CDK14

gene
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Also known as PFTAIRE1

Summary

CDK14 (cyclin dependent kinase 14, HGNC:8883) is a protein-coding gene on chromosome 7q21.13, encoding Cyclin-dependent kinase 14 (O94921). Serine/threonine-protein kinase involved in the control of the eukaryotic cell cycle, whose activity is controlled by an associated cyclin.

Enables cyclin binding activity and cyclin-dependent protein serine/threonine kinase activity. Involved in G2/M transition of mitotic cell cycle and regulation of canonical Wnt signaling pathway. Located in cytosol; nucleoplasm; and plasma membrane. Part of cytoplasmic cyclin-dependent protein kinase holoenzyme complex.

Source: NCBI Gene 5218 — RefSeq curated summary.

At a glance

  • GWAS associations: 7
  • Clinical variants (ClinVar): 84 total
  • Phenotypes (HPO): 1
  • Druggable target: yes — 17 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_001287135

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:8883
Approved symbolCDK14
Namecyclin dependent kinase 14
Location7q21.13
Locus typegene with protein product
StatusApproved
AliasesPFTAIRE1
Ensembl geneENSG00000058091
Ensembl biotypeprotein_coding
OMIM610679
Entrez5218

Gene structure

Transcript identifiers

Ensembl transcripts: 28 — 22 protein_coding, 5 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000265741, ENST00000380050, ENST00000406263, ENST00000430760, ENST00000431029, ENST00000436577, ENST00000446224, ENST00000446790, ENST00000449528, ENST00000456689, ENST00000460493, ENST00000478540, ENST00000484035, ENST00000487145, ENST00000496279, ENST00000859638, ENST00000859639, ENST00000859640, ENST00000859641, ENST00000859642, ENST00000859643, ENST00000915548, ENST00000915549, ENST00000915550, ENST00000915551, ENST00000962109, ENST00000962110, ENST00000962111

RefSeq mRNA: 4 — MANE Select: NM_001287135 NM_001287135, NM_001287136, NM_001287137, NM_012395

CCDS: CCDS5619, CCDS75626, CCDS75627, CCDS75628

Canonical transcript exons

ENST00000380050 — 15 exons

ExonStartEnd
ENSE000012683689059632190596718
ENSE000016158479095569790955817
ENSE000016162779098414890984241
ENSE000016324639111806591118208
ENSE000016396809107943291079480
ENSE000017828249111254291112681
ENSE000018062519104589791045960
ENSE000019181859120716591210590
ENSE000034663719074768190747775
ENSE000034854699091760190917724
ENSE000035379069089929190899353
ENSE000035394459072656790726812
ENSE000035620449060421890604249
ENSE000036247919086317590863269
ENSE000036626599079057390790652

Expression profiles

Bgee: expression breadth ubiquitous, 279 present calls, max score 98.24.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 18.6290 / max 732.0343, expressed in 1592 samples.

FANTOM5 promoters (14 alternative TSS)

Promoter IDTPM avgSamples expressed
794645.11111392
794604.60821346
794762.8884193
794661.5320357
794631.2738765
794750.9823150
2045140.5702347
794730.3507105
794720.336397
794770.260742

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
postcentral gyrusUBERON:000258198.24gold quality
parietal lobeUBERON:000187298.05gold quality
CA1 field of hippocampusUBERON:000388198.04gold quality
substantia nigra pars compactaUBERON:000196597.82gold quality
substantia nigra pars reticulataUBERON:000196697.70gold quality
lateral nuclear group of thalamusUBERON:000273697.70gold quality
entorhinal cortexUBERON:000272897.51gold quality
Brodmann (1909) area 10UBERON:001354197.36gold quality
superior frontal gyrusUBERON:000266197.01gold quality
Brodmann (1909) area 46UBERON:000648396.83gold quality
tendon of biceps brachiiUBERON:000818896.47gold quality
orbitofrontal cortexUBERON:000416796.45gold quality
frontal poleUBERON:000279596.28gold quality
endothelial cellCL:000011594.71gold quality
occipital lobeUBERON:000202193.22gold quality
prefrontal cortexUBERON:000045193.18gold quality
primary visual cortexUBERON:000243693.16gold quality
frontal lobeUBERON:001652593.01gold quality
frontal cortexUBERON:000187093.00gold quality
ponsUBERON:000098892.86gold quality
cerebral cortexUBERON:000095692.57gold quality
superior vestibular nucleusUBERON:000722792.55gold quality
dorsolateral prefrontal cortexUBERON:000983492.49gold quality
neocortexUBERON:000195092.45gold quality
periodontal ligamentUBERON:000826692.45gold quality
tendonUBERON:000004392.36gold quality
calcaneal tendonUBERON:000370192.34gold quality
paraflocculusUBERON:000535192.06gold quality
Brodmann (1909) area 23UBERON:001355491.78gold quality
Brodmann (1909) area 9UBERON:001354091.63gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 4.

ExperimentMarker?Max mean expression
E-CURD-119yes51.47
E-ANND-3yes11.18
E-HCAD-25yes7.39
E-GEOD-137537yes5.09

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

196 targeting CDK14, 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-3925-3P100.0069.951237
HSA-MIR-5011-5P100.0083.465820
HSA-MIR-6130100.0066.692012
HSA-MIR-513A-5P100.0069.772465
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-6127100.0066.762188
HSA-MIR-8485100.0077.574731
HSA-MIR-4510100.0066.602050
HSA-MIR-6129100.0066.462080
HSA-MIR-6133100.0066.482064
HSA-MIR-432-3P100.0067.86705
HSA-MIR-3924100.0072.092394
HSA-MIR-5692A100.0074.406850
HSA-MIR-5196-5P100.0067.982761
HSA-MIR-3667-3P99.9967.171636
HSA-MIR-511-3P99.9968.851467
HSA-MIR-548AW99.9972.573559
HSA-MIR-150-5P99.9966.691976
HSA-MIR-186-5P99.9970.833707
HSA-MIR-485-3P99.9870.681585
HSA-MIR-539-3P99.9870.741616
HSA-MIR-103A-3P99.9869.141595
HSA-MIR-10799.9869.141595
HSA-MIR-27A-3P99.9872.132955
HSA-MIR-27B-3P99.9872.132955
HSA-MIR-998599.9872.112939
HSA-MIR-314899.9775.066478
HSA-MIR-3688-3P99.9772.022834
HSA-MIR-3065-5P99.9771.563281
HSA-MIR-365899.9673.874379

