PMID

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Article Title

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Development of synthetic lethality anticancer therapeutics.

The University of Texas M.D. Anderson Cancer Center

Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.

Novartis Institutes For Biomedical Research

Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.

Novartis Institutes For Biomedical Research

1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.

Newcastle University

Inhibitors of ATR Kinase for Treatment of Cancer.

Therachem Research Medilab (India)

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Novartis Institutes For Biomedical Research

Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.

Astrazeneca

Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.

Cellzome

Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family.

Astrazeneca

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University of Oxford

Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.

Vertex Pharmaceuticals

Small molecule-based reversible reprogramming of cellular lifespan.

Korea Advanced Institute of Science and Technology

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.

Wyeth Research

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.

Kudos Pharmaceuticals

Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.

Sichuan University

Discovery and Evaluation of 3-Quinoxalin Urea Derivatives as Potent, Selective, and Orally Available ATM Inhibitors Combined with Chemotherapy for the Treatment of Cancer via Goal-Oriented Molecule Generation and Virtual Screening.

Sichuan University

Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.

Novartis Institutes for Biomedical Research

Discovery of novel 7,7-dimethyl-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidines as ATR inhibitors based on structure-based drug design.

Shenyang Pharmaceutical University

Discovery of Thieno[3,2-d]pyrimidine derivatives as potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) kinase.

China Pharmaceutical University

Discovery of [1,2,3]Triazolo[4,5-

Sichuan University

Research progress of mTOR inhibitors.

Jilin University

Discovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo.

Sichuan University

Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8

Astrazeneca

Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.

Csir-Indian Institute of Integrative Medicine

Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.

Hubei Polytechnic University

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.

Indian Institute of Technology (B.H.U.)

7-Azaindole, 2,7-diazaindole, and 1H-pyrazole as core structures for novel anticancer agents with potential chemosensitizing properties.

University Hospital Hradec Kralove

Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.

Newcastle University

Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.

University of Newcastle

BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.

Bayer

Structure-Based Exploration of Selectivity for ATM Inhibitors in Huntington's Disease.

Charles River

Optimization of Potent and Selective Ataxia Telangiectasia-Mutated Inhibitors Suitable for a Proof-of-Concept Study in Huntington's Disease Models.

Chdi Management/Chdi Foundation

Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.

Bayer

Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.

Astrazeneca

The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-

Astrazeneca

Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.

Novartis Institutes For Biomedical Research

Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.

Vertex Pharmaceuticals (Europe)

Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.

China Pharmaceutical University

Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.

Astrazeneca

ATR Inhibitors as Potential Treatment for Cancers.

Therachem Research Medilab

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.

Vertex Pharmaceuticals

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals

Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.

Astrazeneca

Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR).

Integral Biosciences

The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).

Astrazeneca

DELIVERY OF THERAPEUTIC ALKALOID COMPOUNDS

Sensorium Therapeutics

DOPAMINE D3/D2 RECEPTOR MODULATING COMPOUNDS

Richter Gedeon

SMALL-MOLECULAR INHIBITORS FOR THE BETA-CATENIN/ B-CELL LYMPHOMA 9 PROTEIN-PROTEIN INTERACTION

H. Lee Moffitt Cancer Center and Research Institute

COMBINATION THERAPIES OF FASN INHIBITORS WITH THYROID HORMONE RECEPTOR AGONISTS

Sagimet Biosciences

Benzamide and active compound compositions and methods of use

Translational Drug Development

Diarylpyrazole compound, composition comprising same, and use thereof

Shenzhen Targetrx

Nucleoside prodrugs and uses related thereto

Emory University

2,4,6-TRISUBSTITUTED 1,3,5-TRIAZINES AS MODULATORS OF CX3CR1

Astrazeneca

PLASMA KALLIKREIN INHIBITORS

Merck Sharp & Dohme

Bicyclic urea kinase inhibitors and uses thereof

The General Hospital

Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity

Shionogi

Prolyl hydroxylase inhibitors and methods of use

Akebia Therapeutics

Substituted benzimidazoles, their preparation and their use as pharmaceuticals

Epigenetix

Tetrahydroisoquinolines and terahydronaphthyridines for the treatment of hepatitis B virus infection

Hoffmann-La Roche

Azaindoles as inhibitors of HPK1

Genentech

Fused pyrimidine compound or salt thereof

Taiho Pharmaceutical

Compositions and methods for treating disorders of circadian and diurnal rhythms using prokineticin 2 agonists and antagonists

University of California

Pyrimidine compounds as JAK kinase inhibitors

Theravance Biopharma R&D Ip

Substituted piperazines as selective HDAC1,2 inhibitors

Regenacy Pharmaceuticals

Potent and Selective EphA4 Agonists for the Treatment of ALS.

Sanford Burnham Prebys Medical Discovery Institute

Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds

Pfizer

Fused pyrazole derivatives as novel ERK inhibitors

Merck Sharp & Dohme

Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof

Kissei Pharmaceutical

Substituted pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors

Array Biopharma

Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.

University of Kansas

Structural determinants of inhibitor selectivity in prokaryotic IMP dehydrogenases.

Brandeis University

Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain.

Pfizer