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Target Report Card

Target Name and Classification

Target ID CHEMBL3142
Preferred Name DNA-dependent protein kinase
Synonyms DNA-PK catalytic subunit | DNA-PKcs | DNA-dependent protein kinase catalytic subunit | DNPK1 | HYRC | HYRC1 | PRKDC | p460
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > atypical protein kinase group > atypical protein kinase pikk family

Target Components

Component Description Relationship Accession
DNA-dependent protein kinase catalytic subunit SINGLE PROTEIN P78527

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL3545426 CC-115 DNA-dependent protein kinase inhibitor 2 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000253729
Ensembl ENSG00000253729
GO Cellular Component GO:0000784 (nuclear chromosome, telomeric region)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005667 (transcription factor complex)
GO:0005730 (nucleolus)
GO:0005829 (cytosol)
GO:0005958 (DNA-dependent protein kinase-DNA ligase 4 complex)
GO:0016020 (membrane)
GO:0032991 (macromolecular complex)
GO:0032993 (protein-DNA complex)
GO:0070419 (nonhomologous end joining complex)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0003677 (DNA binding)
GO:0003690 (double-stranded DNA binding)
GO:0003723 (RNA binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0004677 (DNA-dependent protein kinase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008134 (transcription factor binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019899 (enzyme binding)
GO:0019904 (protein domain specific binding)
GO Biological Process GO:0000723 (telomere maintenance)
GO:0001756 (somitogenesis)
GO:0001933 (negative regulation of protein phosphorylation)
GO:0002218 (activation of innate immune response)
GO:0002326 (B cell lineage commitment)
GO:0002328 (pro-B cell differentiation)
GO:0002360 (T cell lineage commitment)
GO:0002376 (immune system process)
GO:0002377 (immunoglobulin production)
GO:0002638 (negative regulation of immunoglobulin production)
GO:0002684 (positive regulation of immune system process)
GO:0006281 (DNA repair)
GO:0006302 (double-strand break repair)
GO:0006303 (double-strand break repair via nonhomologous end joining)
GO:0006310 (DNA recombination)
GO:0006464 (cellular protein modification process)
GO:0006468 (protein phosphorylation)
GO:0006974 (cellular response to DNA damage stimulus)
GO:0007420 (brain development)
GO:0007507 (heart development)
GO:0008283 (cell proliferation)
GO:0008630 (intrinsic apoptotic signaling pathway in response to DNA damage)
GO:0010212 (response to ionizing radiation)
GO:0010332 (response to gamma radiation)
GO:0014823 (response to activity)
GO:0016233 (telomere capping)
GO:0016310 (phosphorylation)
GO:0016567 (protein ubiquitination)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0030098 (lymphocyte differentiation)
GO:0031648 (protein destabilization)
GO:0032481 (positive regulation of type I interferon production)
GO:0032869 (cellular response to insulin stimulus)
GO:0033077 (T cell differentiation in thymus)
GO:0033151 (V(D)J recombination)
GO:0033152 (immunoglobulin V(D)J recombination)
GO:0033153 (T cell receptor V(D)J recombination)
GO:0035234 (ectopic germ cell programmed cell death)
GO:0042752 (regulation of circadian rhythm)
GO:0043065 (positive regulation of apoptotic process)
GO:0043066 (negative regulation of apoptotic process)
GO:0045087 (innate immune response)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0048146 (positive regulation of fibroblast proliferation)
GO:0048511 (rhythmic process)
GO:0048536 (spleen development)
GO:0048538 (thymus development)
GO:0048639 (positive regulation of developmental growth)
GO:0048660 (regulation of smooth muscle cell proliferation)
GO:0072431 (signal transduction involved in mitotic G1 DNA damage checkpoint)
GO:0097681 (double-strand break repair via alternative nonhomologous end joining)
GO:2000773 (negative regulation of cellular senescence)
GO:2001229 (negative regulation of response to gamma radiation)
Wikipedia DNA-PKcs

Target Cross References - Protein

canSAR P78527
Human Protein Atlas ENSG00000253729
IntAct P78527
Guide to Pharmacology 2800
Open Targets ENSG00000253729
PharmGKB PA33776
Pharos P78527 (Tchem)
Reactome R-HSA-1834949 (Cytosolic sensors of pathogen-associated DNA.)
R-HSA-3270619 (IRF3-mediated induction of type I IFN.)
R-HSA-5693571 (Nonhomologous End-Joining (NHEJ).)
R-HSA-8866654 (E3 ubiquitin ligases ubiquitinate target proteins.)
UniProt P78527 P78528 Q13327 Q13337 Q14175 Q59H99 Q7Z611 Q96SE6 Q9UME3

Target Cross References - Domain

InterPro IPR000403 (PI3/4_kinase_cat_dom.)
IPR003151 (PIK-rel_kinase_FAT.)
IPR003152 (FATC_dom.)
IPR011009 (Kinase-like_dom_sf.)
IPR012582 (NUC194.)
IPR014009 (PIK_FAT.)
IPR016024 (ARM-type_fold.)
IPR018936 (PI3/4_kinase_CS.)
IPR036940 (PI3/4_kinase_cat_sf.)
IPR037706 (DNA-PK_dom.)
Pfam PF00454 (PI3_PI4_kinase)
PF02259 (FAT)
PF02260 (FATC)
PF08163 (NUC194)

Target Cross References - Structure