Literature-anchored findings (GeneRIF, showing 39)

  • Ser119 is crucial for the interaction between hPFTAIRE1 and the 14-3-3 proteins. Binding with the 14-3-3 proteins does not contribute to the subcellular localization of the hPFTAIRE1, although the binding may be involved in its signaling regulation. (PMID:16775625)
  • PFTK1 acts as a cyclin-dependent kinase that regulates cell cycle progression and cell proliferation (PMID:17517622)
  • Novel biological cascade that involved the phosphorylation activation of CaD by PFTK1 kinase in promoting formation of actin stress fibers. (PMID:21184254)
  • Taken together, our data propose a novel, oncogene-tumor suppressor interplay, where oncogenic PFTK1 confers HCC cell motility through inactivating the actin-binding motile suppressing function of TAGLN2 via phosphorylation. (PMID:21577206)
  • in patients with oesophageal squamous cell carcinoma 5-year overall survival rate was poorer in patients positive for PFTK1 than those with negative expression; uni- and multivariate analyses identified PFTK1 as an independent marker of prognosis (PMID:22333595)
  • binding of CCNY to 14-3-3 significantly enhanced the association between CCNY and CDK14 (PMID:24618387)
  • Human cyclin Y (CCNY) is a phosphoprotein in vivo and phosphorylation of CCNY by CDK14 triggers its ubiquitination and degradation. (PMID:24794231)
  • findings indicate that brain PP-1I associates with and is regulated by the associated protein kinases C-TAK1 and PFTK1 (PMID:25028520)
  • Cigarette smoke down regulates CDK14 levels and impairs Wnt signaling. (PMID:25680692)
  • Up-regulated PFTK1 might promote breast cancer progression. (PMID:26033031)
  • Knockdown of PFTK1 increases E-cadherin expression, decreases vimentin expression and inhibits migration of glioma cells. (PMID:26234562)
  • PFTK1 overexpression promoted proliferation, migration and invasion of gastric cancer cells, while PFTK1 knockdown led to the opposite results. (PMID:26488471)
  • The expression level of PFTK1 was correlated with tumor grade, FIGO stage, lymph node metastasis of EOC patients as well as poor prognosis. (PMID:26772918)
  • Knockdown of PFTK1 inhibited the proliferation and invasion of pancreatic cancer cells as well as the EMT progress by suppressing the PI3K/Akt signaling pathway. (PMID:26823712)
  • these results suggest that knockdown of PFTK1 inhibited the proliferation and invasion of colon cancer cells as well as the EMT progress by suppressing the Sonic hedgehog signaling pathway. (PMID:27458094)
  • we report that PFTK1 downregulation might inhibit the proliferation and invasion of NSCLC cells by suppressing the Wnt/beta-catenin signaling pathway. (PMID:27458099)
  • findings revealed an unrecognized role of Caprin-2 in facilitating LRP5/6 constitutive phosphorylation at G2/M through forming a quaternary complex with CDK14, Cyclin Y, and LRP5/6. (PMID:27821587)
  • miR-455 inhibits breast cancer cell proliferation through targeting CDK14 (PMID:28300591)
  • PFTK1 expression is significantly higher in CRC tissues compared with matched adjacent noncancerous colorectal tissues. The associations between PFTK1 expression and clinicopathological characters, and PFTK1 expression and the OS rate following resection suggested that PFTK1 may represent a novel biomarker of poor prognosis in CRC (PMID:28498444)
  • CDK14 expression was closely associated with poor prognosis and overall survival of Osteosarcoma patients. miR-216a inhibits CDK14 expression by binding to the 3’-untranslated region of CDK14. (PMID:29022909)
  • Results show that CDK14 and DYRK2 expression were inversely correlated in human breast cancer tissues and identified CDK14 as a target of DYRK2. (PMID:29193658)
  • CDK14 mediated miR-1202 to exert its anti-tumor effects. (PMID:29217161)
  • Data suggest the risk-associated single nucleotide polymorphism (SNP) rs10272859 of cyclin dependent kinase 14 (CDK14) gene at 7q21.13 conferring both susceptibility and prognosis to HBV-related hepatocellular carcinoma (HCC). (PMID:29246937)
  • MiR-431 expression was reduced both in pancreatic cancer tissues and cell lines. Cell proliferative ability was effectively lessened after up-regulating miR-431. Elevated miR-431 significantly induced cell apoptosis and modulated cell cycle arrest. Meanwhile, CDK14 was a direct target gene of miR-431, and over-expression of miR-431 decreased the level of CDK14. (PMID:30058687)
  • OIP5-AS1 acts as a miR-223 ‘sponge’ to trigger CDK14 expression to promote osteosarcoma tumorigenesis. (PMID:30119217)
  • knockdown of E2F5 and PFTK1 mimicked the tumor-suppressive effects of miR-1-3p overexpression on PCa progression. Conversely, concomitant knockdown of miR-1-3p and E2F5 and PFTK1 substantially reversed the inhibitory effects of either E2F5 or PFTK1 silencing alone. (PMID:30185212)
  • LncRNA H19/miR-194/PFTK1 axis modulates the cell proliferation and migration of pancreatic cancer. (PMID:30474270)
  • our findings indicated that NEAT1/miR-107/CDK14 axis participated in glioma development. NEAT1 could act as a significant prognostic biomarker in glioma progression. (PMID:30480816)
  • CDK14 overexpression reversed the suppressive effects of miR-542-3p in ovarian cancer cells. (PMID:30557834)
  • we demonstrated that MSC-AS1/miR-29b-3p axis modulates the cell proliferation and GEM-induced cell apoptosis in PDAC cell lines through CDK14. We provided a novel experimental basis for PDAC treatment from the perspective of lncRNA-miRNA-mRNA network. (PMID:30915884)
  • Upregulation of miR-1825 inhibits the progression of glioblastoma by suppressing CDK14 though Wnt/beta-catenin signaling pathway. (PMID:32605563)
  • CircCDK14 protects against Osteoarthritis by sponging miR-125a-5p and promoting the expression of Smad2. (PMID:32802182)
  • MiR-205 Inhibits Sporadic Vestibular Schwannoma Cell Proliferation by Targeting Cyclin-Dependent Kinase 14. (PMID:33217595)
  • LncRNA NORAD accelerates the progression of non-small cell lung cancer via targeting miRNA-455/CDK14 axis. (PMID:33764714)
  • Depletion of circRNA circ_CDK14 inhibits osteosarcoma progression by regulating the miR-520a-3p/GAB1 axis. (PMID:34348465)
  • CircCDK14 Promotes Tumor Progression and Resists Ferroptosis in Glioma by Regulating PDGFRA. (PMID:35002529)
  • P300/SP1 complex mediating elevated METTL1 regulates CDK14 mRNA stability via internal m7G modification in CRPC. (PMID:37599359)
  • Genetic and pharmacological reduction of CDK14 mitigates synucleinopathy. (PMID:38575601)
  • N6-methyladenosine-modified circCDK14 promotes ossification of the ligamentum flavum via epigenetic modulation by targeting AFF4. (PMID:39414635)

