocytes; additionally, genome-wide association studies suggest that 2 SNPs in NUAK2/SNARK (rs4682880, rs4682676) are associated with obesity in women. (PMID:29298809)
  • NUAK2 localization in normal skin and its expression in a variety of skin tumors with YAP. (PMID:32001115)
  • A loss-of-function NUAK2 mutation in humans causes anencephaly due to impaired Hippo-YAP signaling. (PMID:32845958)
  • NUAK2 silencing inhibits the proliferation, migration and epithelialtomesenchymal transition of cervical cancer cells via upregulating CYFIP2. (PMID:34558636)
  • GPR65 promotes intestinal mucosal Th1 and Th17 cell differentiation and gut inflammation through downregulating NUAK2. (PMID:35343079)
  • Circ_0000033 up-regulates NUAK2 by sequestering miR-378a-3p to promote breast tumorigenesis. (PMID:37357410)
  • Enhanced SARS-CoV-2 entry via UPR-dependent AMPK-related kinase NUAK2. (PMID:37421942)
  • OTUD7B deubiquitinates and stabilizes YAP1 to upregulate NUAK2 expression, thus accelerating gastric cancer procession. (PMID:37429790)

Cross-species orthologs

9 orthologs

OrganismSymbolGene ID
danio_rerionuak2ENSDARG00000063661
mus_musculusNuak2ENSMUSG00000009772
rattus_norvegicusNuak2ENSRNOG00000000034
drosophila_melanogasterSnrkFBGN0033915
drosophila_melanogasterNuakFBGN0262617
caenorhabditis_elegansWBGENE00012638
caenorhabditis_elegansZK524.4WBGENE00013994
caenorhabditis_eleganstag-344WBGENE00015230
caenorhabditis_elegansWBGENE00044388

Paralogs (17): NUAK1 (ENSG00000074590), PRKAA1 (ENSG00000132356), TSSK4 (ENSG00000139908), HUNK (ENSG00000142149), SIK1 (ENSG00000142178), BRSK1 (ENSG00000160469), SIK3 (ENSG00000160584), PRKAA2 (ENSG00000162409), TSSK3 (ENSG00000162526), SNRK (ENSG00000163788), MELK (ENSG00000165304), SIK2 (ENSG00000170145), BRSK2 (ENSG00000174672), NIM1K (ENSG00000177453), TSSK6 (ENSG00000178093), TSSK2 (ENSG00000206203), TSSK1B (ENSG00000212122)

Protein

Protein identifiers

NUAK family SNF1-like kinase 2Q9H093 (reviewed: Q9H093)

Alternative names: Omphalocele kinase 2, SNF1/AMP kinase-related kinase

All UniProt accessions (1): Q9H093

UniProt curated annotations — full annotation on UniProt →

Function. Stress-activated kinase involved in tolerance to glucose starvation. Induces cell-cell detachment by increasing F-actin conversion to G-actin. Expression is induced by CD95 or TNF, via NF-kappa-B. Protects cells from CD95-mediated apoptosis and is required for the increased motility and invasiveness of CD95-activated tumor cells. Phosphorylates LATS1 and LATS2. Plays a key role in neural tube closure during embryonic development through LATS2 phosphorylation and regulation of the nuclear localization of YAP1 a critical downstream regulatory target in the Hippo signaling pathway.

Post-translational modifications. Phosphorylated at Thr-208 by STK11/LKB1 in complex with STE20-related adapter-alpha (STRADA) pseudo kinase and CAB39. Autophosphorylation is also possible at Thr-208.

Disease relevance. Anencephaly 2 (ANPH2) [MIM:619452] A form of anencephaly, an extreme neural tube defect resulting in the absence of brain tissues, and death in utero or perinatally. Infants are born with intact spinal cords, cerebellums, and brainstems, but lack formation of neural structures above this level. The skull is only partially formed. ANPH2 features may also include frontonasal dysplasia with midline cleft of the upper lip and alveolar ridge, bifid nose, and clinical anophthalmia. ANPH2 inheritance is autosomal recessive. The disease is caused by variants affecting the gene represented in this entry.

Activity regulation. Activated by phosphorylation on Thr-208.

