Details of the Drug Therapeutic Target (DTT)

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]
• Related Disease:
  Rectum cancer [ICD-11: 2B92]
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• 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.
• Reactome Pathway: Nonhomologous End-Joining (NHEJ) (R-HSA-5693571)

Molecular Interaction Atlas (MIA) 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]

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]

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).