Cross-species orthologs

3 orthologs

OrganismSymbolGene ID
danio_reriocdk14ENSDARG00000074665
mus_musculusCdk14ENSMUSG00000028926
rattus_norvegicusCdk14ENSRNOG00000007151

Paralogs (26): CDKL3 (ENSG00000006837), CDKL5 (ENSG00000008086), CDK11A (ENSG00000008128), CDK17 (ENSG00000059758), CDK13 (ENSG00000065883), CDKL1 (ENSG00000100490), CDK16 (ENSG00000102225), CDK6 (ENSG00000105810), PRP4K (ENSG00000112739), CDK18 (ENSG00000117266), CDK2 (ENSG00000123374), CDK8 (ENSG00000132964), CDK7 (ENSG00000134058), CDK4 (ENSG00000135446), CDK9 (ENSG00000136807), CDK15 (ENSG00000138395), CDKL2 (ENSG00000138769), CDK19 (ENSG00000155111), CDK20 (ENSG00000156345), CDK5 (ENSG00000164885), CDK12 (ENSG00000167258), CDK1 (ENSG00000170312), CDK10 (ENSG00000185324), CDKL4 (ENSG00000205111), CDK11B (ENSG00000248333), CDK3 (ENSG00000250506)

Protein

Protein identifiers

Cyclin-dependent kinase 14O94921 (reviewed: O94921)

Alternative names: Cell division protein kinase 14, Serine/threonine-protein kinase PFTAIRE-1

All UniProt accessions (5): O94921, C9IYJ9, C9JWL6, E7EUK8, F8WF96

UniProt curated annotations — full annotation on UniProt →

Function. Serine/threonine-protein kinase involved in the control of the eukaryotic cell cycle, whose activity is controlled by an associated cyclin. Acts as a cell-cycle regulator of Wnt signaling pathway during G2/M phase by mediating the phosphorylation of LRP6 at ‘Ser-1490’, leading to the activation of the Wnt signaling pathway. Acts as a regulator of cell cycle progression and cell proliferation via its interaction with CCDN3. Phosphorylates RB1 in vitro, however the relevance of such result remains to be confirmed in vivo. May also play a role in meiosis, neuron differentiation and may indirectly act as a negative regulator of insulin-responsive glucose transport.

Subunit / interactions. Found in a complex with LRP6, CCNY and CAPRIN2 during G2/M stage; CAPRIN2 functions as a scaffold for the complex by binding to CCNY via its N terminus and to CDK14 via its C terminus. Interacts with CCNY; CCNY mediates its recruitment to the plasma membrane and promotes phosphorylation of LRP6. Interacts with CCDN3 and CDKN1A. Interacts with SEPT8. Interacts with 14-3-3 proteina YWHAB, YWHAE, YWHAH and YWHAQ.

Subcellular location. Cell membrane. Cytoplasm. Nucleus.

Tissue specificity. Highly expressed in brain, pancreas, kidney, heart, testis and ovary. Also detected at lower levels in other tissues except in spleen and thymus where expression is barely detected.

Activity regulation. Serine/threonine-protein kinase activity is promoted by associated cyclins CCDN3 and CCNY and repressed by CDKN1A.

Similarity. Belongs to the protein kinase superfamily. CMGC Ser/Thr protein kinase family. CDC2/CDKX subfamily.

Isoforms (3)

UniProt IDNamesCanonical?
O94921-11yes
O94921-22
O94921-33

RefSeq proteins (4): NP_001274064, NP_001274065, NP_001274066, NP_036527 (=MANE)

Domains & families (InterPro)

IDNameType
IPR000719Prot_kinase_domDomain
IPR008271Ser/Thr_kinase_ASActive_site
IPR011009Kinase-like_dom_sfHomologous_superfamily
IPR017441Protein_kinase_ATP_BSBinding_site
IPR050108CDKFamily

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): modified residue 4, splice variant 2, sequence variant 2, sequence conflict 2, region of interest 2, binding site 2, chain 1, domain 1, mutagenesis site 1, compositionally biased region 1, active site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O94921-F171.100.50

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): 256 (proton acceptor)

Ligand- & substrate-binding residues (2): 141–149; 164

Post-translational modifications (4): 95, 134, 24, 78

Mutagenesis-validated functional residues (1):

