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153 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28591512 114 Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.EBI GlaxoSmithKline
27983846 66 Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.EBI University of Bath
28001384 189 Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.EBI Health & Science University
27163581 110 Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases.EBI University of Bath
26985304 23 Potential Use of Inhibitors of Tankyrases and PARP-1 as Treatment for Cancer and Other Diseases.EBI Therachem Research Medilab (India) Pvt. Ltd.
26652717 96 Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent.EBI BioMarin Pharmaceutical Inc
26706174 46 Development and structural analysis of adenosine site binding tankyrase inhibitors.EBI University of Oulu
26231158 29 Selective inhibition of PARP10 using a chemical genetics strategy.EBI Oregon Health & Science University
26342868 14 Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation.EBI China Pharmaceutical University
26312434 1 Recent developments regarding the use of thieno[2,3-d]pyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties.EBI Xinjiang Technical Institute of Physics and Chemistry
26222319 192 Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.EBI Nerviano Medical Sciences srl
26183543 87 Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.EBI University of Oulu
26088338 50 Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH.EBI University of Malaya
26026769 24 Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases.EBI University of Bath
26061013 55 Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library.EBI Philochem AG
25761096 17 Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.EBI Istituto di Ricerche di Biologia Molecolare
25899312 6 Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.EBI Peking University
25847771 121 Towards small molecule inhibitors of mono-ADP-ribosyltransferases.EBI Karolinska Institutet
25555733 11 Synthesis and biological evaluation of isoindoloisoquinolinone, pyroloisoquinolinone and benzoquinazolinone derivatives as poly(ADP-ribose) polymerase-1 inhibitors.EBI Pondicherry University
25086680 11 Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors.EBI Beijing Institute of Pharmacology and Toxicology
24922587 45 Discovery and structure-activity relationship of novel 2,3-dihydrobenzofuran-7-carboxamide and 2,3-dihydrobenzofuran-3(2H)-one-7-carboxamide derivatives as poly(ADP-ribose)polymerase-1 inhibitors.EBI St. John's University
24815508 29 Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.EBI Chinese Academy of Sciences
24527792 8 Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors.EBI Universit£ degli Studi di Perugia
24521039 5 Nitric oxide (NO) releasing poly ADP-ribose polymerase 1 (PARP-1) inhibitors targeted to glutathione S-transferase P1-overexpressing cancer cells.EBI National Cancer Institute-Frederick
24503274 7 Synthesis, [╣8F] radiolabeling, and evaluation of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors for in vivo imaging of PARP-1 using positron emission tomography.EBI Washington University Saint Louis
24900770 5 Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.EBI University of Oulu
24398383 24 7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors.EBI Universit£ di Milano
24388690 48 Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.EBI R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
24900633 11 Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.EBI Amgen Inc
24900625 52 Design and Discovery of 2-Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases.EBI University of Bath
24188023 32 Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3.EBI Ume£ University
24074844 6 Identification of novel PARP-1 inhibitors by structure-based virtual screening.EBI St. John's University
24116873 16 Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity.EBI University of Oulu
23879431 11 Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.EBI Novartis Institutes for Biomedical Research Incorporated
23844574 71 Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.EBI Novartis Institutes for BioMedical Research
23849206 22 One-pot tandem Hurtley-retro-Claisen-cyclisation reactions in the synthesis of 3-substituted analogues of 5-aminoisoquinolin-1-one (5-AIQ), a water-soluble inhibitor of PARPs.EBI University of Bath
23850199 89 Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors.EBI Takeda California Inc
23701517 12 Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.EBI Amgen Inc
23672613 8 Fragment-based ligand design of novel potent inhibitors of tankyrases.EBI Nanyang Technological University
23522835 7 In silico identification of poly(ADP-ribose)polymerase-1 inhibitors and their chemosensitizing effects against cisplatin-resistant human gastric cancer cells.EBI Sungkyunkwan [corrected] University
