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213 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28235701 10 Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors.EBI Peking University
26652969 15 Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.EBI Xi'an Jiaotong University
28109945 25 Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.EBI Hangzhou Xixi Hospital
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University of Sydney
27479483 61 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.EBI CSIR-Indian Institute of Integrative Medicine
27448924 53 Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.EBI Second Military Medical University
27994725 107 Imidazopyridazine Inhibitors of PI3K▀.EBI Dart Neuroscience LLC
27644332 59 Class II Phosphoinositide 3-Kinases as Novel Drug Targets.EBI Curtin University
27115835 85 Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.EBI University of Edinburgh
27353887 9 Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety.EBI Jiangxi Science & Technology Normal University
27096040 17 Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.EBI Genentech
27089211 38 Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI Zhejiang University
27043268 16 Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Ka/mTOR inhibitors.EBI Jiangxi Science & Technology Normal University
26731167 32 Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.EBI Sun Yat-sen University
26819001 29 Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.EBI Second Military Medical University
26318067 34 Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI Hanyang University
26086931 38 Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.EBI Shandong University
26298499 47 The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.EBI Amgen Inc
26210161 15 Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea.EBI Xi'an Jiaotong University
26162498 1 4-(N-Phenyl-N'-substituted benzenesulfonyl)-6-(4-hydroxyphenyl)quinolines as inhibitors of mammalian target of rapamycin.EBI India Academy of Scientific & Innovative Research (AcSIR)
25980912 41 Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.EBI AstraZeneca
26102506 40 Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.EBI Celgene Corporation
26083478 66 Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.EBI Celgene Corporation
25893045 44 Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.EBI PKUCare Pharmaceutical R & D Center
25835317 63 Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.EBI Sichuan University
25659752 16 Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Ka inhibitors.EBI Jiangxi Science & Technology Normal University
25643210 16 Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.EBI AstraZeneca
25387153 53 Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.EBI University Hospital Hradec Kralove
25139570 31 Synthesis and structure-activity relationships of PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives.EBI PKUCare Pharmaceutical R & D Center
25086238 13 Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.EBI Shenyang Pharmaceutical University
24893124 4 Development of synthetic lethality anticancer therapeutics.EBI The University of Texas M.D. Anderson Cancer Center
25589928 37 Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.EBI Novartis Institutes for BioMedical Research
25589927 36 Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.EBI Novartis Institutes for BioMedical Research
25589915 41 Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.EBI Monash University (Parkville Campus)
25468038 8 Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors.EBI TBA
25466188 21 Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.EBI Amgen Inc
25440879 13 Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.EBI Shenyang Pharmaceutical University
24805946 25 Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness.EBI Northeastern University
24773549 20 Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.EBI Development Center for Biotechnology
24433860 60 Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors.EBI PKUCare Pharmaceutical R & D Center
24393580 6 Virtual screening and biochemical evaluation to identify new inhibitors of mammalian target of rapamycin (mTOR).EBI Sejong University
24387221 150 Discovery and optimization of pyrimidone indoline amide PI3K▀ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.EBI Sanofi
24091081 49 Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.EBI Merck Research Laboratories
23855836 147 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.EBI Newcastle University
23932790 73 A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.EBI Genentech
23726034 117 Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.EBI Novartis Institutes for BioMedical Research
23662903 34 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): a▀-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.EBI Genentech
23540645 140 Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase▀ isoform.EBI Genentech Inc
23506825 71 Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.EBI Pfizer Inc
23414803 9 Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.EBI Celgene Corporation
23473235 21 Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).EBI Genentech
23448267 17 Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1.EBI GlaxoSmithKline
23375793 26 Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.EBI AstraZeneca
24900569 25 Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.EBI Genentech
24900568 27 Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.EBI Pfizer Inc
23410005 147 Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.EBI The University of Arizona
23394205 106 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 AstraZeneca
10843203 12 Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.EBI Glaxo Wellcome
22520259 65 Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor.EBI Spanish National Cancer Research Centre (CNIO)
22832322 40 Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.EBI Amgen Inc
22726925 216 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.EBI Cellzome Ltd
23199076 28 Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.EBI Genentech
22946614 9 The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinasea.EBI Genentech
23063403 21 Recent results in protein kinase inhibition for tropical diseases.EBI Montclair State University
22897589 100 Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.EBI Amgen Inc
22765895 72 Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.EBI Amgen Inc
22548365 293 Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.EBI Amgen Inc
23021994 108 Identification of pyrimidine derivatives as hSMG-1 inhibitors.EBI Pfizer Inc
22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis Inc
22981333 103 Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kß inhibitors.EBI Sanofi
22863202 94 Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.EBI Novartis Institutes for BioMedical Research
22765900 24 Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors.EBI Pfizer Inc
22524426 281 Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kß inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.EBI Sanofi Research & Development
22819764 35 Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.EBI Spanish National Cancer Research Centre (CNIO)
22749419 22 Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Ka and mTOR.EBI Pfizer Inc