PositionPhenotype
164abolishes protein kinase activity.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 332 (showing top): DAVIES_MULTIPLE_MYELOMA_VS_MGUS_DN, AP1_01, FAELT_B_CLL_WITH_VH_REARRANGEMENTS_DN, GAANYNYGACNY_UNKNOWN, AREB6_03, KAAB_HEART_ATRIUM_VS_VENTRICLE_UP, GOBP_CELL_CYCLE_PHASE_TRANSITION, GEORGES_CELL_CYCLE_MIR192_TARGETS, TGACCTY_ERR1_Q2, GOBP_REGULATION_OF_WNT_SIGNALING_PATHWAY, EVI1_05, GOBP_CANONICAL_WNT_SIGNALING_PATHWAY, SASSON_RESPONSE_TO_FORSKOLIN_DN, GOBP_REGULATION_OF_CELL_CYCLE, CAATGCA_MIR33

GO Biological Process (6): G2/M transition of mitotic cell cycle (GO:0000086), Wnt signaling pathway (GO:0016055), cell division (GO:0051301), regulation of canonical Wnt signaling pathway (GO:0060828), regulation of cell cycle phase transition (GO:1901987), protein phosphorylation (GO:0006468)

GO Molecular Function (11): cyclin-dependent protein serine/threonine kinase activity (GO:0004693), ATP binding (GO:0005524), cyclin binding (GO:0030332), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), heme binding (GO:0020037)

GO Cellular Component (8): cyclin-dependent protein kinase holoenzyme complex (GO:0000307), cytoplasmic cyclin-dependent protein kinase holoenzyme complex (GO:0000308), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure4
protein kinase activity2
cytoplasm2
mitotic cell cycle1
mitotic cell cycle phase transition1
cell cycle G2/M phase transition1
cell surface receptor signaling pathway1
cellular process1
regulation of Wnt signaling pathway1
canonical Wnt signaling pathway1
regulation of cell cycle process1
cell cycle phase transition1
phosphorylation1
protein modification process1
protein serine/threonine kinase activity1
cyclin-dependent protein kinase activity1
adenyl ribonucleotide binding1
purine ribonucleoside triphosphate binding1
protein 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
tetrapyrrole binding1
serine/threonine protein kinase complex1
cyclin-dependent protein kinase holoenzyme complex1
intracellular membrane-bounded organelle1
nuclear lumen1
intracellular anatomical structure1
membrane1
cell periphery1

Protein interactions and networks

STRING

2983 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
CDK14CCNYQ8ND76992
CDK14CCND3P30281756
CDK14AKT3Q9Y243610
CDK14CCNL2Q96S94602
CDK14CCNYL1Q8N7R7573
CDK14YWHAHQ04917458
CDK14YWHABP31946453
CDK14LRP6O75581439
CDK14ZNF148Q9UQR1439
CDK14SFNP31947422
CDK14YWHAQP27348421
CDK14CILK1Q9UPZ9420
CDK14YWHAEP29360415
CDK14GPATCH3Q96I76408
CDK14RSPRY1Q96DX4399

IntAct

62 interactions, top by confidence:

ABTypeScore
CDK5FIBPpsi-mi:“MI:0914”(association)0.840
YWHABPIK3C2Apsi-mi:“MI:0914”(association)0.800
YWHAHCDK14psi-mi:“MI:0915”(physical association)0.780
CDK14YWHAHpsi-mi:“MI:0915”(physical association)0.780
CDKN1ACDK14psi-mi:“MI:0915”(physical association)0.770
CDK14CDKN1Apsi-mi:“MI:0915”(physical association)0.770
CDKN1ACDK14psi-mi:“MI:0914”(association)0.770
CDK14CDKN1Apsi-mi:“MI:0914”(association)0.770
CDK14YWHABpsi-mi:“MI:0915”(physical association)0.750
YWHABCDK14psi-mi:“MI:0915”(physical association)0.750
YWHAQCDK14psi-mi:“MI:0915”(physical association)0.720
CDK14YWHAQpsi-mi:“MI:0915”(physical association)0.720
YWHAGBLTP3Bpsi-mi:“MI:0914”(association)0.640
ELL3CCNT1psi-mi:“MI:0914”(association)0.640
CDK14YWHAEpsi-mi:“MI:0915”(physical association)0.630
YWHAECDK14psi-mi:“MI:0915”(physical association)0.630
CDK14CCND3psi-mi:“MI:0915”(physical association)0.620
CCND3CDK14psi-mi:“MI:0915”(physical association)0.620
CDK14CCND3psi-mi:“MI:0914”(association)0.620

BioGRID (90): CDK14 (Affinity Capture-MS), HSP90AA5P (Affinity Capture-MS), CDK17 (Affinity Capture-MS), ICK (Affinity Capture-MS), CDKN1A (Affinity Capture-MS), CDK14 (Affinity Capture-MS), CDK14 (Affinity Capture-MS), ICK (Affinity Capture-MS), FGR (Affinity Capture-MS), CDKN1A (Affinity Capture-MS), CDK17 (Affinity Capture-MS), CDK14 (Affinity Capture-MS), CDK14 (Affinity Capture-MS), HSP90AA5P (Affinity Capture-MS), CDK14 (Affinity Capture-MS)

ESM2 similar proteins: A0A8I3S724, A4IGM9, A4IIW7, A5GFW1, B0VXL7, B6A7Q3, C0RW22, D7UQM5, F4I4F2, O08605, O14965, O35495, O55099, O59790, O70126, O80673, O94921, P18266, P27466, P49841, P59241, P97477, Q00771, Q0VD22, Q13555, Q16566, Q2TA06, Q501Q9, Q58D94, Q5XIT0, Q66JF3, Q6BVA0, Q6C3J2, Q6CWQ4, Q6DE08, Q6DGS3, Q6GPL3, Q6Z8C8, Q755C4, Q7YRC6

Diamond homologs: A4IIW7, A8XA58, B0VXE8, B0VXL7, B6A7Q3, C0RW22, G5ECH7, O35495, O35831, O35832, O55076, O61847, O74456, O94921, O96821, P00546, P04551, P06493, P11440, P13863, P17157, P23111, P23437, P23572, P23573, P24033, P24100, P24923, P24941, P25859, P29618, P29619, P34112, P34117, P35567, P38973, P39951, P43063, P43450, P48609

SIGNOR signaling

8 interactions.