Similarity. Belongs to the protein kinase superfamily. CAMK Ser/Thr protein kinase family. SNF1 subfamily.

RefSeq proteins (1): NP_112214* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000719Prot_kinase_domDomain
IPR008271Ser/Thr_kinase_ASActive_site
IPR011009Kinase-like_dom_sfHomologous_superfamily
IPR017441Protein_kinase_ATP_BSBinding_site

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 (23 total): modified residue 7, sequence variant 6, region of interest 2, mutagenesis site 2, binding site 2, chain 1, domain 1, compositionally biased region 1, active site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9H093-F163.450.36

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): 175 (proton acceptor)

Ligand- & substrate-binding residues (2): 59–67; 81

Post-translational modifications (7): 435, 523, 544, 547, 573, 1, 208

Mutagenesis-validated functional residues (2):

PositionPhenotype
81loss of autophosphorylation, kinase activity and of anti-apoptotic activity.
208prevents phosphorylation and activation by stk11/lkb1 complex.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 154 (showing top): GSE45365_NK_CELL_VS_CD11B_DC_DN, LEE_NEURAL_CREST_STEM_CELL_DN, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, GOBP_HIPPO_SIGNALING, RICKMAN_METASTASIS_DN, WTGAAAT_UNKNOWN, AACTTT_UNKNOWN, GOBP_CELLULAR_RESPONSE_TO_STARVATION, GOBP_PROTEIN_LOCALIZATION_TO_ORGANELLE, TAATGTG_MIR323, GOBP_CELLULAR_RESPONSE_TO_GLUCOSE_STARVATION, GOBP_PROTEIN_LOCALIZATION_TO_NUCLEUS, GOBP_RESPONSE_TO_STARVATION, TGGAAA_NFAT_Q4_01, GOMF_MAGNESIUM_ION_BINDING

GO Biological Process (7): protein phosphorylation (GO:0006468), apoptotic process (GO:0006915), actin cytoskeleton organization (GO:0030036), protein localization to nucleus (GO:0034504), regulation of hippo signaling (GO:0035330), cellular response to glucose starvation (GO:0042149), negative regulation of apoptotic process (GO:0043066)

GO Molecular Function (10): magnesium ion binding (GO:0000287), 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), metal ion binding (GO:0046872)

GO Cellular Component (0):

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
protein kinase activity2
phosphorylation1
protein modification process1
programmed cell death1
apoptotic signaling pathway1
execution phase of apoptosis1
cytoskeleton organization1
actin filament-based process1
protein localization to organelle1
hippo signaling1
regulation of intracellular signal transduction1
cellular response to starvation1
apoptotic process1
regulation of apoptotic process1
negative regulation of programmed cell death1
metal ion binding1
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
binding1
transferase activity, transferring phosphorus-containing groups1
catalytic activity1
cation binding1

Protein interactions and networks

STRING

766 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
NUAK2SIK3Q9Y2K2603
NUAK2SIK2Q9H0K1540
NUAK2ARHGEF17Q96PE2530
NUAK2MPRIPQ6WCQ1498
NUAK2SIK1P57059474
NUAK2A0A0B4J2F2A0A0B4J2F2472
NUAK2PTPN14Q15678458
NUAK2ACVR1Q04771430
NUAK2AMOTL2Q9Y2J4427
NUAK2CAB39Q9Y376415
NUAK2WDR49Q8IV35408
NUAK2PPP1R12AO14974407
NUAK2PLEKHH3Q7Z736399
NUAK2XRN1Q8IZH2389
NUAK2PLA2G4CQ9UP65387

IntAct

20 interactions, top by confidence:

ABTypeScore
TNIP1NFKB1psi-mi:“MI:0914”(association)0.790
NUAK2PPP1R12Apsi-mi:“MI:0914”(association)0.640
GRIPAP1NUAK2psi-mi:“MI:0915”(physical association)0.560
SFNNUAK2psi-mi:“MI:0915”(physical association)0.560
NUAK2SMAD3psi-mi:“MI:0915”(physical association)0.520
SMAD3NUAK2psi-mi:“MI:0915”(physical association)0.520
YWHAENUAK2psi-mi:“MI:0915”(physical association)0.400
NUAK2SMAD2psi-mi:“MI:0915”(physical association)0.400
TGFBR1NUAK2psi-mi:“MI:0915”(physical association)0.400
NUAK2HSP90AB1psi-mi:“MI:0915”(physical association)0.400
NUAK2HSP90AA1psi-mi:“MI:0914”(association)0.350
NUAK2PPP1R12Apsi-mi:“MI:0914”(association)0.350
NUAK2AP3D1psi-mi:“MI:0914”(association)0.350
NUAK2GRIPAP1psi-mi:“MI:0915”(physical association)0.000