22607682 47 Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor.EBI AstraZeneca
22475557 75 Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potentß isoform selective phosphatidylinositol 3-kinase inhibitors.EBI GlaxoSmithKline
24900266 24 Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.EBI TBA
24900269 18 Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.EBI TBA
21353571 26 Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.EBI Hanyang University
20166697 71 Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.EBI Wyeth Research
17350953 3 The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain.EBI Stanford University
16134928 34 Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.EBI The Scripps Research Institute
15369399 3 A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma.EBI Novartis Institutes for BioMedical Research and Novartis Pharma Development
22325943 71 Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.EBI Spanish National Cancer Research Centre (CNIO)
22136433 67 7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.EBI Ludwig-Maximilians University of Munich
21978683 78 Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.EBI Celgene Corporation
22197143 17 Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors.EBI S*BIO Pte Ltd
22040023 63 Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).EBI Pfizer Inc
22177407 104 Novel pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.EBI University of Auckland
22177405 104 Discovery of pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors.EBI University of Auckland
21981714 48 Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.EBI Genentech
22014755 36 Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI Hanyang University
21612232 113 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 Amgen Inc
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21936542 143 Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.EBI Novartis Institute for BioMedical Research
21714526 54 Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.EBI Amgen Inc
21763134 57 Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.EBI Pfizer Inc
20561789 6 Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.EBI Sanofi-Aventis
21636270 27 Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.EBI Genentech Inc
21621413 24 Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.EBI Dana-Farber Cancer Institute Inc
21495671 95 Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.EBI Genentech
21438579 4 Isolation and structure of homotemsirolimuses A, B, and C.EBI Wyeth Research
21332118 157 Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.EBI Amgen Inc
21413798 174 Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.EBI Vertex Pharmaceuticals Inc
21388141 22 Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.EBI Korea Advanced Institute of Science and Technology
21376583 232 Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.EBI Amgen Inc
21316229 12 Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.EBI Chugai Pharmaceutical Co. Ltd
24900252 33 Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase InhibitorsEBI TBA
21269826 39 Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.EBI Pfizer Inc
21062009 70 Design, Synthesis, and Structure−Activity Relationships of 3-Ethynyl-1H-indazoles as Inhibitors of the Phosphatidylinositol 3-Kinase Signaling PathwayEBI TBA
20860370 83 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 Dana-Farber Cancer Institute Inc
20822905 28 Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.EBI Genentech
20817449 19 4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.EBI Pfizer Inc
20797855 63 PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.EBI Pfizer Inc
20483602 23 5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.EBI Wyeth Research
20363128 42 Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.EBI Wyeth Research
19894727 164 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.EBI Wyeth Research
20346656 25 Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.EBI Genentech
20334367 78 Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.EBI Wyeth Research
20307980 22 B-Raf kinase inhibitors: hit enrichment through scaffold hopping.EBI Wyeth Research
20303263 87 Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies.EBI Wyeth Research
20223663 100 2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.EBI Wyeth Research
20188552 75 Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI Wyeth Research
20188551 56 4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI Wyeth Research
19884006 47 Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI Wyeth Research
20166671 85 Selectively nonselective kinase inhibition: striking the right balance.EBI Schering-Plough
20050669 61 Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.EBI Genentech
19762236 9 The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.EBI KuDOS Pharmaceuticals Ltd
19968288 83 Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.EBI Wyeth Research
20089401 46 Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.EBI Wyeth Research
19969455 70 Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.EBI Wyeth Research
19963384 26 Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI Wyeth Research
19954970 64 Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.EBI Wyeth Research
19897362 52 Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K.EBI Wyeth Research
19896845 54 Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.EBI Wyeth Research
19733066 25 Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.EBI KuDOS Pharmaceuticals Ltd
19916508 76 Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.EBI Wyeth Research
19362830 47 Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.EBI Wyeth Research
19317452 155 Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.EBI Wyeth Research
18815050 34 4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.EBI Wyeth Research
18644721 131 Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.EBI UCB Pharma SA
17562705 6 Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.EBI Stony Brook University
16185865 4 Rapamycin analogs with reduced systemic exposure.EBI Abbott Laboratories
16143526 1 Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases.EBI Chinese Academy of Sciences
15658870 104 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 Newcastle University
15546735 25 Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.EBI University of Newcastle
10411471 19 Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.EBI Abbott Laboratories
26996374 75 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 AstraZeneca
26505898 123 Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.EBI Novartis Institutes for Biomedical Research
26596710 27 Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.EBI Zhejiang University
24345273 111 Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors.EBI Universit£ d'Orl£ans
30359003 104 Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.EBI University of Basel
30015070 8 Synthesis and anticancer activity of new dihydropyrimidinone derivatives.EBI Mansoura University
30380865 19 Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.EBI University of California San Diego
30346772 124 Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.EBI AstraZeneca
29541370 41 Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.EBI WuXi AppTec (Shanghai) Co. Ltd.
