General Information of Drug Therapeutic Target (DTT) (ID: TTK3PY9)

DTT Name DNA-dependent protein kinase catalytic (PRKDC)
Synonyms p460; HYRC1; HYRC; DNPK1; DNA-dependent protein kinase catalytic subunit; DNA-PKcs; DNA-PK catalytic subunit
Gene Name PRKDC
DTT Type
Clinical trial target
[1]
BioChemical Class
Kinase
UniProt ID
PRKDC_HUMAN
TTD ID
T81735
EC Number
EC 2.7.11.1
Sequence
MAGSGAGVRCSLLRLQETLSAADRCGAALAGHQLIRGLGQECVLSSSPAVLALQTSLVFS
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
FRLTRQFINLMLPMKETGLMYSIMVHALRAFRSDPGLLTNTMDVFVKEPSFDWKNFEQKM
LKKGGSWIQEINVAEKNWYPRQKICYAKRKLAGANPAVITCDELLLGHEKAPAFRDYVAV
ARGSKDHNIRAQEPESGLSEETQVKCLMDQATDPNILGRTWEGWEPWM
Function
Serine/threonine-protein kinase that acts as a molecular sensor for DNA damage. Involved in DNA non-homologous end joining (NHEJ) required for double-strand break (DSB) repair and V(D)J recombination. Must be bound to DNA to express its catalytic properties. Promotes processing of hairpin DNA structures in V(D)J recombination by activation of the hairpin endonuclease artemis (DCLRE1C). The assembly of the DNA-PK complex at DNA ends is also required for the NHEJ ligation step. Required to protect and align broken ends of DNA. May also act as a scaffold protein to aid the localization of DNA repair proteins to the site of damage. Found at the ends of chromosomes, suggesting a further role in the maintenance of telomeric stability and the prevention of chromosomal end fusion. Also involved in modulation of transcription. Recognizes the substrate consensus sequence [ST]-Q. Phosphorylates 'Ser-139' of histone variant H2AX/H2AFX, thereby regulating DNA damage response mechanism. Phosphorylates DCLRE1C, c-Abl/ABL1, histone H1, HSPCA, c-jun/JUN, p53/TP53, PARP1, POU2F1, DHX9, FH, SRF, XRCC1, XRCC1, XRCC4, XRCC5, XRCC6, WRN, MYC and RFA2. Can phosphorylate C1D not only in the presence of linear DNA but also in the presence of supercoiled DNA. Ability to phosphorylate p53/TP53 in the presence of supercoiled DNA is dependent on C1D. Contributes to the determination of the circadian period length by antagonizing phosphorylation of CRY1 'Ser-588' and increasing CRY1 protein stability, most likely through an indirect mechanism (By similarity). Plays a role in the regulation of DNA virus-mediated innate immune response by assembling into the HDP-RNP complex, a complex that serves as a platform for IRF3 phosphorylation and subsequent innate immune response activation through the cGAS-STING pathway.
KEGG Pathway
Non-homologous end-joining (hsa03450 )
Cell cycle (hsa04110 )
Reactome Pathway
Nonhomologous End-Joining (NHEJ) (R-HSA-5693571 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
3 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AZD7648 DMD9Y5T Solid tumour/cancer 2A00-2F9Z Phase 1/2 [2]
M3814 DMK2L38 Locally advanced rectal cancer 2B92 Phase 1/2 [1]
M9831 DM59TI2 Solid tumour/cancer 2A00-2F9Z Phase 1 [1]
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103 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
1-Morpholin-4-yl-benzo[f]chromen-3-one DMYOJ01 Discovery agent N.A. Investigative [3]
2-(1H-indol-5-yl)-6-morpholino-4H-pyran-4-one DMZNML4 Discovery agent N.A. Investigative [4]
2-(2-aminophenyl)-6-morpholino-4H-pyran-4-one DMCLSJZ Discovery agent N.A. Investigative [4]
