Therapeutic Targets Database
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Target Validation Information
TTD IDTTDS00191
Target NamePoly [ADP-ribose] polymerase-1    
Type of TargetSuccessful target    
Drug Potency against TargetNicotinamideIC50 = 7800000 nM[1]
BSI-201EC50 = 1.4 nM[2]
AG-14699Ki < 5 nM[3]
2-(2-Chlorophenyl)-2H-indazole-7-carboxamideIC50 = 100 nM[4]
pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dioneIC50 = 10000 nM[5]
3-(4-cyanophenyl)quinoxaline-5-carboxamideIC50 = 101 nM[6]
8-Hydroxy-2-phenyl-3H-quinazolin-4-oneIC50 = 1060 nM[7]
2-(3-Piperidin-1-yl-propyl)-3H-quinazolin-4-oneIC50 = 1100 nM[8]
2-(4-methoxyphenyl)quinoline-8-carboxamideIC50 = 1100 nM[9]
benzo[c][1,5]naphthyridin-6(5H)-oneIC50 = 116 nM[6]
4-(5-Morpholin-4-yl-pentyl)-2H-phthalazin-1-oneIC50 = 119 nM[10]
5-Chloro-2-methyl-3H-quinazolin-4-oneIC50 = 1200 nM[8]
2-Benzyl-2H-indazole-7-carboxamideIC50 = 130 nM[4]
8-Methyl-2-(4-nitro-phenyl)-3H-quinazolin-4-oneIC50 = 130 nM[7]
2-(3-Chlorophenyl)-2H-indazole-7-carboxamideIC50 = 14 nM[4]
3-Phenylquinoline-8-carboxamideIC50 = 15000 nM[9]
2H-Isoquinolin-1-oneIC50 = 15800 nM[7]
CEP-6800IC50 = 18 nM[11]
3-aminobenzo[c][1,5]naphthyridin-6(5H)-oneIC50 = 180 nM[6]
5-aminoisoquinolin-1(2H)-oneIC50 = 1800 nM[9]
2-(4-Methoxy-phenyl)-8-methyl-3H-quinazolin-4-oneIC50 = 190 nM[7]
Quinoline-8-carboxamideIC50 = 1900 nM[9]
3-Amino-benzamideIC50 = 19100 nM[7]
2-(4-Azido-phenyl)-8-methoxy-3H-quinazolin-4-oneIC50 = 1930 nM[7]
4-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dioneIC50 = 2000 nM[5]
2-(4-Hydroxy-phenyl)-8-methyl-3H-quinazolin-4-oneIC50 = 220 nM[7]
3-Prop-1-ynylquinoline-8-carboxamideIC50 = 2200 nM[9]
(E)-N-(4-Phenylthiazol-2-yl) cinnamamideIC50 = 224 nM[6]
3-Morpholin-4-ylmethyl-5H-phenanthridin-6-oneIC50 = 23 nM[10]
8-Hydroxy-2-(4-nitro-phenyl)-3H-quinazolin-4-oneIC50 = 230 nM[7]
3-Ethynylquinoline-8-carboxamideIC50 = 2300 nM[9]
2-(4-Chlorophenyl)-2H-indazole-7-carboxamideIC50 = 24 nM[4]
2-phenyl-2H-indazole-7-carboxamideIC50 = 24 nM[4]
4-amino-1,8-naphthalimideIC50 = 26 nM[5]
KU-0058948IC50 = 3.4 nM[12]
8-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-oneIC50 = 300 nM[13]
3-Methylquinoline-8-carboxamideIC50 = 3400 nM[9]
3-Ethylquinoline-8-carboxamideIC50 = 3700 nM[9]
2,8-Dimethyl-3H-quinazolin-4-oneIC50 = 390 nM[7]
1,7,8,9-tetrahydro-1,5-diaza-trindene-4,6-dioneIC50 = 40 nM[5]
NU-1025IC50 = 400 nM[7]
5-amino-3,4-dihydroisoquinolin-1(2H)-oneIC50 = 410 nM[14]
8-Methoxy-2-phenyl-3H-quinazolin-4-oneIC50 = 4200 nM[7]
2-(4-Amino-phenyl)-8-methyl-3H-quinazolin-4-oneIC50 = 440 nM[7]
PD-128763IC50 = 440 nM[7]
KU-58684IC50 = 5 nM[6]
2-Methylquinoline-8-carboxamideIC50 = 500 nM[9]
8-Nitro-6H,11H-indeno[1,2-c]isoquinolin-5-oneIC50 = 500 nM[13]
8-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-oneIC50 = 500 nM[13]
5-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dioneIC50 = 5000 nM[5]
2-(4-Amino-phenyl)-8-hydroxy-3H-quinazolin-4-oneIC50 = 520 nM[7]
