Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01142

Target Information
NameDNA-dependent protein kinase catalytic subunit    
Type of targetResearch target    
SynonymsDNA-PK    
DNA-PKcs    
DNA-dependent protein kinase    
DNPK1    
P460    
DiseaseLeukemia, unspecified
[ICD9: 208.9   ICD10: C91-C95]
[1]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.37
PathwayCell cycle
Non-homologous end-joining
UniProt IDP78527
FunctionSer/thr kinase involved in dna double-stranded break repair, v(d)j recombination and modulation of transcription. Must be bound to dna to express its catalytic properties.    
SequenceMAGSGAGVRCSLLRLQETLSAADRCGAALAGHQLIRGLGQECVLSSSPAVLALQTSLVFS RDFGLLVFVRKSLNSIEFRECREEILKFLCIFLEKMGQKIAPYSVEIKNTCTSVYTKDRA AKCKIPALDLLIKLLQTFRSSRLMDEFKIGELFSKFYGELALKKKIPDTVLEKVYELLGL LGEVHPSEMINNAENLFRAFLGELKTQMTSAVREPKLPVLAGCLKGLSSLLCNFTKSMEE DPQTSREIFNFVLKAIRPQIDLKRYAVPSAGLRLFALHASQFSTCLLDNYVSLFEVLLKW CAHTNVELKKAALSALESFLKQVSNMVAKNAEMHKNKLQYFMEQFYGIIRNVDSNNKELS IAIRGYGLFAGPCKVINAKDVDFMYVELIQRCKQMFLTQTDTGDDRVYQMPSFLQSVASV LLYLDTVPEVYTPVLEHLVVMQIDSFPQYSPKMQLVCCRAIVKVFLALAAKGPVLRNCIS TVVHQGLIRICSKPVVLPKGPESESEDHRASGEVRTGKWKVPTYKDYVDLFRHLLSSDQM MDSILADEAFFSVNSSSESLNHLLYDEFVKSVLKIVEKLDLTLEIQTVGEQENGDEAPGV WMIPTSDPAANLHPAKPKDFSAFINLVEFCREILPEKQAEFFEPWVYSFSYELILQSTRL PLISGFYKLLSITVRNAKKIKYFEGVSPKSLKHSPEDPEKYSCFALFVKFGKEVAVKMKQ YKDELLASCLTFLLSLPHNIIELDVRAYVPALQMAFKLGLSYTPLAEVGLNALEEWSIYI DRHVMQPYYKDILPCLDGYLKTSALSDETKNNWEVSALSRAAQKGFNKVVLKHLKKTKNL SSNEAISLEEIRIRVVQMLGSLGGQINKNLLTVTSSDEMMKSYVAWDREKRLSFAVPFRE MKPVIFLDVFLPRVTELALTASDRQTKVAACELLHSMVMFMLGKATQMPEGGQGAPPMYQ LYKRTFPVLLRLACDVDQVTRQLYEPLVMQLIHWFTNNKKFESQDTVALLEAILDGIVDP VDSTLRDFCGRCIREFLKWSIKQITPQQQEKSPVNTKSLFKRLYSLALHPNAFKRLGASL AFNNIYREFREEESLVEQFVFEALVIYMESLALAHADEKSLGTIQQCCDAIDHLCRIIEK KHVSLNKAKKRRLPRGFPPSASLCLLDLVKWLLAHCGRPQTECRHKSIELFYKFVPLLPG NRSPNLWLKDVLKEEGVSFLINTFEGGGCGQPSGILAQPTLLYLRGPFSLQATLCWLDLL LAALECYNTFIGERTVGALQVLGTEAQSSLLKAVAFFLESIAMHDIIAAEKCFGTGAAGN RTSPQEGERYNYSKCTVVVRIMEFTTTLLNTSPEGWKLLKKDLCNTHLMRVLVQTLCEPA SIGFNIGDVQVMAHLPDVCVNLMKALKMSPYKDILETHLREKITAQSIEELCAVNLYGPD AQVDRSRLAAVVSACKQLHRAGLLHNILPSQSTDLHHSVGTELLSLVYKGIAPGDERQCL PSLDLSCKQLASGLLELAFAFGGLCERLVSLLLNPAVLSTASLGSSQGSVIHFSHGEYFY SLFSETINTELLKNLDLAVLELMQSSVDNTKMVSAVLNGMLDQSFRERANQKHQGLKLAT TILQHWKKCDSWWAKDSPLETKMAVLALLAKILQIDSSVSFNTSHGSFPEVFTTYISLLA DTKLDLHLKGQAVTLLPFFTSLTGGSLEELRRVLEQLIVAHFPMQSREFPPGTPRFNNYV