2-(2-Fluoro-phenyl)-benzo[h]chromen-4-one DMDUG9M Discovery agent N.A. Investigative [3]
2-(2-methoxyphenyl)-6-morpholino-4H-pyran-4-one DMXVCL0 Discovery agent N.A. Investigative [4]
2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one DMAHZR9 Discovery agent N.A. Investigative [5]
2-(3-acetylphenyl)-6-morpholino-4H-pyran-4-one DMJ2NPY Discovery agent N.A. Investigative [4]
2-(3-Fluoro-phenyl)-benzo[h]chromen-4-one DMNYWAT Discovery agent N.A. Investigative [3]
2-(3-methoxyphenyl)-6-morpholino-4H-pyran-4-one DMASH36 Discovery agent N.A. Investigative [4]
2-(4-Amino-phenyl)-benzo[h]chromen-4-one DM2P9L5 Discovery agent N.A. Investigative [3]
2-(4-chlorophenyl)-6-morpholino-4H-pyran-4-one DM7EUOX Discovery agent N.A. Investigative [4]
2-(4-fluorophenyl)-6-morpholino-4H-pyran-4-one DMECX8S Discovery agent N.A. Investigative [4]
2-(4-methoxyphenyl)-6-morpholino-4H-pyran-4-one DMVQU1M Discovery agent N.A. Investigative [4]
2-(benzofuran-2-yl)-6-morpholino-4H-pyran-4-one DMO3G6Q Discovery agent N.A. Investigative [4]
2-(furan-2-yl)-6-morpholino-4H-pyran-4-one DM6BHUF Discovery agent N.A. Investigative [4]
2-(piperidin-1-yl)-4H-benzo[h]chromen-4-one DMGQX1I Discovery agent N.A. Investigative [6]
2-biphenyl-4-yl-6-morpholin-4-yl-pyran-4-one DML1W5Z Discovery agent N.A. Investigative [4]
2-dibenzofuran-4-yl-6-morpholin-4-yl-pyran-4-one DM4A527 Discovery agent N.A. Investigative [4]
2-morpholin-4-yl-6-phenyl-4H-thiopyran-4-one DMCVF7R Discovery agent N.A. Investigative [4]
2-Morpholin-4-yl-6-phenyl-chromen-4-one DMTB1KV Discovery agent N.A. Investigative [3]
2-morpholin-4-yl-8-naphthalen-2-ylchromen-4-one DMC1TWI Discovery agent N.A. Investigative [6]
2-morpholin-4-yl-8-phenoxathiin-4-ylchromen-4-one DMVN38H Discovery agent N.A. Investigative [6]
2-morpholin-4-yl-8-styrylchromen-4-one DMNHYQ0 Discovery agent N.A. Investigative [6]
2-morpholin-4-yl-8-thiophen-2-ylchromen-4-one DM5JHT6 Discovery agent N.A. Investigative [6]
2-morpholin-4-yl-8-thiophen-3-ylchromen-4-one DMCY4EP Discovery agent N.A. Investigative [6]
2-Morpholin-4-yl-benzo[h]chromene-4-thione DM3ZWNI Discovery agent N.A. Investigative [3]
2-Morpholin-4-yl-pyrido[1,2-a]pyrimidin-4-one DMCKSX7 Discovery agent N.A. Investigative [3]
2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one DM79ZOV Discovery agent N.A. Investigative [3]
2-morpholino-4H-benzo[g]chromen-4-one DM5J6IT Discovery agent N.A. Investigative [6]
2-morpholino-6-(naphthalen-1-yl)-4H-chromen-4-one DMZL6Q1 Discovery agent N.A. Investigative [6]
2-morpholino-6-(naphthalen-1-yl)-4H-pyran-4-one DMEOI0V Discovery agent N.A. Investigative [4]
2-morpholino-6-(naphthalen-2-yl)-4H-pyran-4-one DMO7QCN Discovery agent N.A. Investigative [4]
2-morpholino-6-(quinolin-8-yl)-4H-pyran-4-one DMTBRLK Discovery agent N.A. Investigative [4]
2-morpholino-6-(thianthren-1-yl)-4H-chromen-4-one DMATVZB Discovery agent N.A. Investigative [6]
2-morpholino-6-(thiophen-2-yl)-4H-pyran-4-one DMTWJMN Discovery agent N.A. Investigative [4]
2-morpholino-6-(thiophen-3-yl)-4H-pyran-4-one DMF3NPW Discovery agent N.A. Investigative [4]
2-morpholino-6-phenyl-4H-pyran-4-one DMMC0ZP Discovery agent N.A. Investigative [4]
2-morpholino-6-styryl-4H-pyran-4-one DM8ZPJI Discovery agent N.A. Investigative [4]