AEffectBMechanism
CCNYup-regulatesCDK14binding
CDK14up-regulatesLRP6phosphorylation
CDK14“down-regulates quantity by destabilization”CCNYphosphorylation
CDK14“down-regulates activity”TAGLN2phosphorylation
CDK14“form complex”CyclinY/CDK14binding
CDK14“up-regulates activity”LRP6

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 32 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
Activation of BAD and translocation to mitochondria6169.2×8e-11
Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex6149.3×1e-10
SARS-CoV-1 targets host intracellular signalling and regulatory pathways6149.3×1e-10
Activation of BH3-only proteins6110.3×5e-10
FOXO-mediated transcription674.6×5e-09
RHO GTPases activate PKNs670.5×7e-09
Intrinsic Pathway for Apoptosis665.1×1e-08
SARS-CoV-1-host interactions639.0×2e-07

GO biological processes:

GO termPartnersFoldFDR
protein targeting561.1×6e-06
intracellular protein localization620.9×6e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance58
Likely benign3
Benign2

Top pathogenic / likely-pathogenic (0)

SpliceAI

3576 predictions. Top by Δscore:

VariantEffectΔscore
7:90596701:A:Tdonor_gain1.0000
7:90596714:CATTG:Cdonor_gain1.0000
7:90596715:ATTG:Adonor_gain1.0000
7:90596716:TTG:Tdonor_gain1.0000
7:90596717:TG:Tdonor_gain1.0000
7:90596717:TGG:Tdonor_loss1.0000
7:90596718:GG:Gdonor_gain1.0000
7:90596718:GGT:Gdonor_loss1.0000
7:90596719:G:GGdonor_gain1.0000
7:90596719:GTG:Gdonor_loss1.0000
7:90596720:T:Adonor_loss1.0000
7:90604215:T:Gacceptor_gain1.0000
7:90604216:A:AGacceptor_gain1.0000
7:90604217:G:GAacceptor_gain1.0000
7:90720946:T:Gdonor_gain1.0000
7:90726562:CTCA:Cacceptor_loss1.0000
7:90726562:CTCAG:Cacceptor_gain1.0000
7:90726563:TCA:Tacceptor_loss1.0000
7:90726563:TCAGA:Tacceptor_gain1.0000
7:90726564:CA:Cacceptor_loss1.0000
7:90726564:CAG:Cacceptor_gain1.0000
7:90726565:A:AGacceptor_gain1.0000
7:90726565:A:Cacceptor_gain1.0000
7:90726566:G:GGacceptor_gain1.0000
7:90726566:G:Tacceptor_gain1.0000
7:90726566:GA:Gacceptor_gain1.0000
7:90726566:GAT:Gacceptor_gain1.0000
7:90726566:GATA:Gacceptor_gain1.0000
7:90726566:GATAT:Gacceptor_gain1.0000
7:90726808:GCTCG:Gdonor_gain1.0000

AlphaMissense

3090 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
7:90747700:G:AG130E1.000
7:90747714:T:CY135H1.000
7:90747714:T:GY135D1.000
7:90747735:G:AG142R1.000
7:90747735:G:CG142R1.000
7:90747735:G:TG142W1.000
7:90747736:G:AG142E1.000
7:90747736:G:TG142V1.000
7:90747741:G:AG144R1.000
7:90747741:G:CG144R1.000
7:90747742:G:AG144E1.000
7:90747742:G:CG144A1.000
7:90747742:G:TG144V1.000
7:90747747:T:CY146H1.000
7:90747750:G:CA147P1.000
7:90747751:C:AA147D1.000
7:90747751:C:TA147V1.000
7:90747756:G:CV149L1.000
7:90747756:G:TV149L1.000
7:90747757:T:AV149E1.000
7:90747757:T:CV149A1.000
7:90747765:G:AG152R1.000
7:90747765:G:CG152R1.000
7:90747765:G:TG152W1.000
7:90747766:G:AG152E1.000
7:90790593:C:AA162D1.000
7:90790596:T:CL163P1.000
7:90790598:A:CK164Q1.000
7:90790598:A:GK164E1.000
7:90790599:A:CK164T1.000

dbSNP variants (sampled 300 via entrez): RS1000000124 (7:90808588 A>C,G), RS1000002381 (7:91010553 T>C), RS1000005396 (7:91190235 T>C), RS1000009321 (7:90896895 T>C), RS1000013991 (7:91097103 G>A), RS1000016533 (7:90969360 C>A,T), RS1000016967 (7:91033736 A>G), RS1000026835 (7:90888081 A>G), RS1000028586 (7:90686939 C>G), RS1000029264 (7:90678440 G>C), RS1000030930 (7:90601714 G>T), RS1000032657 (7:90765296 A>G), RS1000044041 (7:90603752 A>C), RS1000050859 (7:91141564 G>T), RS1000053545 (7:90915511 A>C,G)

Disease associations

OMIM: gene MIM:610679 | disease phenotypes: MIM:209850

GenCC curated gene-disease

Mondo (1): autism (MONDO:0005260)

Orphanet (0):

HPO phenotypes

1 total (1 of 1 shown, HPO-id order):

HPOTerm
HP:0000717Autism

GWAS associations

7 associations (top):

StudyTraitp-value
GCST002707_8Serum thyroid-stimulating hormone levels5.000000e-06
GCST004361_1Estrone/androstenedione ratio in resected early stage-receptor positive breast cancer1.000000e-06
GCST005570_1Hepatitis B virus-related hepatocellular carcinoma9.000000e-10
GCST006491_18Circulating fibroblast growth factor 23 levels2.000000e-06
GCST006626_4Pulse pressure1.000000e-13
GCST007269_273Pulse pressure3.000000e-09
GCST010396_95Gut microbiota (bacterial taxa, hurdle binary method)1.000000e-06

