Target Validation Information
Target ID T06273
Target Name Poly [ADP-ribose] polymerase-1
Target Type
Successful
Drug Potency against Target 3-aminobenzo[c][1,5]naphthyridin-6(5H)-one Drug Info IC50 = 180 nM [529901]
(E)-N-(4-Phenylthiazol-2-yl) cinnamamide Drug Info IC50 = 224 nM [529901]
AG-014376 Drug Info Ki = 6.4 nM [527248]
2-Methylquinoline-8-carboxamide Drug Info IC50 = 500 nM [529894]
8-Nitro-6H,11H-indeno[1,2-c]isoquinolin-5-one Drug Info IC50 = 500 nM [527674]
CEP-6800 Drug Info IC50 = 18 nM [528503]
ABT-888 Drug Info Ki = 5 nM [529921]
BSI-201 Drug Info EC50 = 1.4 nM [552548]
3-Morpholin-4-ylmethyl-5H-phenanthridin-6-one Drug Info IC50 = 23 nM [527682]
4-(5-Morpholin-4-yl-pentyl)-2H-phthalazin-1-one Drug Info IC50 = 119 nM [527682]
4-(4-Morpholin-4-yl-butyl)-2H-phthalazin-1-one Drug Info IC50 = 950 nM [527682]
3-Ethenylquinoline-8-carboxamide Drug Info IC50 = 5800 nM [529894]
9-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one Drug Info IC50 = 650 nM [527674]
5-amino-3,4-dihydroisoquinolin-1(2H)-one Drug Info IC50 = 410 nM [530584]
Pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Drug Info IC50 = 10000 nM [527871]
8-Methoxy-2-methyl-3H-quinazolin-4-one Drug Info IC50 = 780 nM [534774]
KU-0058948 Drug Info IC50 = 3.4 nM [530062]
2-ethylquinoline-8-carboxamide Drug Info IC50 = 800 nM [529894]
3-Hydroxy-benzamide Drug Info IC50 = 8000 nM [534774]
2,3-dihydro-1H-benzo[de]isoquinolin-1-one Drug Info IC50 = 540 nM [530584]
5-Chloro-2-methyl-3H-quinazolin-4-one Drug Info IC50 = 1200 nM [527159]
2-(3-Piperidin-1-yl-propyl)-3H-quinazolin-4-one Drug Info IC50 = 1100 nM [527159]
1,7,8,9-tetrahydro-1,5-diaza-trindene-4,6-dione Drug Info IC50 = 40 nM [527871]
5-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Drug Info IC50 = 5000 nM [527871]
2-(4-Chlorophenyl)-2H-indazole-7-carboxamide Drug Info IC50 = 24 nM [530485]
2-Benzyl-2H-indazole-7-carboxamide Drug Info IC50 = 130 nM [530485]
9-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one Drug Info IC50 = 98 nM [527674]
2-(3-Chlorophenyl)-2H-indazole-7-carboxamide Drug Info IC50 = 14 nM [530485]
Nicotinamide Drug Info IC50 = 7800000 nM [553187]
2-(4-Amino-phenyl)-8-hydroxy-3H-quinazolin-4-one Drug Info IC50 = 520 nM [534774]
Olaparib Drug Info IC50 = 6 nM [536853]
Rucaparib Drug Info Ki < 5 nM
8-Methyl-2-(4-nitro-phenyl)-3H-quinazolin-4-one Drug Info IC50 = 130 nM [534774]
8-Methoxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one Drug Info IC50 = 850 nM [534774]
3-Ethynylquinoline-8-carboxamide Drug Info IC50 = 2300 nM [529894]
2-phenylquinoline-8-carboxamide Drug Info IC50 = 900 nM [529894]
Quinoline-8-carboxamide Drug Info IC50 = 1900 nM [529894]
3-Ethylquinoline-8-carboxamide Drug Info IC50 = 3700 nM [529894]
3-Methylquinoline-8-carboxamide Drug Info IC50 = 3400 nM [529894]
3-Prop-1-ynylquinoline-8-carboxamide Drug Info IC50 = 2200 nM [529894]
2-(4-methoxyphenyl)quinoline-8-carboxamide Drug Info IC50 = 1100 nM [529894]
8-Methoxy-2-phenyl-3H-quinazolin-4-one Drug Info IC50 = 4200 nM [534774]
2-phenylpyrazolo-[1,5-a]pyridine-7-carboxamide Drug Info IC50 = 55 nM [530485]
2-(2-Chlorophenyl)-2H-indazole-7-carboxamide Drug Info IC50 = 100 nM [530485]
KU-58684 Drug Info IC50 = 5 nM [529901]
3-Phenylquinoline-8-carboxamide Drug Info IC50 = 15000 nM [529894]
8-Hydroxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one Drug Info IC50 = 230 nM [534774]
2-(4-Methoxy-phenyl)-8-methyl-3H-quinazolin-4-one Drug Info IC50 = 190 nM [534774]
2-(4-Amino-phenyl)-8-methyl-3H-quinazolin-4-one Drug Info IC50 = 440 nM [534774]
1,2,3,4,4a,5-hexahydrophenanthridin-6(10bH)-one Drug Info IC50 = 7500 nM [529901]
4-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Drug Info IC50 = 2000 nM [527871]
3-(4-methoxyphenyl)quinoxaline-5-carboxamide Drug Info IC50 = 71 nM [529901]
4-benzylphthalazin-1(2H)-one Drug Info IC50 = 770 nM [529901]
5-aminoisoquinolin-1(2H)-one Drug Info IC50 = 1800 nM [529894]
Benzo[c][1,5]naphthyridin-6(5H)-one Drug Info IC50 = 116 nM [529901]
2-phenyl-2H-indazole-7-carboxamide Drug Info IC50 = 24 nM [530485]
3-(4-aminophenyl)quinoxaline-5-carboxamide Drug Info IC50 = 87 nM [529901]
2-phenyl-2H-benzo[d][1,2,3]triazole-4-carboxamide Drug Info IC50 = 71 nM [530485]
8-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one Drug Info IC50 = 300 nM [527674]
8-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one Drug Info IC50 = 500 nM [527674]
3-Amino-benzamide Drug Info IC50 = 19100 nM [534774]
PD-128763 Drug Info IC50 = 440 nM [534774]
3-(4-cyanophenyl)quinoxaline-5-carboxamide Drug Info IC50 = 101 nM [529901]
Pyrrolo[3,4-e]indole-1,3(2H,6H)-dione Drug Info IC50 = 750 nM [527871]