23481647 9 Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors.EBI China Pharmaceutical University
23574272 30 Screening and structural analysis of flavones inhibiting tankyrases.EBI University of Oulu
23473053 35 Design, synthesis, and biological evaluation of a series of benzo[de][1,7]naphthyridin-7(8H)-ones bearing a functionalized longer chain appendage as novel PARP1 inhibitors.EBI Chinese Academy of Sciences
23316926 12 Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.EBI Amgen Inc
21413808 170 Synopsis of some recent tactical application of bioisosteres in drug design.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
22766219 67 Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.EBI Abbott Laboratories
22233320 19 Structural basis of selective inhibition of human tankyrases.EBI Abo Akademi University
22260203 73 [1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.EBI Novartis Institutes for BioMedical Research
21634396 55 Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.EBI Cephalon Inc
20565110 7 Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.EBI Karolinska Institutet
17074482 31 Novel poly(ADP-ribose) polymerase-1 inhibitors.EBI Cephalon Inc
12825952 31 Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries.EBI Guilford Pharmaceuticals Inc
11425538 29 Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors.EBI Guilford Pharmaceuticals Inc
22365563 29 Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose)polymerase-1 inhibitors.EBI St. John's University
22153339 27 Novel poly(ADP-ribose) polymerase-1 inhibitors.EBI Cephalon Inc
21692479 27 Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG).EBI University of Arizona
21417348 48 5-Benzamidoisoquinolin-1-ones and 5-(κ-carboxyalkyl)isoquinolin-1-ones as isoform-selective inhibitors of poly(ADP-ribose) polymerase 2 (PARP-2).EBI University of Bath
21174434 13 Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.EBI Cylene Pharmaceuticals
20364863 30 Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.EBI Johns Hopkins University Brain Science Institute
19873981 34 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.EBI IRBM/Merck Research Laboratories
20337371 79 Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.EBI Abbott Laboratories
20189385 18 Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI Jeil Pharmaceutical Co., Ltd
20045315 26 Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.EBI Abbott Laboratories
20031401 54 Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).EBI IRBM/Merck Research Laboratories
20022747 35 Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.EBI Merck Research Laboratories
20015648 94 Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI IRBM-Merck Research Laboratories Rome
20007017 45 Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.EBI IRBM-Merck Research Laboratories Rome
19800803 16 Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors.EBI Sookmyung Women's University
19888760 44 Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.EBI Abbott Laboratories
19553114 38 Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI Abbott Laboratories
19553107 27 Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.EBI IRBM-Merck Research Laboratories Rome
19541484 45 Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.EBI IRBM-Merck Research Laboratories Rome
19354255 10 Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3.EBI Institutet
19125579 58 Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.EBI Huazhong University of Science and Technology
19117416 18 Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.EBI University of Bath
18586490 40 Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.EBI Abbott Laboratories
17804225 33 Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.EBI Astellas Pharma Inc
16359865 22 Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI Cephalon Inc
16290935 17 Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.EBI Cephalon Inc
16290932 33 Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.EBI KuDOS Pharmaceuticals Ltd
16098744 18 4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.EBI Fujisawa Pharmaceutical Co., Ltd
15837300 30 Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.EBI KuDOS Horsham Ltd
15481984 45 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.EBI Pfizer Inc
15293985 33 Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.EBI Fujisawa Pharmaceutical Co., Ltd
15109627 16 Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.EBI University of Newcastle
12852955 25 Design and synthesis of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1,3,4,5-tetrahydro-benzo[c][1,6]- and [c][1,7]-naphthyridin-6-ones.EBI Guilford Pharmaceuticals Inc
12519059 10 Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.EBI Pfizer Inc
12408707 32 Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.EBI Pfizer Inc