DCMKKFLDALELSQSPMLLELMTEVLCREQQHVMEELFQSSFRRIARRGSCVTQVGLLES VYEMFRKDDPRLSFTRQSFVDRSLLTLLWHCSLDALREFFSTIVVDAIDVLKSRFTKLNE STFDTQITKKMGYYKILDVMYSRLPKDDVHAKESKINQVFHGSCITEGNELTKTLIKLCY DAFTENMAGENQLLERRRLYHCAAYNCAISVICCVFNELKFYQGFLFSEKPEKNLLIFEN LIDLKRRYNFPVEVEVPMERKKKYIEIRKEAREAANGDSDGPSYMSSLSYLADSTLSEEM SQFDFSTGVQSYSYSSQDPRPATGRFRRREQRDPTVHDDVLELEMDELNRHECMAPLTAL VKHMHRSLGPPQGEEDSVPRDLPSWMKFLHGKLGNPIVPLNIRLFLAKLVINTEEVFRPY AKHWLSPLLQLAASENNGGEGIHYMVVEIVATILSWTGLATPTGVPKDEVLANRLLNFLM KHVFHPKRAVFRHNLEIIKTLVECWKDCLSIPYRLIFEKFSGKDPNSKDNSVGIQLLGIV MANDLPPYDPQCGIQSSEYFQALVNNMSFVRYKEVYAAAAEVLGLILRYVMERKNILEES LCELVAKQLKQHQNTMEDKFIVCLNKVTKSFPPLADRFMNAVFFLLPKFHGVLKTLCLEV VLCRVEGMTELYFQLKSKDFVQVMRHRDDERQKVCLDIIYKMMPKLKPVELRELLNPVVE FVSHPSTTCREQMYNILMWIHDNYRDPESETDNDSQEIFKLAKDVLIQGLIDENPGLQLI IRNFWSHETRLPSNTLDRLLALNSLYSPKIEVHFLSLATNFLLEMTSMSPDYPNPMFEHP LSECEFQEYTIDSDWRFRSTVLTPMFVETQASQGTLQTRTQEGSLSARWPVAGQIRATQQ QHDFTLTQTADGRSSFDWLTGSSTDPLVDHTSPSSDSLLFAHKRSERLQRAPLKSVGPDF GKKRLGLPGDEVDNKVKGAAGRTDLLRLRRRFMRDQEKLSLMYARKGVAEQKREKEIKSE LKMKQDAQVVLYRSYRHGDLPDIQIKHSSLITPLQAVAQRDPIIAKQLFSSLFSGILKEM DKFKTLSEKNNITQKLLQDFNRFLNTTFSFFPPFVSCIQDISCQHAALLSLDPAAVSAGC LASLQQPVGIRLLEEALLRLLPAELPAKRVRGKARLPPDVLRWVELAKLYRSIGEYDVLR GIFTSEIGTKQITQSALLAEARSDYSEAAKQYDEALNKQDWVDGEPTEAEKDFWELASLD CYNHLAEWKSLEYCSTASIDSENPPDLNKIWSEPFYQETYLPYMIRSKLKLLLQGEADQS LLTFIDKAMHGELQKAILELHYSQELSLLYLLQDDVDRAKYYIQNGIQSFMQNYSSIDVL LHQSRLTKLQSVQALTEIQEFISFISKQGNLSSQVPLKRLLNTWTNRYPDAKMDPMNIWD DIITNRCFFLSKIEEKLTPLPEDNSMNVDQDGDPSDRMEVQEQEEDISSLIRSCKFSMKM KMIDSARKQNNFSLAMKLLKELHKESKTRDDWLVSWVQSYCRLSHCRSRSQGCSEQVLTV LKTVSLLDENNVSSYLSKNILAFRDQNILLGTTYRIIANALSSEPACLAEIEEDKARRIL ELSGSSSEDSEKVIAGLYQRAFQHLSEAVQAAEEEAQPPSWSCGPAAGVIDAYMTLADFC DQQLRKEEENASVIDSAELQAYPALVVEKMLKALKLNSNEARLKFPRLLQIIERYPEETL SLMTKEISSVPCWQFISWISHMVALLDKDQAVAVQHSVEEITDNYPQAIVYPFIISSESY SFKDTSTGHKNKEFVARIKSKLDQGGVIQDFINALDQLSNPELLFKDWSNDVRAELAKTP VNKKNIEKMYERMYAALGDPKAPGLGAFRRKFIQTFGKEFDKHFGKGGSKLLRMKLSDFN DITNMLLLKMNKDSKPPGNLKECSPWMSDFKVEFLRNELEIPGQYDGRGKPLPEYHVRIA GFDERVTVMASLRRPKRIIIRGHDEREHPFLVKGGEDLRQDQRVEQLFQVMNGILAQDSA CSQRALQLRTYSVVPMTSRLGLIEWLENTVTLKDLLLNTMSQEEKAAYLSDPRAPPCEYK DWLTKMSGKHDVGAYMLMYKGANRTETVTSFRKRESKVPADLLKRAFVRMSTSPEAFLAL RSHFASSHALICISHWILGIGDRHLNNFMVAMETGGVIGIDFGHAFGSATQFLPVPELMP FRLTRQFINLMLPMKETGLMYSIMVHALRAF
Target ValidationClick to Find Target Validation Information.    