EFO canonical traits (4, from GWAS)

EFO IDTrait name
EFO:0007970estrone measurement
EFO:0007972androstenedione measurement
EFO:0005763pulse pressure measurement
EFO:0007874gut microbiome measurement

MeSH disease descriptors (1)

DescriptorNameTree numbers
D001321Autistic DisorderF03.625.164.113.500

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL3559691 (PROTEIN FAMILY), CHEMBL4296115 (PROTEIN COMPLEX), CHEMBL6162 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

17 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 229,940 (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
CHEMBL1336SORAFENIB486,060
CHEMBL288441BOSUTINIB412,255
CHEMBL502835NINTEDANIB48,545
CHEMBL535SUNITINIB479,020
CHEMBL300138ENZASTAURIN33,209
CHEMBL428690ALVOCIDIB327,781
CHEMBL603469LESTAURTINIB3
CHEMBL1276127INDIRUBIN2181
CHEMBL445813AT-751922,614
CHEMBL5199065ISTISOCICLIB221
CHEMBL1230609FORETINIB23,096
CHEMBL1721885SU-0148132363
CHEMBL384304RG-547293
CHEMBL1908397KW-24491622
CHEMBL296468BMS-38703212,075
CHEMBL574738AST-4871451

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — TAIRE subfamily

Binding affinities (BindingDB)

7 measured of 7 human assays (7 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
StaurosporineKD1.7 nM
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamideKD370 nM
1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]ureaKD1400 nM
BMS-387072KD1800 nM
1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3bKD3100 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
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S)-3-hydroxy-1-methyl-4-piperidinyl]-1-benzopyran-4-oneKD5300 nM

ChEMBL bioactivities

114 potent at pChembl≥5 of 115 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.40IC500.4nMCHEMBL4563703
9.10IC500.8nMCHEMBL4535078
8.80IC501.6nMCHEMBL4446451
8.74IC501.8nMCHEMBL4522598
8.59IC502.6nMCHEMBL4515515
8.52IC503nMCHEMBL4542127
8.52IC503nMCHEMBL4530961
8.47IC503.4nMCHEMBL4527767
8.19IC506.4nMCHEMBL4579572
8.00IC5010nMCHEMBL4519165
7.96IC5011nMCHEMBL4456492
7.96Kd11nMRG-547
7.85IC5014nMCHEMBL4459422
7.85IC5014nMCHEMBL4563705
7.80Kd16nMAT-7519
7.79IC5016.1nMCHEMBL6144731
7.77IC5017nMCHEMBL4555069
7.77Kd17nMAST-487
7.70IC5019.8nMAT-7519
7.57IC5027nMCHEMBL4589122
7.51Kd31nMFORETINIB
7.47IC5034nMCHEMBL4473682
7.41IC5039nMCHEMBL4580787
7.40IC5039.6nMCHEMBL4434727
7.39IC5041nMCHEMBL4584359
7.35IC5045nMCHEMBL4554744
7.35IC5045nMCHEMBL4576258
7.32IC5048nMCHEMBL4544087
7.31IC5049nMCHEMBL4474689
7.30IC5050nMCHEMBL4464758
7.30IC5050nMCHEMBL4522598
7.30IC5050nMCHEMBL4542127
7.21IC5062nMCHEMBL4586749
7.20IC5062.7nMCHEMBL4856177
7.17IC5068nMCHEMBL4583677
7.14IC5072nMCHEMBL4466362
7.11IC5077nMCHEMBL4459085
7.11IC5078.4nMCHEMBL4848734
7.09IC5082nMCHEMBL4447871
7.09IC5082nMCHEMBL4466865
7.08IC5083nMCHEMBL4556640
7.08IC5083.8nMSTAUROSPORINE
7.06IC5088nMCHEMBL4580787
7.06IC5088nMCHEMBL4435761
7.06IC5088nMCHEMBL4434727
7.00IC50101nMSTAUROSPORINE
6.97IC50108nMCHEMBL4536978
6.96Kd110nMALVOCIDIB
6.93IC50117nMCHEMBL4561411
6.90IC50126nMCHEMBL4444448