BioGRID (66): NUAK2 (Reconstituted Complex), HSP90AB3P (Affinity Capture-MS), LZTR1 (Affinity Capture-MS), PPP1R12A (Affinity Capture-MS), MARK3 (Affinity Capture-MS), UBXN7 (Affinity Capture-MS), FLNC (Affinity Capture-MS), BTRC (Affinity Capture-MS), AHCYL2 (Affinity Capture-MS), MARK2 (Affinity Capture-MS), FBXW11 (Affinity Capture-MS), DCAF5 (Affinity Capture-MS), USP7 (Affinity Capture-MS), NUAK2 (Affinity Capture-RNA), NUAK2 (Two-hybrid)

ESM2 similar proteins: A0AUV4, A1A5Q6, A1A5R7, A2KF29, B1WAS2, C0HKC8, C0HKC9, D3ZML2, O60285, O74536, O88831, O88866, P41279, P51956, P57058, P97756, Q20443, Q2T9U5, Q5R7G9, Q5XHI9, Q60670, Q63562, Q641K5, Q66HE5, Q68UT7, Q6P431, Q6VZ17, Q7T0B0, Q7T0B1, Q7TNJ7, Q7TNL4, Q8BHI9, Q8BZN4, Q8C078, Q8C0N0, Q8C0V7, Q8C0X8, Q8CIP4, Q8IY84, Q8K4K4

Diamond homologs: A1Z9X0, A2CI34, A2CI35, A8KBH6, A8XW88, F1M7Y5, O70146, P00542, P00543, P04409, P05126, P05128, P05129, P05696, P05771, P05772, P07332, P09215, P0CD62, P10102, P10829, P13678, P14238, P16054, P16879, P17252, P20444, P21137, P22612, P23298, P24723, P28867, P32866, P41743, P43057, P48562, P50527, P57078, P63318, P63319

SIGNOR signaling

5 interactions.

AEffectBMechanism
STK11up-regulatesNUAK2phosphorylation
NUAK2down-regulatesLATS1phosphorylation
NUAK2“up-regulates activity”WDR45phosphorylation
NUAK2“down-regulates activity”PPP1R12Aphosphorylation
NUAK2“down-regulates activity”LATphosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic1
Likely pathogenic1
Uncertain significance95
Likely benign8
Benign1

Top pathogenic / likely-pathogenic (2)

Variant IDHGVSClassification
1184278NM_030952.3(NUAK2):c.412_433delinsG (p.Tyr138_Gln145delinsGlu)Pathogenic
3911831NM_030952.3(NUAK2):c.1666C>T (p.Gln556Ter)Likely pathogenic

SpliceAI

1143 predictions. Top by Δscore:

VariantEffectΔscore
1:205304509:GGCAT:Gacceptor_gain1.0000
1:205304510:GCAT:Gacceptor_gain1.0000
1:205304511:CAT:Cacceptor_gain1.0000
1:205304511:CATC:Cacceptor_gain1.0000
1:205304511:CATCT:Cacceptor_loss1.0000
1:205304512:AT:Aacceptor_gain1.0000
1:205304512:ATCTG:Aacceptor_loss1.0000
1:205304513:TCT:Tacceptor_loss1.0000
1:205304514:C:CAacceptor_loss1.0000
1:205304514:C:CCacceptor_gain1.0000
1:205304515:T:Aacceptor_loss1.0000
1:205304522:C:CTacceptor_gain1.0000
1:205304523:A:Tacceptor_gain1.0000
1:205305193:A:ACdonor_gain1.0000
1:205305194:C:CCdonor_gain1.0000
1:205305196:CA:Cdonor_loss1.0000
1:205305197:A:ACdonor_gain1.0000
1:205305197:AC:Adonor_gain1.0000
1:205305198:C:CTdonor_gain1.0000
1:205305198:CC:Cdonor_gain1.0000
1:205305198:CCA:Cdonor_gain1.0000
1:205305198:CCAG:Cdonor_gain1.0000
1:205305198:CCAGA:Cdonor_gain1.0000
1:205305327:TCCAC:Tacceptor_gain1.0000
1:205305328:CCACC:Cacceptor_gain1.0000
1:205305329:CAC:Cacceptor_gain1.0000
1:205305332:C:CCacceptor_gain1.0000
1:205305332:C:CGacceptor_loss1.0000
1:205306183:CTTA:Cdonor_loss1.0000
1:205306184:TTACC:Tdonor_loss1.0000

