91 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
La Trobe University
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Celgene
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University Hospital Hradec Kralove
Development of synthetic lethality anticancer therapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The University of Texas M.D. Anderson Cancer Center
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Monash University (Parkville Campus)
Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sanofi
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Newcastle University
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): aß-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Exelixis
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
La Trobe University
Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Oxford
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Synthesis, structural elucidation, DNA-PK inhibition, homology modelling and anti-platelet activity of morpholino-substituted-1,3-naphth-oxazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
La Trobe University
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Dana-Farber Cancer Institute
DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Newcastle University
Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Dana-Farber Cancer Institute
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Newcastle University
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kudos Pharmaceuticals
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Newcastle University
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Stony Brook University
Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Newcastle University
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
School of Natural Sciences--Chemistry
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hubei Polytechnic University
Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zhuhai Campus of Zunyi Medical University
Synthesis and biological evaluation of 4H-benzo[e][1,3]oxazin-4-ones analogues of TGX-221 as inhibitors of PI3K?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
La Trobe University
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Newcastle University
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Newcastle
BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bayer
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Harvard Medical School
Structure-Based Exploration of Selectivity for ATM Inhibitors in Huntington's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Charles River
2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Newcastle
Synthetic Lethality through the Lens of Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Istituto Italiano Di Tecnologia
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
A*Star
Optimization of Potent and Selective Ataxia Telangiectasia-Mutated Inhibitors Suitable for a Proof-of-Concept Study in Huntington's Disease Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chdi Management/Chdi Foundation
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3K? Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Newcastle University
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Department of Molecular Oncogenesis
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bayer
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline R&D
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals (Europe)
Evolution of PI3K? and ? Inhibitors for Inflammatory and Autoimmune Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cleave Biosciences
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
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).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinase? (PI3K?) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Synthesis and biological evaluation of 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones against DNA-PK, PI3K, PDE3A enzymes and platelet aggregation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
La Trobe University
Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nankai University
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Basel
Kinetic and in silico analysis of thiazolidin-based inhibitors of a-carbonic anhydrase isoenzymes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Ondokuz Mayis University
[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Abbott Laboratories
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of California San Francisco
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Ono Pharmaceutical