PMID

Data

Article Title

Organization

Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.

University Of Bath

Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.

Health & Science University

Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases.

University Of Bath

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.

Biomarin Pharmaceutical

Development and structural analysis of adenosine site binding tankyrase inhibitors.

University Of Oulu

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.

Nerviano Medical Sciences

Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.

University Of Oulu

Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors.

Universit£

Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.

Amgen

Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.

Amgen

Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity.

University Of Oulu

Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.

Novartis Institutes For Biomedical Research

Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.

Novartis Institutes For Biomedical Research

Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.

Amgen

Fragment-based ligand design of novel potent inhibitors of tankyrases.

Nanyang Technological University

Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.

Amgen

Structural basis of selective inhibition of human tankyrases.

Abo Akademi University

[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.

Novartis Institutes For Biomedical Research

Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.

Johns Hopkins University Brain Science Institute

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.

Irbm/Merck Research Laboratories

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.

Abbott Laboratories

Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

Irbm-Merck Research Laboratories Rome

Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.

Irbm-Merck Research Laboratories Rome

Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.

Boehringer Ingelheim Pharmaceuticals