30077608 24 Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3K?.EBI China Pharmaceutical University
29945756 29 Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3K?/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity.EBI Nanjing University of Chinese Medicine
29305298 28 Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.EBI Chinese Academy of Medical Sciences and Peking Union Medical College
30128072 68 Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.EBI AstraZeneca
30034607 60 Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.EBI Shanghai Haiyan Pharmaceutical Technology Co. Ltd.
29466002 193 Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.EBI University of Edinburgh
29017786 35 Identification of novel PI3K inhibitors through a scaffold hopping strategy.EBI Spanish National Cancer Research Centre (CNIO)
29683659 127 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 AstraZeneca
29927604 90 Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.EBI Chinese Academy of Medical Sciences and Peking Union Medical College
29107429 7 Discovery of 1-(3-aryl-4-chlorophenyl)-3-(p-aryl)urea derivatives against breast cancer by inhibiting PI3K/Akt/mTOR and Hedgehog signalings.EBI Tsinghua University
28947947 112 Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.EBI Novartis Institutes for BioMedical Research
28835784 77 Potential of PI3K? Inhibitors in the Treatment of Cancer and Other Diseases.EBI Therachem Research Medilab (India) Pvt. Ltd.
28633896 13 Design, synthesis and biological evaluation of novel 3H-imidazole [4,5-b] pyridine derivatives as selective mTOR inhibitors.EBI China Pharmaceutical University
28409639 83 Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.EBI West China Hospital of Sichuan University
28259529 31 Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.EBI The Ohio State University
28526367 30 Discovery of a novel aminopyrazine series as selective PI3K? inhibitors.EBI AstraZeneca
29308895 24 Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer.EBI Nankai University
28571824 65 Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3K?/mTOR inhibitors.EBI Temple University
28829592 109 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 University of Basel
28347666 45 Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours.EBI AstraZeneca
22957724 30 Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors.BDB Dumlupinar University
22188522 45 Sulfapyridine-like benzenesulfonamide derivatives as inhibitors of carbonic anhydrase isoenzymes I, II and VI.BDB Ataturk University
21635211 12 Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products.BDB AtatŘrk University
20030504 38 Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1.BDB Dublin City University
27595330 6 Small-molecule WNK inhibition regulates cardiovascular and renal function.BDB Novartis Institutes
12815170 15 [125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding.BDB Abbott Laboratories
11907190 4 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A): a potent and selective corticotrophin-releasing factor(1) receptor antagonist. I. Biochemical and pharmacological characterization.BDB Sanofi Synthelabo
11882920 41 Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols.BDB Institut de Recherches Servier
11303063 11 Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland.BDB Creighton University
12616631 18 D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.BDB University of Queensland Brisbane
19012568 7 Binding properties of the C-terminal domain of VIAF.BDB The Burnham Institute for Medical Research
16873019 6 MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.BDB GPC Biotech Incorporated
18817367 28 Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.BDB Abbott Laboratories
17574423 44 Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.BDB Pfizer Inc
17352464 51 Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.BDB Abbott Laboratories
8879560 22 Structure-activity relationships of HIV-1 PR inhibitors containing AHPBA--II. Modification of pyrrolidine ring at P1' proline.BDB Sankyo Co., Ltd
8893827 17 Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.BDB Upjohn