AlphaMissense

4085 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
1:205306299:G:CD193E1.000
1:205306299:G:TD193E1.000
1:205306300:T:AD193V1.000
1:205306300:T:GD193A1.000
1:205306301:C:GD193H1.000
1:205308211:T:AD175V1.000
1:205308211:T:GD175A1.000
1:205308214:C:GR174P1.000
1:205311814:C:AK81N1.000
1:205311814:C:GK81N1.000
1:205305272:A:CF250L0.999
1:205305272:A:TF250L0.999
1:205305274:A:GF250L0.999
1:205305276:G:TP249H0.999
1:205305322:A:GW234R0.999
1:205305322:A:TW234R0.999
1:205305328:C:GD232H0.999
1:205306242:G:CS212R0.999
1:205306242:G:TS212R0.999
1:205306244:T:GS212R0.999
1:205306246:C:TG211E0.999
1:205306291:A:GL196P0.999
1:205306300:T:CD193G0.999
1:205306303:G:TA192D0.999
1:205308195:G:CN180K0.999
1:205308195:G:TN180K0.999
1:205308210:A:CD175E0.999
1:205308210:A:TD175E0.999
1:205308211:T:CD175G0.999
1:205311758:T:AE100V0.999

dbSNP variants (sampled 300 via entrez): RS1000065722 (1:205314387 C>A,G), RS1000067557 (1:205315850 G>A,T), RS1000098269 (1:205316190 A>G), RS1000136971 (1:205315956 A>G), RS1000458589 (1:205303613 T>A,G), RS1000786912 (1:205304809 A>G), RS1000845560 (1:205321933 A>C), RS1001001055 (1:205301938 A>C), RS1001047192 (1:205302013 C>G), RS1001115106 (1:205308391 C>T), RS1001276124 (1:205322164 T>A,C), RS1001438335 (1:205310455 G>C,T), RS1001691733 (1:205313050 G>T), RS1001852357 (1:205306911 G>A), RS1002033654 (1:205311464 A>G)

Disease associations

OMIM: gene MIM:608131 | disease phenotypes: MIM:619452

GenCC curated gene-disease

DiseaseClassificationInheritance
anencephaly 2ModerateAutosomal recessive

Mondo (1): anencephaly 2 (MONDO:0030338)

Orphanet (0):

HPO phenotypes

9 total (9 of 9 shown, HPO-id order):

HPOTerm
HP:0000007Autosomal recessive inheritance
HP:0000161Median cleft upper lip
HP:0000528Anophthalmia
HP:0002323Anencephaly
HP:0003577Congenital onset
HP:0009099Median cleft palate
HP:0010289Cleft maxillary alveolar ridge
HP:0011803Bifid nose
HP:0012745Short palpebral fissure

GWAS associations

10 associations (top):

StudyTraitp-value
GCST005993_65Mean corpuscular hemoglobin1.000000e-10
GCST010002_349Refractive error8.000000e-13
GCST010143_9Meat-related diet4.000000e-11
GCST010697_12Cortical surface area (min-P)6.000000e-10
GCST010698_16Subcortical volume (min-P)8.000000e-09
GCST010699_52Brain morphology (min-P)5.000000e-08
GCST010700_66Cortical thickness (MOSTest)3.000000e-09
GCST010701_17Cortical surface area (MOSTest)5.000000e-08
GCST010702_2Subcortical volume (MOSTest)3.000000e-08
GCST010703_27Brain morphology (MOSTest)5.000000e-09