2-morpholinobenzo[h]quinolin-4(1H)-one DMYP0UI Discovery agent N.A. Investigative [6]
2-Pyridin-3-yl-benzo[h]chromen-4-one DMT21UX Discovery agent N.A. Investigative [3]
2-Pyrrolidin-1-yl-benzo[h]chromen-4-one DMGPI0C Discovery agent N.A. Investigative [3]
2-Thiomorpholin-4-yl-pyrido[1,2-a]pyrimidin-4-one DMSKNBA Discovery agent N.A. Investigative [3]
2-thiomorpholino-4H-benzo[h]chromen-4-one DMFXG2E Discovery agent N.A. Investigative [6]
2-[1,4]Oxazepan-4-yl-benzo[h]chromen-4-one DMC8IEM Discovery agent N.A. Investigative [3]
3-(6-morpholino-4-oxo-4H-pyran-2-yl)benzaldehyde DMS9DPO Discovery agent N.A. Investigative [4]
3-(6-morpholino-4-oxo-4H-pyran-2-yl)benzoic acid DM2VNLK Discovery agent N.A. Investigative [4]
3-(6-morpholino-4-oxo-4H-pyran-2-yl)benzonitrile DM2J63V Discovery agent N.A. Investigative [4]
3-morpholino-1H-benzo[f]chromen-1-one DMGWH0E Discovery agent N.A. Investigative [4]
4-(6-morpholino-4-oxo-4H-pyran-2-yl)benzonitrile DM9O8VY Discovery agent N.A. Investigative [4]
4-Morpholin-4-yl-benzo[g]chromen-2-one DMEJ6G9 Discovery agent N.A. Investigative [3]
4-Morpholin-4-yl-benzo[h]chromen-2-one DMW2MRP Discovery agent N.A. Investigative [3]
4-Morpholin-4-yl-chromen-2-one DM7T3CU Discovery agent N.A. Investigative [3]
4-morpholino-6-phenyl-2H-pyran-2-one DM8QPTJ Discovery agent N.A. Investigative [4]
4-Piperidin-1-yl-chromen-2-one DMOHDRS Discovery agent N.A. Investigative [3]
4-Thiomorpholin-4-yl-benzo[g]chromen-2-one DMA8SHN Discovery agent N.A. Investigative [3]
6-(2-acetylphenyl)-2-morpholin-4-ylchromen-4-one DMA9LFR Discovery agent N.A. Investigative [6]
6-(3-hydroxyphenyl)-2-morpholino-4H-chromen-4-one DM28DPY Discovery agent N.A. Investigative [6]
6-(4-chlorophenyl)-2-morpholin-4-ylpyridin-4-ol DMSO2JW Discovery agent N.A. Investigative [4]
6-(4-chlorophenyl)-4-morpholino-2H-pyran-2-one DMMTG7L Discovery agent N.A. Investigative [4]
6-(4-fluorostyryl)-2-morpholino-4H-chromen-4-one DMKGTRF Discovery agent N.A. Investigative [6]
6-(4-hydroxyphenyl)-2-morpholino-4H-chromen-4-one DMTYWCS Discovery agent N.A. Investigative [6]
6-(4-methoxyphenyl)-4-morpholino-2H-pyran-2-one DMUHCO8 Discovery agent N.A. Investigative [4]
6-biphenyl-2-yl-2-morpholin-4-yl-chromen-4-one DMZPY69 Discovery agent N.A. Investigative [6]
6-Chloro-4-morpholin-4-yl-chromen-2-one DMHJIN0 Discovery agent N.A. Investigative [3]
6-isopropyl-2-morpholin-4-yl-4H-thiopyran-4-one DMGXMZL Discovery agent N.A. Investigative [4]
6-Methoxy-4-morpholin-4-yl-chromen-2-one DMPB9MY Discovery agent N.A. Investigative [3]
6-Methyl-4-morpholin-4-yl-chromen-2-one DMO7RPW Discovery agent N.A. Investigative [3]
6-tert-Butyl-2-morpholin-4-yl-4H-thiopyran-4-one DMQAG1B Discovery agent N.A. Investigative [4]
7-benzoyloxy-2-(morpholin-4-yl)-chromen-4-one DMZDP5S Discovery agent N.A. Investigative [6]
7-benzyloxy-2-(morpholin-4-yl)-chromen-4-one DMMXAEN Discovery agent N.A. Investigative [6]
7-ethyloxyethoxy-2-morpholin-4-yl-chromen-4-one DMXM2G7 Discovery agent N.A. Investigative [6]
7-hydroxy-2-(morpholin-4-yl)chromen-4-one DMIKSTL Discovery agent N.A. Investigative [6]
7-Methoxy-2-morpholin-4-yl-chromen-4-one DMR713M Discovery agent N.A. Investigative [3]
7-Methoxy-4-morpholin-4-yl-chromen-2-one DMNFIZD Discovery agent N.A. Investigative [3]
7-phenylethoxy-2-morpholin-4-yl-chromen-4-one DMEDOFB Discovery agent N.A. Investigative [6]