12372530 76 Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI Bayer AG
11689065 27 Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.EBI Università di Perugia
11063605 36 Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.EBI Newcastle University
26546219 47 Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.EBI AstraZeneca
26469301 12 Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo.EBI University of Glasgow
30006177 103 4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10.EBI University of Oulu
29107427 13 Targeting Wnt-driven cancers: Discovery of novel tankyrase inhibitors.EBI University of Perugia
30403352 171 Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides.EBI The University of Manchester
29335205 70 Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.EBI Chinese Academy of Sciences
29934219 8 Identification by Inverse Virtual Screening of magnolol-based scaffold as new tankyrase-2 inhibitors.EBI University of Salerno
29456106 19 Design, synthesis and anticancer activities evaluation of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units.EBI China Medical University
29856625 43 Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.EBI University of Pennsylvania
28763648 23 Design, synthesis and biological evaluation of 4-amidobenzimidazole acridine derivatives as dual PARP and Topo inhibitors for cancer therapy.EBI Tsinghua University
28692916 42 Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced inávivo efficacy for cancer therapy.EBI East China University of Science and Technology
29748053 87 Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14.EBI McDaniel College
28622906 52 Discovery of novel quinazoline-2,4(1H,3H)-dione derivatives as potent PARP-2 selective inhibitors.EBI Chinese Academy of Medical Sciences & Peking Union Medical College
28601509 20 Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.EBI Tsinghua University
28445046 1 Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.EBI Regina Elena National Cancer Institute
29155568 29 Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach.EBI Leibniz-Forschungsinstitut f�r Molekulare Pharmakologie (FMP)
28438542 13 Identification of low micromolar dual inhibitors for aldose reductase (ALR2) and poly (ADP-ribose) polymerase (PARP-1) using structure based design approach.EBI Punjabi University
28340412 71 Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with inávivo anti-tumor activity.EBI Chinese Academy of Medical Sciences & Peking Union Medical College
28495083 70 Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14.EBI McDaniel College
 4 Discovery of potent inhibitors of PLproCoV2 by screening a library of selenium-containing compoundsBDB University ofAmsterdam
23488740 12 Novel inhibitor of bacterial sphingomyelinase, SMY-540, developed based on three-dimensional structure analysis.BDB Tokushima Bunri University
21981000 104 Polyphenol fatty acid esters as serine protease inhibitors: a quantum-chemical QSAR analysis.BDB Slovak University of Technology
28196602 16 Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity.BDB Hanoi University of Pharmacy
23864660 3 Crystal structure of 3-hydroxybenzoate 6-hydroxylase uncovers lipid-assisted flavoprotein strategy for regioselective aromatic hydroxylation.BDB Wageningen University
26895387 24 Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.BDB Stony Brook University
8301582 57 Expression and pharmacological characterization of the human D3 dopamine receptor.BDB Neuroscience Research Centre
8169832 9 Characterization of a 5-hydroxytryptamine receptor in mouse neuroblastoma N18TG2 cells.BDB University of Pennsylvania
8161940 9 Melatonin receptors: localization, molecular pharmacology and physiological significance.BDB Rowett Research Institute
8155646 3 Selective activation of inhibitory G-protein alpha-subunits by partial agonists of the human 5-HT1A receptor.BDB Medical University of South Carolina
7908054 71 Characterization of [3H]RX821002 binding to alpha-2 adrenergic receptor subtypes.BDB University of Nebraska
7902811 5 Dopamine D1 receptors: efficacy of full (dihydrexidine) vs. partial (SKF38393) agonists in primates vs. rodents.BDB University of North Carolina
19729306 15 Structure-based design of novel human Pin1 inhibitors (I).BDB Pfizer Inc
19231176 48 Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator.BDB F. Hoffmann-La Roche Inc
18800822 40 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.BDB KuDOS Pharmaceuticals Ltd
19111460 94 Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.BDB Boehringer Ingelheim Pharmaceuticals Inc
16337119 48 Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.BDB Academy of Sciences of the Czech Republic
17035017 25 2,6-Quinolinyl derivatives as potent VLA-4 antagonists.BDB UCB Pharma SA
16806920 32 Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48.BDB Wyeth Research
16162008 146 Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.BDB Abbott Laboratories