EFO canonical traits (4, from GWAS)

EFO IDTrait name
EFO:0004527mean corpuscular hemoglobin
EFO:0008111diet measurement
EFO:0004346neuroimaging measurement
EFO:0004840cortical thickness

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5698 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

34 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 330,942 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1287853FEDRATINIB43,554
CHEMBL1289926AXITINIB415,732
CHEMBL1789941RUXOLITINIB411,547
CHEMBL180022NERATINIB49,404
CHEMBL2103743TOFACITINIB CITRATE41,672
CHEMBL221959TOFACITINIB410,408
CHEMBL288441BOSUTINIB412,255
CHEMBL502835NINTEDANIB48,545
CHEMBL535SUNITINIB479,020
CHEMBL601719CRIZOTINIB414,403
CHEMBL608533MIDOSTAURIN47,259
CHEMBL939GEFITINIB4117,814
CHEMBL270995BRIVANIB ALANINATE31,077
CHEMBL300138ENZASTAURIN33,209
CHEMBL3137331DEFACTINIB31,229
CHEMBL3904602LEROCICLIB31,012
CHEMBL428690ALVOCIDIB327,781
CHEMBL522892DOVITINIB34,944
CHEMBL603469LESTAURTINIB3
CHEMBL91829RUBOXISTAURIN377
CHEMBL1721885SU-0148132
CHEMBL3115681NARAZACICLIB2
CHEMBL402548DANUSERTIB2
CHEMBL475251R-4062
CHEMBL572878TOZASERTIB2
CHEMBL575448BMS-7548072
CHEMBL607707PELITINIB2
CHEMBL1908394GSK-4613641
CHEMBL1908397KW-24491
CHEMBL296468BMS-3870321

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — NuaK subfamily

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

LigandActionAffinityParameter
WZ4003Inhibition7.0pIC50
HTH-02-006Inhibition6.9pIC50

Binding affinities (BindingDB)

11 measured of 11 human assays (11 total across all organisms); most potent 11 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
StaurosporineKD1.7 nM
PKC-412KD190 nM
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyrilKD520 nM
(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.1^{7,14}.0^{2,6}.0^{8,13}.0^{22,27}]nonacosa-1(28),2(6),7(29),8(13),9,11,22(27),23,25-nonaene-3,5-dioneKD700 nM
N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamideKD1100 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
1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3bKD3100 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
3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrileKD5000 nM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S)-3-hydroxy-1-methyl-4-piperidinyl]-1-benzopyran-4-oneKD5300 nM

ChEMBL bioactivities

89 potent at pChembl≥5 of 90 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.07Kd0.086nMSTAUROSPORINE
9.15Kd0.7nMLEROCICLIB
9.00Kd1nMLESTAURTINIB
8.92Kd1.2nMTAE-684
8.79IC501.62nMSTAUROSPORINE
8.78IC501.67nMSTAUROSPORINE
8.72IC501.9nMSTAUROSPORINE
8.52Kd3nMBRIVANIB ALANINATE
8.46Kd3.5nMCHEMBL4284499
8.30IC505.012nMNARAZACICLIB
8.15Kd7nMCYC-116
8.00Kd10nMCHEMBL4465866
8.00Kd10nMCHEMBL1229592
7.96Kd11nMCHEMBL4576489
7.80IC5015.85nMCHEMBL6175168
7.68Kd21nMNINTEDANIB
7.64Kd23nMGSK-461364
7.62Kd24nMPF-03814735
7.60Kd25nMDANUSERTIB
7.60IC5025.12nMCHEMBL190684
7.60IC5025.12nMCHEMBL6177408
7.58Kd26nMJNJ-7706621
7.40IC5039.81nMCHEMBL6167301
7.31Kd49nMFEDRATINIB
7.27Kd54nMKW-2449
7.20Kd63nMMIDOSTAURIN
7.20IC5063.1nMCHEMBL6177133
7.19Kd65nMR-406
7.14Kd72nMLESTAURTINIB
7.07Kd86nMGSK-690693
7.00IC50100nMCHEMBL4303523
7.00IC50100nMCHEMBL6163620
6.92IC50120nMCHEMBL5199998
6.92Kd120nMCRIZOTINIB
6.90IC50126nMCHEMBL5202966
6.90IC50125.9nMCHEMBL6170125
6.89Kd130nMDOVITINIB
6.89Kd130nMCHEMBL1908395
6.85Kd140nMNERATINIB
6.82Kd150nMSUNITINIB
6.66Kd220nMBOSUTINIB
6.62Kd240nMTOFACITINIB CITRATE
6.62Kd240nMTOFACITINIB
6.50Kd320nMRUBOXISTAURIN
6.50Kd320nMRUXOLITINIB
6.40Kd400nMSU-014813
6.38Kd420nMTOFACITINIB CITRATE
6.38Kd420nMTOFACITINIB
6.36Kd440nMCGP-52421
6.34Kd454nMDEFACTINIB

