PMID

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Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.

Nerviano Medical Sciences

MutT Homolog 1 (MTH1): The Silencing of a Target.

Nerviano Medical Sciences

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

Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.

Nerviano Medical Sciences

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.

Nerviano Medical Sciences

Discovery of 2-(cyclohexylmethylamino)pyrimidines as a new class of reversible valosine containing protein inhibitors.

Nerviano Medical Sciences

Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.

Nerviano Medical Sciences

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).

Nerviano Medical Sciences

4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.

Nerviano Medical Sciences

Structure-based optimization of potent PDK1 inhibitors.

Nerviano Medical Sciences

Through the"gatekeeper door": exploiting the active kinase conformation.

Nerviano Medical Sciences

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Nerviano Medical Sciences

5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.

Nerviano Medical Sciences

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Nerviano Medical Sciences

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

Nerviano Medical Sciences

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Nerviano Medical Sciences

Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.

Nerviano Medical Sciences

Identification of unprecedented ATP-competitive choline kinase inhibitors.

Nerviano Medical Sciences

Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515.

Nerviano Medical Sciences

Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.

Nerviano Medical Sciences

Urea-substituted aromatic ring-linked dioxinoquinoline compounds, preparation method and uses thereof

Beijing Scitech-Mq Pharmaceuticals

Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof

Washington University

Triazole phenyl compounds as agonists of the APJ receptor

Amgen

1,8-naphthyridinone compounds and uses thereof

Nuvation Bio

Process of making somatostatin modulators

Crinetics Pharmaceuticals

Substituted bipiperidinyl derivatives

Bayer Pharma Aktiengesellschaft

Substituted piperidinyltetrahydroquinolines

Bayer Pharma Aktiengesellschaft

Branched 3-phenylpropionic acid derivatives and their use

Bayer Pharma Aktiengesellschaft

Inhibitors of human immunodeficiency virus replication

Viiv Healthcare UK (NO.5)

Oxazine derivatives and their use in the treatment of disease

Novartis

Benzoic acid derivatives

Hoffmann-La Roche

Substituted imidazo[1,2-B]pyridazines

Bayer Intellectual Property

Bivalent diazo bicyclic Smac mimetics and the uses thereof

The Regents of The University of Michigan

4-substituted-2-amino-pyrimidine derivatives

Abbvie

Azinone-substituted azapolycycle MCH-1 antagonists, methods of making, and use thereof

Albany Molecular Research

Chromane derivatives as TRPV3 modulators

Glenmark Pharamceuticals

Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.

Taisho Pharmaceutical

High affinity antagonists of the vanilloid receptor.

National Cancer Institute-Bethesda

[125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.

Novartis Pharma

A novel competitive class of α-glucosidase inhibitors: (E)-1-phenyl-3-(4-styrylphenyl)urea derivatives.

Gyeongsang National University

Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties.

Dainippon Pharmaceutical

Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase.

New York University

The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action.

Novo Industri

Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.

Seattle Veterans Affairs Medical Center

Characterization of [3H]quinpirole binding to D2-like dopamine receptors in rat brain.

Dupont Pharmaceuticals

Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.

Novartis Pharmaceuticals

Structural analysis of inhibitor binding to human carbonic anhydrase II.

University of Pennsylvania

Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.

University of Pennsylvania

Synthesis of potent C(2)-symmetric, diol-based hiv-1 protease inhibitors. Investigation of thioalkyl and thioaryl P1/P1' substituents.

Stockholm University

Role of inhibitor aliphatic chain in the thermodynamics of inhibitor binding to Escherichia coli enoyl-ACP reductase and the Phe203Leu mutant: a proposed mechanism for drug resistance.

University of Alabama At Birmingham