Target Validation Information
TTD ID T81735
Target Name DNA-dependent protein kinase catalytic (PRKDC)
Type of Target
Clinical trial
Drug Potency against Target 1-Morpholin-4-yl-benzo[f]chromen-3-one Drug Info IC50 = 1900 nM [2]
2-(1H-indol-5-yl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 400 nM [4]
2-(2-aminophenyl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 7800 nM [4]
2-(2-Fluoro-phenyl)-benzo[h]chromen-4-one Drug Info IC50 = 8590 nM [2]
2-(2-methoxyphenyl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 310 nM [4]
2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one Drug Info IC50 = 190 nM [1]
2-(3-acetylphenyl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 4700 nM [4]
2-(3-Fluoro-phenyl)-benzo[h]chromen-4-one Drug Info IC50 = 5710 nM [2]
2-(3-methoxyphenyl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 540 nM [4]
2-(4-Amino-phenyl)-benzo[h]chromen-4-one Drug Info IC50 = 7700 nM [2]
2-(4-chlorophenyl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 180 nM [4]
2-(4-fluorophenyl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 350 nM [4]
2-(4-methoxyphenyl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 220 nM [4]
2-(benzofuran-2-yl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 800 nM [4]
2-(furan-2-yl)-6-morpholino-4H-pyran-4-one Drug Info IC50 = 1000 nM [4]
2-(piperidin-1-yl)-4H-benzo[h]chromen-4-one Drug Info IC50 = 3810 nM [3]
2-biphenyl-4-yl-6-morpholin-4-yl-pyran-4-one Drug Info IC50 = 800 nM [4]
2-dibenzofuran-4-yl-6-morpholin-4-yl-pyran-4-one Drug Info IC50 = 1200 nM [4]
2-morpholin-4-yl-6-phenyl-4H-thiopyran-4-one Drug Info IC50 = 650 nM [4]
2-Morpholin-4-yl-6-phenyl-chromen-4-one Drug Info IC50 = 2240 nM [2]
2-morpholin-4-yl-8-naphthalen-2-ylchromen-4-one Drug Info IC50 = 3000 nM [3]
2-morpholin-4-yl-8-phenoxathiin-4-ylchromen-4-one Drug Info IC50 = 5800 nM [3]
2-morpholin-4-yl-8-styrylchromen-4-one Drug Info IC50 = 1500 nM [3]
2-morpholin-4-yl-8-thiophen-2-ylchromen-4-one Drug Info IC50 = 700 nM [3]
2-morpholin-4-yl-8-thiophen-3-ylchromen-4-one Drug Info IC50 = 300 nM [3]
2-Morpholin-4-yl-benzo[h]chromene-4-thione Drug Info IC50 = 260 nM [2]
2-Morpholin-4-yl-pyrido[1,2-a]pyrimidin-4-one Drug Info IC50 = 2000 nM [2]
2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one Drug Info IC50 = 280 nM [2]
2-morpholino-4H-benzo[g]chromen-4-one Drug Info IC50 = 400 nM [3]
2-morpholino-6-(naphthalen-1-yl)-4H-pyran-4-one Drug Info IC50 = 2300 nM [4]
2-morpholino-6-(naphthalen-2-yl)-4H-pyran-4-one Drug Info IC50 = 1300 nM [4]
2-morpholino-6-(quinolin-8-yl)-4H-pyran-4-one Drug Info IC50 = 900 nM [4]
2-morpholino-6-(thiophen-2-yl)-4H-pyran-4-one Drug Info IC50 = 1100 nM [4]
2-morpholino-6-(thiophen-3-yl)-4H-pyran-4-one Drug Info IC50 = 1600 nM [4]
2-morpholino-6-phenyl-4H-pyran-4-one Drug Info IC50 = 1300 nM [4]
2-morpholino-6-styryl-4H-pyran-4-one Drug Info IC50 = 4200 nM [4]
2-morpholinobenzo[h]quinolin-4(1H)-one Drug Info IC50 = 250 nM [3]
2-Pyridin-3-yl-benzo[h]chromen-4-one Drug Info IC50 = 1920 nM [2]
2-Pyrrolidin-1-yl-benzo[h]chromen-4-one Drug Info IC50 = 6170 nM [2]
2-Thiomorpholin-4-yl-pyrido[1,2-a]pyrimidin-4-one Drug Info IC50 = 1690 nM [2]
2-thiomorpholino-4H-benzo[h]chromen-4-one Drug Info IC50 = 1380 nM [3]
2-[1,4]Oxazepan-4-yl-benzo[h]chromen-4-one Drug Info IC50 = 2010 nM [2]
3-(6-morpholino-4-oxo-4H-pyran-2-yl)benzaldehyde Drug Info IC50 = 2500 nM [4]
3-(6-morpholino-4-oxo-4H-pyran-2-yl)benzoic acid Drug Info IC50 = 7200 nM [4]
3-(6-morpholino-4-oxo-4H-pyran-2-yl)benzonitrile Drug Info IC50 = 3100 nM [4]