Inhibitor1-Morpholin-4-yl-benzo[f]chromen-3-one[2]
2- (1H-indol-5-yl)-6-morpholino-4H-pyran-4-one[3]
2- (2-Fluoro-phenyl)-benzo[h]chromen-4-one[2]
2- (2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one[4]
2- (2-aminophenyl)-6-morpholino-4H-pyran-4-one[3]
2- (2-methoxyphenyl)-6-morpholino-4H-pyran-4-one[3]
2- (3-Fluoro-phenyl)-benzo[h]chromen-4-one[2]
2- (3-acetylphenyl)-6-morpholino-4H-pyran-4-one[3]
2- (3-methoxyphenyl)-6-morpholino-4H-pyran-4-one[3]
2- (4-Amino-phenyl)-benzo[h]chromen-4-one[2]
2- (4-chlorophenyl)-6-morpholino-4H-pyran-4-one[3]
2- (4-fluorophenyl)-6-morpholino-4H-pyran-4-one[3]
2- (4-methoxyphenyl)-6-morpholino-4H-pyran-4-one[3]
2- (benzofuran-2-yl)-6-morpholino-4H-pyran-4-one[3]
2- (furan-2-yl)-6-morpholino-4H-pyran-4-one[3]
2- (piperidin-1-yl)-4H-benzo[h]chromen-4-one[5]
2-Morpholin-4-yl-6-phenyl-chromen-4-one[2]
2-Morpholin-4-yl-benzo[h]chromene-4-thione[2]
2-Morpholin-4-yl-pyrido[1,2-a]pyrimidin-4-one[2]
2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one[2]
2-Pyridin-3-yl-benzo[h]chromen-4-one[2]
2-Pyrrolidin-1-yl-benzo[h]chromen-4-one[2]
2-Thiomorpholin-4-yl-pyrido[1,2-a]pyrimidin-4-one[2]
2-[1,4]Oxazepan-4-yl-benzo[h]chromen-4-one[2]
2-biphenyl-4-yl-6-morpholin-4-yl-pyran-4-one[3]
2-dibenzofuran-4-yl-6-morpholin-4-yl-pyran-4-one[3]
2-morpholin-4-yl-6-phenyl-4H-thiopyran-4-one[3]
2-morpholin-4-yl-8-naphthalen-2-ylchromen-4-one[5]
2-morpholin-4-yl-8-phenoxathiin-4-ylchromen-4-one[5]
2-morpholin-4-yl-8-styrylchromen-4-one[5]
2-morpholin-4-yl-8-thiophen-2-ylchromen-4-one[5]
2-morpholin-4-yl-8-thiophen-3-ylchromen-4-one[5]
2-morpholino-4H-benzo[g]chromen-4-one[5]
2-morpholino-6- (naphthalen-1-yl)-4H-chromen-4-one[5]
2-morpholino-6- (naphthalen-1-yl)-4H-pyran-4-one[3]
2-morpholino-6- (naphthalen-2-yl)-4H-pyran-4-one[3]
2-morpholino-6- (quinolin-8-yl)-4H-pyran-4-one[3]
2-morpholino-6- (thianthren-1-yl)-4H-chromen-4-one[5]
2-morpholino-6- (thiophen-2-yl)-4H-pyran-4-one[3]
2-morpholino-6- (thiophen-3-yl)-4H-pyran-4-one[3]
2-morpholino-6-phenyl-4H-pyran-4-one[3]
2-morpholino-6-styryl-4H-pyran-4-one[3]
2-morpholinobenzo[h]quinolin-4 (1H)-one[5]
2-thiomorpholino-4H-benzo[h]chromen-4-one[5]
3- (6-morpholino-4-oxo-4H-pyran-2-yl)benzaldehyde[3]
3- (6-morpholino-4-oxo-4H-pyran-2-yl)benzoic acid[3]
3- (6-morpholino-4-oxo-4H-pyran-2-yl)benzonitrile[3]
3-morpholino-1H-benzo[f]chromen-1-one[3]
4- (6-morpholino-4-oxo-4H-pyran-2-yl)benzonitrile[3]
4-Morpholin-4-yl-benzo[g]chromen-2-one[2]
4-Morpholin-4-yl-benzo[h]chromen-2-one[2]
4-Morpholin-4-yl-chromen-2-one[2]
4-Piperidin-1-yl-chromen-2-one[2]
4-Thiomorpholin-4-yl-benzo[g]chromen-2-one[2]
4-morpholino-6-phenyl-2H-pyran-2-one[3]