7-phenyloxyethoxy-2-morpholin-4-yl-chromen-4-one DMSBJ4M Discovery agent N.A. Investigative [6]
7-propoxy-2-(morpholin-4-yl)-chromen-4-one DMO8WB2 Discovery agent N.A. Investigative [6]
8-(1H-indol-5-yl)-2-morpholin-4-ylchromen-4-one DMMBH9N Discovery agent N.A. Investigative [6]
8-(2-acetylphenyl)-2-morpholin-4-ylchromen-4-one DM8SRM0 Discovery agent N.A. Investigative [6]
8-(3-hydroxyphenyl)-2-morpholin-4-ylchromen-4-one DM15LVG Discovery agent N.A. Investigative [6]
8-(4-acetylphenyl)-2-morpholin-4-ylchromen-4-one DMAK0P3 Discovery agent N.A. Investigative [6]
8-(4-chlorophenyl)-2-morpholin-4-ylchromen-4-one DM4186A Discovery agent N.A. Investigative [6]
8-(4-hydroxyphenyl)-2-morpholin-4-ylchromen-4-one DMLANGY Discovery agent N.A. Investigative [6]
8-biphenyl-2-yl-2-morpholin-4-ylchromen-4-one DMMCAZG Discovery agent N.A. Investigative [6]
8-dibenzofuran-4-yl-2-morpholin-4-ylchromen-4-one DMUR97N Discovery agent N.A. Investigative [6]
8-furan-2-yl-2-morpholin-4-ylchromen-4-one DMPY9OI Discovery agent N.A. Investigative [6]
8-Methoxy-2-morpholin-4-yl-chromen-4-one DMYE1X2 Discovery agent N.A. Investigative [3]
8-Methoxy-4-morpholin-4-yl-chromen-2-one DMHLKAE Discovery agent N.A. Investigative [3]
8-Methyl-2-morpholin-4-yl-chromen-4-one DMLQ90D Discovery agent N.A. Investigative [3]
8-Methyl-4-morpholin-4-yl-chromen-2-one DMVAOIG Discovery agent N.A. Investigative [3]
8-Phenyl-2-piperidin-1-yl-chromen-4-one DM29L4D Discovery agent N.A. Investigative [3]
8-Phenyl-2-thiomorpholin-4-yl-chromen-4-one DMJMWOE Discovery agent N.A. Investigative [3]
ALPHA-NAPHTHOFLAVONE DMELOIQ Discovery agent N.A. Investigative [3]
AMA37 DMIZQOG Discovery agent N.A. Investigative [7]
Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate DM3FH02 Discovery agent N.A. Investigative [6]
IC86621 DMWRVGE Discovery agent N.A. Investigative [8]
KU-0060648 DMQWS6U Discovery agent N.A. Investigative [9]
KU-55933 DMDT42X Solid tumour/cancer 2A00-2F9Z Investigative [4]
LY-292223 DML36ZE Discovery agent N.A. Investigative [5]
NU-7432 DMDNUM5 Discovery agent N.A. Investigative [6]
PIK-75 DM9BQTX Discovery agent N.A. Investigative [10]
PP121 DMU8KTO Discovery agent N.A. Investigative [11]
ShRNA molecule silencing DNAPK radiosensitizer DMTKHR3 Prostate cancer 2C82.0 Investigative [12]
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⏷ Show the Full List of 103 Investigative Drug(s)

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity. Nat Commun. 2019 Nov 7;10(1):5065.
3 Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and... J Med Chem. 2005 Jan 27;48(2):569-85.
4 Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependen... J Med Chem. 2007 Apr 19;50(8):1958-72.
5 Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7.
6 Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. J Med Chem. 2005 Dec 1;48(24):7829-46.
7 Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one. J Biol Chem. 2007 Aug 17;282(33):24463-70.
8 Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5352-9.
9 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401.
10 A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.
11 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
12 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2800).