3-morpholino-1H-benzo[f]chromen-1-one Drug Info IC50 = 1250 nM [4]
4-(6-morpholino-4-oxo-4H-pyran-2-yl)benzonitrile Drug Info IC50 = 2500 nM [4]
4-Morpholin-4-yl-benzo[g]chromen-2-one Drug Info IC50 = 3240 nM [2]
4-Morpholin-4-yl-benzo[h]chromen-2-one Drug Info IC50 = 6660 nM [2]
4-Morpholin-4-yl-chromen-2-one Drug Info IC50 = 4820 nM [2]
4-morpholino-6-phenyl-2H-pyran-2-one Drug Info IC50 = 1800 nM [4]
4-Piperidin-1-yl-chromen-2-one Drug Info IC50 = 8810 nM [2]
4-Thiomorpholin-4-yl-benzo[g]chromen-2-one Drug Info IC50 = 5150 nM [2]
6-(4-chlorophenyl)-2-morpholin-4-ylpyridin-4-ol Drug Info IC50 = 8100 nM [4]
6-(4-chlorophenyl)-4-morpholino-2H-pyran-2-one Drug Info IC50 = 470 nM [4]
6-(4-methoxyphenyl)-4-morpholino-2H-pyran-2-one Drug Info IC50 = 530 nM [4]
6-Chloro-4-morpholin-4-yl-chromen-2-one Drug Info IC50 = 3270 nM [2]
6-isopropyl-2-morpholin-4-yl-4H-thiopyran-4-one Drug Info IC50 = 5900 nM [4]
6-Methoxy-4-morpholin-4-yl-chromen-2-one Drug Info IC50 = 1750 nM [2]
6-Methyl-4-morpholin-4-yl-chromen-2-one Drug Info IC50 = 5350 nM [2]
6-tert-Butyl-2-morpholin-4-yl-4H-thiopyran-4-one Drug Info IC50 = 1060 nM [4]
7-benzoyloxy-2-(morpholin-4-yl)-chromen-4-one Drug Info IC50 = 1680 nM [3]
7-benzyloxy-2-(morpholin-4-yl)-chromen-4-one Drug Info IC50 = 380 nM [3]
7-ethyloxyethoxy-2-morpholin-4-yl-chromen-4-one Drug Info IC50 = 8400 nM [3]
7-hydroxy-2-(morpholin-4-yl)chromen-4-one Drug Info IC50 = 450 nM [3]
7-Methoxy-2-morpholin-4-yl-chromen-4-one Drug Info IC50 = 950 nM [2]
7-Methoxy-4-morpholin-4-yl-chromen-2-one Drug Info IC50 = 11310 nM [2]
7-phenylethoxy-2-morpholin-4-yl-chromen-4-one Drug Info IC50 = 2990 nM [3]
7-phenyloxyethoxy-2-morpholin-4-yl-chromen-4-one Drug Info IC50 = 4590 nM [3]
7-propoxy-2-(morpholin-4-yl)-chromen-4-one Drug Info IC50 = 1320 nM [3]
8-(1H-indol-5-yl)-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 2600 nM [3]
8-(2-acetylphenyl)-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 14900 nM [3]
8-(3-hydroxyphenyl)-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 1200 nM [3]
8-(4-acetylphenyl)-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 1000 nM [3]
8-(4-chlorophenyl)-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 2400 nM [3]
8-(4-hydroxyphenyl)-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 2600 nM [3]
8-biphenyl-2-yl-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 10600 nM [3]
8-dibenzofuran-4-yl-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 40 nM [3]
8-furan-2-yl-2-morpholin-4-ylchromen-4-one Drug Info IC50 = 2800 nM [3]
8-Methoxy-2-morpholin-4-yl-chromen-4-one Drug Info IC50 = 1200 nM [2]
8-Methoxy-4-morpholin-4-yl-chromen-2-one Drug Info IC50 = 10940 nM [2]
8-Methyl-2-morpholin-4-yl-chromen-4-one Drug Info IC50 = 1650 nM [2]
8-Methyl-4-morpholin-4-yl-chromen-2-one Drug Info IC50 = 8050 nM [2]
8-Phenyl-2-piperidin-1-yl-chromen-4-one Drug Info IC50 = 4670 nM [2]
8-Phenyl-2-thiomorpholin-4-yl-chromen-4-one Drug Info IC50 = 1610 nM [2]
ALPHA-NAPHTHOFLAVONE Drug Info IC50 = 4980 nM [2]
Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate Drug Info IC50 = 230 nM [3]
KU-55933 Drug Info IC50 = 1800 nM [4]
LY-292223 Drug Info IC50 = 1300 nM [1]
NU-7432 Drug Info Ki = 0.65 nM [3]
References
REF 1 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.
REF 2 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.
REF 3 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.
REF 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.

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