6- (2-acetylphenyl)-2-morpholin-4-ylchromen-4-one[5]
6- (3-hydroxyphenyl)-2-morpholino-4H-chromen-4-one[5]
6- (4-chlorophenyl)-2-morpholin-4-ylpyridin-4-ol[3]
6- (4-chlorophenyl)-4-morpholino-2H-pyran-2-one[3]
6- (4-fluorostyryl)-2-morpholino-4H-chromen-4-one[5]
6- (4-hydroxyphenyl)-2-morpholino-4H-chromen-4-one[5]
6- (4-methoxyphenyl)-4-morpholino-2H-pyran-2-one[3]
6-Chloro-4-morpholin-4-yl-chromen-2-one[2]
6-Methoxy-4-morpholin-4-yl-chromen-2-one[2]
6-Methyl-4-morpholin-4-yl-chromen-2-one[2]
6-biphenyl-2-yl-2-morpholin-4-yl-chromen-4-one[5]
6-isopropyl-2-morpholin-4-yl-4H-thiopyran-4-one[3]
6-tert-Butyl-2-morpholin-4-yl-4H-thiopyran-4-one[3]
7-Methoxy-2-morpholin-4-yl-chromen-4-one[2]
7-Methoxy-4-morpholin-4-yl-chromen-2-one[2]
7-benzoyloxy-2- (morpholin-4-yl)-chromen-4-one[5]
7-benzyloxy-2- (morpholin-4-yl)-chromen-4-one[5]
7-ethyloxyethoxy-2-morpholin-4-yl-chromen-4-one[5]
7-hydroxy-2- (morpholin-4-yl)chromen-4-one[5]
7-phenylethoxy-2-morpholin-4-yl-chromen-4-one[5]
7-phenyloxyethoxy-2-morpholin-4-yl-chromen-4-one[5]
7-propoxy-2- (morpholin-4-yl)-chromen-4-one[5]
8- (1H-indol-5-yl)-2-morpholin-4-ylchromen-4-one[5]
8- (2-acetylphenyl)-2-morpholin-4-ylchromen-4-one[5]
8- (3-hydroxyphenyl)-2-morpholin-4-ylchromen-4-one[5]
8- (4-acetylphenyl)-2-morpholin-4-ylchromen-4-one[5]
8- (4-chlorophenyl)-2-morpholin-4-ylchromen-4-one[5]
8- (4-hydroxyphenyl)-2-morpholin-4-ylchromen-4-one[5]
8-Methoxy-2-morpholin-4-yl-chromen-4-one[2]
8-Methoxy-4-morpholin-4-yl-chromen-2-one[2]
8-Methyl-2-morpholin-4-yl-chromen-4-one[2]
8-Methyl-4-morpholin-4-yl-chromen-2-one[2]
8-Phenyl-2-piperidin-1-yl-chromen-4-one[2]
8-Phenyl-2-thiomorpholin-4-yl-chromen-4-one[2]
8-biphenyl-2-yl-2-morpholin-4-ylchromen-4-one[5]
8-dibenzofuran-4-yl-2-morpholin-4-ylchromen-4-one[5]
8-furan-2-yl-2-morpholin-4-ylchromen-4-one[5]
ALPHA-NAPHTHOFLAVONE[2]
KU-55933[3]
LY-292223[4]
LY-293646[5]
LY-294002[5]
NU-7432,   NU-7441[5]
NU7026[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1A novel DNA-dependent protein kinase inhibitor, NU7026, potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia. Blood. 2004 Jun 15;103(12):4659-65. Epub 2004 Mar 9. To Reference
Ref 2J Med Chem. 2005 Jan 27;48(2):569-85.Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. To Reference
Ref 3J Med Chem. 2007 Apr 19;50(8):1958-72. Epub 2007 Mar 20.Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase. To Reference
Ref 4Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7.Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. To Reference
Ref 5J Med Chem. 2005 Dec 1;48(24):7829-46.Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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