PubChem BioAssay actives

74 with measured affinity, of 551 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.

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-one435559: Binding constant for SNARK kinase domainkd0.0001uM
4-[[5-(4-propan-2-ylpiperazin-1-yl)-2-pyridinyl]amino]spiro[1,3,5,11-tetrazatricyclo[7.4.0.02,7]trideca-2,4,6,8-tetraene-13,1’-cyclohexane]-10-one1609450: Binding affinity to SNARK (unknown origin)kd0.0007uM
(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-one508088: Binding affinity to SNARKkd0.0010uM
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-diamine1845591: Binding affinity to NUAK2 (unknown origin) assessed as dissociation constantkd0.0012uM
[(2R)-1-[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-yl] (2S)-2-aminopropanoate1425095: 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.kd0.0030uM
9-(cyclohexylmethyl)-4,5-dimethoxy-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-8-one1415053: Binding affinity to DNA-tagged recombinant human SNARK (22 to 333 residues) expressed in mammalian expression system by KINOMEscan assaykd0.0035uM
4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine1425095: 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.kd0.0070uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide1526222: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged NUAK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assaykd0.0100uM
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide2185074: Binding affinity to SNARK (unknown origin) assessed as dissociation constantkd0.0100uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide1526222: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged NUAK2 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assaykd0.0110uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate625139: Binding constant for SNARK kinase domainkd0.0210uM
5-[6-[(4-methylpiperazin-1-yl)methyl]benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide1845591: Binding affinity to NUAK2 (unknown origin) assessed as dissociation constantkd0.0230uM
N-[2-[4-[[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-trien-11-yl]-2-oxoethyl]acetamide1425095: 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.kd0.0240uM
N-[5-[(2R)-2-methoxy-2-phenylacetyl]-4,6-dihydro-1H-pyrrolo[3,4-d]pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide1425095: 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.kd0.0250uM
4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide435559: Binding constant for SNARK kinase domainkd0.0260uM
Fedratinib625139: Binding constant for SNARK kinase domainkd0.0490uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone625139: Binding constant for SNARK kinase domainkd0.0540uM
Midostaurin435559: Binding constant for SNARK kinase domainkd0.0630uM
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one625139: Binding constant for SNARK kinase domainkd0.0650uM
4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[[(3S)-piperidin-3-yl]methoxy]imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol625139: Binding constant for SNARK kinase domainkd0.0860uM
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide1845578: Inhibition of N-terminal GST-tagged human NUAK2 expressed in Escherichia coli DH5alpha incubated for 30 mins in presence of gamma-[32P]ATP by cerenkov counting analysisic500.1000uM
Crizotinib625139: Binding constant for SNARK kinase domainkd0.1200uM
7-[(1S)-4-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-methylsulfonylpyrrolo[2,3-d]pyrimidin-6-one1845564: Inhibition of NUAK2 (unknown origin)ic500.1200uM
N-[3-[5-iodo-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]butanamide1845564: Inhibition of NUAK2 (unknown origin)ic500.1260uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one435559: Binding constant for SNARK kinase domainkd0.1300uM
5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride625139: Binding constant for SNARK kinase domainkd0.1300uM
Neratinib625139: Binding constant for SNARK kinase domainkd0.1400uM
Sunitinib435559: Binding constant for SNARK kinase domainkd0.1500uM
Bosutinib625139: Binding constant for SNARK kinase domainkd0.2200uM
Tofacitinib625139: Binding constant for SNARK kinase domainkd0.2400uM
(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione435559: Binding constant for SNARK kinase domainkd0.3200uM
Ruxolitinib625139: Binding constant for SNARK kinase domainkd0.3200uM
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-carboxamide435559: Binding constant for SNARK kinase domainkd0.4000uM