2,3-dihydro-1H-benzo[de]isoquinolin-1-oneIC50 = 540 nM[14]
2-phenylpyrazolo-[1,5-a]pyridine-7-carboxamideIC50 = 55 nM[4]
3-Ethenylquinoline-8-carboxamideIC50 = 5800 nM[9]
AZD-2281IC50 = 6 nM[15]
9-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-oneIC50 = 650 nM[13]
2-phenyl-2H-benzo[d][1,2,3]triazole-4-carboxamideIC50 = 71 nM[4]
3-(4-methoxyphenyl)quinoxaline-5-carboxamideIC50 = 71 nM[6]
pyrrolo[3,4-e]indole-1,3(2H,6H)-dioneIC50 = 750 nM[5]
1,2,3,4,4a,5-hexahydrophenanthridin-6(10bH)-oneIC50 = 7500 nM[6]
N-(4-Phenylthiazol-2-yl)isonicotinamideIC50 = 753 nM[6]
4-benzylphthalazin-1(2H)-oneIC50 = 770 nM[6]
8-Methoxy-2-methyl-3H-quinazolin-4-oneIC50 = 780 nM[7]
2-ethylquinoline-8-carboxamideIC50 = 800 nM[9]
3-Hydroxy-benzamideIC50 = 8000 nM[7]
8-Methoxy-2-(4-nitro-phenyl)-3H-quinazolin-4-oneIC50 = 850 nM[7]
3-(4-aminophenyl)quinoxaline-5-carboxamideIC50 = 87 nM[6]
8-Methyl-2-phenyl-3H-quinazolin-4-oneIC50 = 870 nM[7]
2-phenylquinoline-8-carboxamideIC50 = 900 nM[9]
4-(4-Morpholin-4-yl-butyl)-2H-phthalazin-1-oneIC50 = 950 nM[10]
9-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-oneIC50 = 98 nM[13]
ABT-888Ki = 5 nM[16]
AG-014376Ki = 6.4 nM[17]
Ref 1Inflammation. 1995 Jun;19(3):379-87.Modulation of inflammatory arthritis by inhibition of poly(ADP ribose) polymerase. To Reference
Ref 2Curr Top Med Chem. 2005;5(9):869-84.Positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (mGluR2). To Reference
Ref 3PARP inhibitors in ovarian cancer. Hilary Calvert. Newcastle University. To Reference
Ref 4J 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. To Reference
Ref 5Bioorg 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. To Reference
Ref 6J 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. To Reference
Ref 7J 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). To Reference
Ref 8J 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. To Reference
Ref 9J 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. To Reference
Ref 10Bioorg 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. To Reference
Ref 11Bioorg Med Chem Lett. 2007 Jan 15;17(2):542-5. Epub 2006 Oct 10.Novel poly(ADP-ribose) polymerase-1 inhibitors. To Reference
Ref 12J Med Chem. 2009 May 14;52(9):3108-11.Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3. To Reference
Ref 13J 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. To Reference
Ref 14Bioorg 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). To Reference
Ref 15J Med Chem. 2008 Oct 23;51(20):6581-91. Epub 2008 Sep 19.4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. To Reference
Ref 16J 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. To Reference
Ref 17J 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. To Reference



 

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Professor in Department of Pharmacy
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