PubChem BioAssay actives

112 with measured affinity, of 440 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
4-[(2,6-dichloro-3-methoxybenzoyl)amino]-N-[1-[3-(prop-2-enoylamino)phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0004uM
4-[(2-chloro-6-methoxybenzoyl)amino]-N-[1-[3-(prop-2-enoylamino)phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0008uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[[3-(prop-2-enoylamino)phenyl]methyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0010uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[3-(prop-2-enoylamino)phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0010uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]methyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0010uM
4-[(2-fluoro-6-methoxybenzoyl)amino]-N-[1-[3-(prop-2-enoylamino)phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0016uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0018uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0026uM
4-benzamido-N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0030uM
4-[(2-chloro-6-methoxybenzoyl)amino]-N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0030uM
4-[(2,6-difluorobenzoyl)amino]-N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0034uM
4-[(2,6-dichloro-3-methoxybenzoyl)amino]-N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0064uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[[4-(prop-2-enoylamino)phenyl]methyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0100uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[3-(propanoylamino)phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0110uM
[4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone625070: Binding constant for PFTK1 kinase domainkd0.0110uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[[4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]methyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0140uM
N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-4-[[2-(2-methoxyphenyl)acetyl]amino]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0140uM
4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide625070: Binding constant for PFTK1 kinase domainkd0.0160uM
1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea435689: Binding constant for full-length PFTK1kd0.0170uM
4-[(2,6-dichlorobenzoyl)amino]-N-[4-[[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzoyl]amino]phenyl]-1H-pyrazole-3-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0170uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[3-[[(E)-5-(dimethylamino)pent-2-enoyl]amino]phenyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0270uM
1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide625070: Binding constant for PFTK1 kinase domainkd0.0310uM
4-[(2,6-dichlorobenzoyl)amino]-N-[3-[[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzoyl]amino]phenyl]-1H-pyrazole-3-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0340uM
N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-4-[(2,4,6-trichlorobenzoyl)amino]-1H-pyrazole-5-carboxamide1890188: Inhibition of CDK14 (unknown origin) incubated for 6 hrs by NanoBRET assayic500.0390uM
N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-4-[(2,4,6-trichlorobenzoyl)amino]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633948: Inhibition of recombinant NanoLuc-tagged CDK14/cyclin Y expressed in human HCT116 cells at 1 uM incubated for 20 to 24 hrs by by NanoBRET assayic500.0396uM
4-[(2,6-dichlorobenzoyl)amino]-N-[(3R)-1-[4-[[(E)-5-(dimethylamino)pent-2-enoyl]amino]phenyl]sulfonylpyrrolidin-3-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0410uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[4-[[(E)-5-(dimethylamino)pent-2-enoyl]amino]phenyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0450uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[3-(prop-2-enoylamino)benzoyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0450uM
N-[1-[3-(prop-2-enoylamino)phenyl]sulfonylpiperidin-4-yl]-4-[(2,4,6-trimethoxybenzoyl)amino]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0480uM
N-[1-[3-(prop-2-enoylamino)phenyl]sulfonylpiperidin-4-yl]-4-[(2,4,6-trichlorobenzoyl)amino]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0490uM
4-[(2,6-dimethoxybenzoyl)amino]-N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0500uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[4-(prop-2-enoylamino)phenyl]sulfonylpiperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0620uM
4-(4-methylpiperazin-1-yl)-N-[4-(2-methyl-3-propan-2-ylindazol-5-yl)pyrimidin-2-yl]quinolin-7-amine1771107: Inhibition of human CDK14/cyclin-Y using RB protein as substrate incubated for 2 hrs by [gamma-33P]-ATP assayic500.0627uM
4-[(2,6-dichlorobenzoyl)amino]-N-[4-[[4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzoyl]amino]phenyl]-1H-pyrazole-3-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0680uM
4-[(2,6-dichlorobenzoyl)amino]-N-[3-[[4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzoyl]amino]phenyl]-1H-pyrazole-3-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0720uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzoyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0770uM
3-acetyl-7-[[4-(2-methyl-3-propan-2-ylindazol-5-yl)pyrimidin-2-yl]amino]-4-morpholin-4-ylchromen-2-one1771107: Inhibition of human CDK14/cyclin-Y using RB protein as substrate incubated for 2 hrs by [gamma-33P]-ATP assayic500.0784uM
4-[(2,6-dichlorobenzoyl)amino]-N-[4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0820uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[[3-(propanoylamino)phenyl]methyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0820uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzoyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0830uM
(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-one2198169: Inhibition of human CDK14/cyclin Y using RB Protein as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by radiometric Hot-SpotSM Kinase assayic500.0838uM
4-[(2,6-dichlorobenzoyl)amino]-N-[3-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.0880uM
4-[(2,6-dichlorobenzoyl)amino]-N-[[4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]methyl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.1080uM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one435689: Binding constant for full-length PFTK1kd0.1100uM
4-[(2,6-dichlorobenzoyl)amino]-N-[(3R)-1-[4-[[(E)-5-(dimethylamino)pent-2-enoyl]amino]phenyl]pyrrolidin-3-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.1170uM
4-[(2,6-dichlorobenzoyl)amino]-N-[1-[4-(prop-2-enoylamino)benzoyl]piperidin-4-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.1260uM
4-[(2,6-dichlorobenzoyl)amino]-N-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]piperidin-3-yl]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.1480uM
N-[(3R)-1-[[3-[[(E)-but-2-enoyl]amino]phenyl]methyl]pyrrolidin-3-yl]-4-[(2,6-dichlorobenzoyl)amino]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.1510uM
N-[1-[4-[[(E)-but-2-enoyl]amino]phenyl]piperidin-4-yl]-4-[(2,6-dichlorobenzoyl)amino]-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid1633939: Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assayic500.1540uM
N-[3-cyclopropyl-5-[(4-methylpiperazin-1-yl)methyl]phenyl]-5-methyl-18-oxo-9-oxa-17,23,25,26-tetrazatetracyclo[17.5.2.14,8.022,25]heptacosa-1(24),4,6,8(27),19(26),20,22-heptaen-2-yne-6-carboxamide2014049: Inhibition of CDK14 (unknown origin)ic500.1552uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Benzo(a)pyreneaffects methylation, decreases expression, increases methylation5
Valproic Acidaffects expression, decreases expression, decreases methylation3
Aflatoxin B1affects expression, decreases expression, decreases methylation3
Air Pollutantsaffects expression, increases abundance, decreases expression2
Smokeincreases abundance, decreases expression2
Tretinoindecreases expression, increases expression2
Cyclosporinedecreases expression, decreases methylation2
aristolochic acid Idecreases expression1
geldanamycinincreases expression1
methyleugenoldecreases expression1
bisphenol Aaffects methylation1
trichostatin Adecreases expression1
arseniteaffects binding, decreases reaction1
sodium arsenitedecreases expression1
ochratoxin Adecreases acetylation, decreases expression1
benzo(e)pyreneaffects methylation1
potassium chromate(VI)decreases expression1
nickel sulfatedecreases expression1
coumarinincreases phosphorylation1
di-n-butylphosphoric acidaffects expression1
perfluorooctane sulfonic aciddecreases expression1
CGP 52608increases reaction, affects binding1
3-nitrobenzanthronedecreases expression1
torcetrapibincreases expression1
bisphenol Saffects cotreatment, decreases expression1
jinfukangaffects cotreatment, decreases expression1
Temozolomidedecreases expression1
Vorinostatdecreases expression1
Acetaminophendecreases expression1
Cisplatinaffects cotreatment, decreases expression1