2-(4-Azido-phenyl)-8-methoxy-3H-quinazolin-4-one Drug Info IC50 = 1930 nM [534774]
2,8-Dimethyl-3H-quinazolin-4-one Drug Info IC50 = 390 nM [534774]
4-amino-1,8-naphthalimide Drug Info IC50 = 26 nM [527871]
2H-Isoquinolin-1-one Drug Info IC50 = 15800 nM [534774]
8-Methyl-2-phenyl-3H-quinazolin-4-one Drug Info IC50 = 870 nM [534774]
8-Hydroxy-2-phenyl-3H-quinazolin-4-one Drug Info IC50 = 1060 nM [534774]
N-(4-Phenylthiazol-2-yl)isonicotinamide Drug Info IC50 = 753 nM [529901]
2-(4-Hydroxy-phenyl)-8-methyl-3H-quinazolin-4-one Drug Info IC50 = 220 nM [534774]
References
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 527248J Med Chem. 2004 Oct 21;47(22):5467-81.Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 527674J Med Chem. 2005 Aug 11;48(16):5100-3.Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
Ref 528503Bioorg Med Chem Lett. 2007 Jan 15;17(2):542-5. Epub 2006 Oct 10.Novel poly(ADP-ribose) polymerase-1 inhibitors.
Ref 529921J Med Chem. 2009 Jan 22;52(2):514-23.Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.
Ref 552548Positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (mGluR2). Curr Top Med Chem. 2005;5(9):869-84.
Ref 527682Bioorg Med Chem Lett. 2005 Oct 1;15(19):4221-5.4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.
Ref 527682Bioorg Med Chem Lett. 2005 Oct 1;15(19):4221-5.4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.
Ref 527682Bioorg Med Chem Lett. 2005 Oct 1;15(19):4221-5.4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 527674J Med Chem. 2005 Aug 11;48(16):5100-3.Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
Ref 530584Bioorg Med Chem Lett. 2010 Jan 15;20(2):448-52. Epub 2009 Dec 4.Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Ref 527871Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. Epub 2005 Nov 15.Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 530062J Med Chem. 2009 May 14;52(9):3108-11.Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 530584Bioorg Med Chem Lett. 2010 Jan 15;20(2):448-52. Epub 2009 Dec 4.Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Ref 527159J Med Chem. 2004 Aug 12;47(17):4151-4.Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.
Ref 527159J Med Chem. 2004 Aug 12;47(17):4151-4.Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.
Ref 527871Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. Epub 2005 Nov 15.Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Ref 527871Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. Epub 2005 Nov 15.Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Ref 530485J Med Chem. 2009 Nov 26;52(22):7170-85.Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Ref 530485J Med Chem. 2009 Nov 26;52(22):7170-85.Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Ref 527674J Med Chem. 2005 Aug 11;48(16):5100-3.Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
Ref 530485J Med Chem. 2009 Nov 26;52(22):7170-85.Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Ref 553187Modulation of inflammatory arthritis by inhibition of poly(ADP ribose) polymerase. Inflammation. 1995 Jun;19(3):379-87.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 5368534-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91. Epub 2008 Sep 19.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 530485J Med Chem. 2009 Nov 26;52(22):7170-85.Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Ref 530485J Med Chem. 2009 Nov 26;52(22):7170-85.Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 527871Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. Epub 2005 Nov 15.Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 529894J Med Chem. 2009 Feb 12;52(3):868-77.Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 530485J Med Chem. 2009 Nov 26;52(22):7170-85.Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 530485J Med Chem. 2009 Nov 26;52(22):7170-85.Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Ref 527674J Med Chem. 2005 Aug 11;48(16):5100-3.Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
Ref 527674J Med Chem. 2005 Aug 11;48(16):5100-3.Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 527871Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. Epub 2005 Nov 15.Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 527871Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. Epub 2005 Nov 15.Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Ref 529901J Med Chem. 2009 Feb 12;52(3):718-25.Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Ref 534774J Med Chem. 1998 Dec 17;41(26):5247-56.Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).

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