N-[(2S,3R,4R,6R,18S)-18-hydroxy-3-methoxy-2-methyl-16-oxo-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-4-yl]-N-methylbenzamide508088: Binding affinity to SNARKkd0.4400uM
N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide1425095: 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.kd0.4540uM
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide435559: Binding constant for SNARK kinase domainkd0.5300uM
5-(3-ethylsulfonylphenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide1425095: 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.kd0.7050uM
N-[3-[[5-bromo-4-[(4-sulfamoylphenyl)methylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide1823799: Inhibition of full length recombinant human NUAK2 using KKKVSRSGLYRSPSMPENLNRPR as substrate incubated for 40 mins in presence of [gamma-33P-ATP] by radiometric scintillation assayic500.9000uM
(3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one625139: Binding constant for SNARK kinase domainkd0.9100uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide2148895: Binding affinity to human NUAK2 incubated for 45 mins by Kinobead based pull down assaykd1.0108uM
4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide1823799: Inhibition of full length recombinant human NUAK2 using KKKVSRSGLYRSPSMPENLNRPR as substrate incubated for 40 mins in presence of [gamma-33P-ATP] by radiometric scintillation assayic501.1510uM
Axitinib625139: Binding constant for SNARK kinase domainkd1.3000uM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one435559: Binding constant for SNARK kinase domainkd1.4000uM
N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide435559: Binding constant for SNARK kinase domainkd1.7000uM
(2S)-1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methylpyrrolidine-2-carboxamide2167411: Binding affinity to NUAK2 (unknown origin) by phage based competition assaykd1.8000uM
N-[3-[[5-cyclopropyl-2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]propyl]cyclobutanecarboxamide1845564: Inhibition of NUAK2 (unknown origin)ic502.6000uM
(4-hydroxypiperidin-1-yl)-[4-[[4-[4-(3-methylsulfonylpropoxy)indol-1-yl]pyrimidin-2-yl]amino]cyclohexyl]methanone769495: Binding affinity to SNARK (unknown origin)kd2.6000uM
(E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide435559: Binding constant for SNARK kinase domainkd2.7000uM
2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol625139: Binding constant for SNARK kinase domainkd3.6000uM
3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione625139: Binding constant for SNARK kinase domainkd4.1000uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Valproic Acidaffects expression, decreases expression3
perfluorooctane sulfonic aciddecreases expression, increases expression2
Arsenicaffects expression, affects methylation2
Methotrexateaffects cotreatment, increases expression, decreases expression2
Silicon Dioxidedecreases methylation, increases expression2
Silverincreases expression2
Cyclosporinedecreases expression, increases expression2
Aflatoxin B1decreases methylation, increases expression2
aristolochic acid Iincreases expression1
Glupearl 19Sincreases expression1
triphenyl phosphateaffects expression1
bisphenol Adecreases expression1
titanium dioxidedecreases methylation1
salinomycindecreases expression1
quercitrindecreases expression1
trichostatin Adecreases expression1
sodium arseniteincreases expression1
zinc chromatedecreases expression, increases abundance1
potassium chromate(VI)decreases expression1
S-(1,2-dichlorovinyl)cysteineaffects response to substance, increases expression, affects cotreatment, decreases expression1
polyhexamethyleneguanidineaffects expression1
chromium hexavalent iondecreases expression, increases abundance1
CGP 52608increases reaction, affects binding1
2-palmitoylglycerolincreases expression1
abrineincreases expression1
jinfukangdecreases expression, increases reaction1
WZ4003decreases activity1
Temozolomideincreases expression1
Sunitinibincreases expression1
Arsenic Trioxideincreases expression1

ChEMBL screening assays

200 unique, capped per target: 200 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1017050BindingBinding affinity to SNARKExamining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). — J Med Chem

Clinical trials (associated diseases)

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

  • Associated diseases: anencephaly 2
  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): anencephaly 2