ChEMBL screening assays

179 unique, capped per target: 179 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1064257BindingInhibition of CDK in human A2780 cells assessed as reduction of RNAP2 phosphorylation at Ser2 site at 5 uM after 6 hrs by Western blotingDesign, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors. — J Med Chem

Cellosaurus cell lines

1 cell lines: 1 cancer cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_SI24HAP1 CDK14 (-)Cancer cell lineMale

Clinical trials (associated diseases)

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

TrialPhaseStatusTitle
NCT00211796PHASE4COMPLETEDDivalproex Sodium ER in Adult Autism
NCT00391261PHASE4COMPLETEDAn Open-label Trial of Metformin for Weight Control of Pediatric Patients on Antipsychotic Medications.
NCT00409747PHASE4COMPLETEDMinocycline to Treat Childhood Regressive Autism
NCT00576732PHASE4COMPLETEDA Study of the Effectiveness and Safety of Two Doses of Risperidone in the Treatment of Children and Adolescents With Autistic Disorder
NCT00844753PHASE4COMPLETEDAtomoxetine, Placebo and Parent Management Training in Autism
NCT01028820PHASE4COMPLETEDFMRI Brain Activation of Aripiprazole Treatment in Autism Spectrum Disorders
NCT01098383PHASE4UNKNOWNTreatment With Acetyl-Choline Esterase Inhibitors in Children With Autism Spectrum Disorders
NCT01333865PHASE4COMPLETEDA Study of Memantine Hydrochloride (Namenda®) for Cognitive and Behavioral Impairment in Adults With Autism Spectrum Disorders
NCT01337700PHASE4COMPLETEDMilnacipran in Autism and the Functional Locus Coeruleus and Noradrenergic Model of Autism
NCT01695200PHASE4COMPLETEDOmega-3 Fatty Acids in Autism Spectrum Disorders
NCT02069977PHASE4UNKNOWNStudy to Evaluate the Efficacy and Safety of Aripiprazole
NCT02096952PHASE4COMPLETEDMethylphenidate ER Liquid Formulation in Adults With ASD and ADHD
NCT02199925PHASE4UNKNOWNAn Open-Label Study to Evaluate the Efficacy of High-Dose Gammaplex in Children on the Autism Spectrum
NCT02235467PHASE4COMPLETEDMultisite Study: Parental Training Using Video Modelling to Develop Social Skills in Children With Autism
NCT02255565PHASE4COMPLETEDDose Response Effects of Quillivant XR in Children With ADHD and Autism: A Pilot Study
NCT02940574PHASE4COMPLETEDNeural and Behavioral Effects of Oxytocin in Autism Spectrum Disorders
NCT03333629PHASE4COMPLETEDPromoting Positive Outcomes for Individuals With ASD: Linking Early Detection, Treatment, and Long-term Outcomes
NCT03337646PHASE4COMPLETEDEvaluation of the Effect and Safety of Lisdexamfetamine in Children Aged 6-12 With ADHD and Autism
NCT03538431PHASE4COMPLETEDImproving Driving in Young People With Autism Spectrum Disorders
NCT03757585PHASE4COMPLETEDNatural Treatments for the Management of Emotional Dysregulation in Youth With Non-verbal Learning Disability (NVLD) and/or Autism Spectrum Disorders (ASD)
NCT04903353PHASE4COMPLETEDPragmatic Trial Comparing Weight Gain in Children With Autism Taking Risperidone Versus Aripiprazole
NCT05063656PHASE4COMPLETEDBiomarker-Driven Pharmacological Treatment of Adolescents With Autism Spectrum Disorder With Gabapentin
NCT05146245PHASE4UNKNOWNSafety and Pharmacokinetics of Antipsychotics in Children 2: Studying TDM in an RCT
NCT05916339PHASE4RECRUITINGAWARE: Management of ADHD in Autism Spectrum Disorder
NCT05954052PHASE4TERMINATEDA Study of Glutathione in Children With Autism Spectrum Disorder
NCT06853665PHASE4RECRUITINGThe TEAM Study - Treatment Efficacy for Autism/Attention Using Mixed Amphetamine
NCT07054697PHASE4COMPLETEDPilot-RCT With Individualized Homeopathic Treatment in the Children With Autism Spectrum Disorder
NCT07161804PHASE4COMPLETEDPilot RCT Using Homeopathic Medicines in ASD
NCT07439042PHASE4NOT_YET_RECRUITINGBuspirone for Anxiety in Autistic Youth
NCT00036231PHASE3TERMINATEDSynthetic Human Secretin in Children With Autism and Gastrointestinal Dysfunction
NCT00036244PHASE3COMPLETEDSynthetic Human Secretin in Children With Autism
NCT00065884PHASE3UNKNOWNValproate Response in Aggressive Autistic Adolescents
NCT00065962PHASE3COMPLETEDSecretin for the Treatment of Autism
NCT00252603PHASE3COMPLETEDGalantamine Versus Placebo in Childhood Autism
NCT00346736PHASE3COMPLETEDUse of Acupuncture In Children With Autistic Spectrum Disorder
NCT00352248PHASE3COMPLETEDRandomized Controlled Trial of Acupuncture Versus Sham Acupuncture in Autistic Spectrum Disorder
NCT00352352PHASE3COMPLETEDUse of Acupuncture In Children With Autistic Spectrum Disorder
NCT00355329PHASE3COMPLETEDRandomized Control Trial of Using Tongue Acupuncture in Autistic Spectrum Disorder Using PET Scan for Clinical Correlation
NCT00498173PHASE3COMPLETEDEffectiveness of Atomoxetine in Treating ADHD Symptoms in Children and Adolescents With Autism
NCT00541346PHASE3COMPLETEDA Pilot Study of Daytrana TM in Children With Autism Co-Morbid for Attention Deficit Hyperactivity Disorder (ADHD) Symptoms