new BindingDB logo
myBDB logout

206 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28591512 114 Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.EBI A GlaxoSmithKline Company
28017532 140 Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors.EBI AstraZeneca
26652969 15 Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.EBI Xi'an Jiaotong University
28108251 50 Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kd inhibitors.EBI Bristol-Myers Squibb
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
27541357 58 Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.EBI National University of Singapore
28105286 65 Discovery of a Potent, Selective, and Orally Available PI3Kd Inhibitor for the Treatment of Inflammatory Diseases.EBI Rhône-Poulenc Rorer
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
27816514 103 Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.EBI Novartis Institutes for BioMedical Research
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
27994757 41 Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kd.EBI Pvt. Ltd.
27994725 107 Imidazopyridazine Inhibitors of PI3K▀.EBI Dart Neuroscience LLC
27765510 8 Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity.EBI La Trobe University
28004945 52 Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase III▀ (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology.EBI Academy of Sciences of the Czech Republic
27391133 76 Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening.EBI University of Berne
27644332 59 Class II Phosphoinositide 3-Kinases as Novel Drug Targets.EBI Curtin University
27774127 75 Discovery of a Series of 5,11-Dihydro-6EBI Dana-Farber Cancer Institute
27660692 70 Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-┐ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.EBI Infinity Pharmaceuticals, Inc.
27186676 186 Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.EBI West China Hospital of Sichuan University
27217002 96 Discovery of novel 7-azaindoles as PDK1 inhibitors.EBI Merck KGaA
27043133 16 A Prospective Virtual Screening Study: Enriching Hit Rates and Designing Focus Libraries To Find Inhibitors of PI3Kd and PI3K┐.EBI Janssen Research& Development
26885694 34 Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase III▀.EBI University of California
26951753 336 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for BioMedical Research
26819669 39 Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.EBI Novartis Institutes for BioMedical Research
26896709 113 Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.EBI Saarland 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
26854431 47 Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.EBI La Trobe 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
26774655 32 Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.EBI Novartis Institutes for BioMedical Research
26720154 32 (E)-1,3-diphenyl-1H-pyrazole derivatives containing O-benzyl oxime moiety as potential immunosuppressive agents: Design, synthesis, molecular docking and biological evaluation.EBI Anhui Agricultural 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.
26164189 21 Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Ka inhibitor with high PI3K isoform selectivity and potent cellular activity.EBI Novartis Institutes for BioMedical Research
26199119 135 Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.EBI Novartis Institutes for BioMedical Research
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
26087940 287 Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).EBI AstraZeneca
26037808 75 Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Ka inhibitors.EBI Cairo University
25980912 41 Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.EBI AstraZeneca
25890697 6 Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.EBI Punjabi University
26121481 37 Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase┐.EBI Vertex Pharmaceuticals Inc.
26005528 41 Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).EBI GlaxoSmithKline
25893045 44 Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.EBI PKUCare Pharmaceutical R&D Center
25643210 16 Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.EBI AstraZeneca
25514658 182 Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3K▀ and PI3Kd for the treatment of PTEN-deficient cancers.EBI AstraZeneca
25827523 275 Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.EBI Vertex Pharmaceuticals Inc.
25693787 44 6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Ka.EBI Nanjing University
25666823 90 Synthesis and SAR study of potent and selective PI3Kd inhibitors.EBI Amgen Inc.
25415535 118 Inhibitors of c-Jun N-terminal kinases: an update.EBI Eberhard Karls Universit£t T£bingen
25387153 53 Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.EBI University Hospital Hradec Kralove
25050878 98 Discovery of nanomolar phosphoinositide 3-kinase gamma (PI3K┐) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.EBI The University of Jordan
25042253 52 Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3K▀ inhibitors, useful as antiplatelet agents.EBI AstraZeneca
24992874 58 Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3K▀/d inhibitors for the treatment of PTEN-deficient tumours.EBI AstraZeneca
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
24754609 35 Structural basis for isoform selectivity in a class of benzothiazole inhibitors of phosphoinositide 3-kinase┐.EBI Vertex Pharmaceuticals Inc.
25589920 72 Quinalozinones as Inhibitors of Class I PI3K Kinases.EBI Dart Neuroscience LLC
25589915 41 Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.EBI Monash University (Parkville Campus)
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
24560540 119 Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3K▀ inhibitors.EBI Sanofi
23944386 55 Discovery of selective small molecule type III phosphatidylinositol 4-kinase alpha (PI4KIIIa) inhibitors as anti hepatitis C (HCV) agents.EBI GlaxoSmithKline
24387221 150 Discovery and optimization of pyrimidone indoline amide PI3K▀ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.EBI Sanofi
24262886 23 Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase┐ inhibitor for the treatment of inflammatory diseases.EBI Taisho Pharmaceutical Co., Ltd
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
23820386 32 Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.EBI Novartis Institutes for Biomedical Research
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.
23394126 170 Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI Exelixis
23375793 26 Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.EBI AstraZeneca
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
23265896 36 Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase.EBI Monash Institute of Pharmaceutical Sciences
23795239 62 L-Aminoacyl-triazine derivatives are isoform-selective PI3K? inhibitors that target non-conserved Asp862 of PI3K?EBI Monash University (Parkville Campus)
23360348 11 Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Ka.EBI Celgene Avilomics Research
22520259 65 Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor.EBI Spanish National Cancer Research Centre (CNIO)
24900504 107 Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.EBI TBA
22924688 128 PI3Kd and PI3K¿ as targets for autoimmune and inflammatory diseases.EBI Amgen Inc.
23122859 43 Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase¿ inhibitors.EBI Taisho Pharmaceutical Co., Ltd
23059543 39 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 La Trobe University
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
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.
22877085 33 Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.EBI Genentech
22876881 72 Discovery and in vivo evaluation of dual PI3Kß/d inhibitors.EBI Amgen Inc.
23010262 46 Discovery of phosphoinositide 3-kinases (PI3K) p110ß isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance.EBI AstraZeneca
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.
23010274 48 Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110ß isoform inhibitors through structure-based fragment optimisation.EBI AstraZeneca
22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis
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
22819766 173 SAR studies around a series of triazolopyridines as potent and selective PI3K¿ inhibitors.EBI Cellzome Ltd
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
22727369 6 Design, synthesis, biological evaluation and molecular modeling of novel 1,3,4-oxadiazole derivatives based on Vanillic acid as potential immunosuppressive agents.EBI Nanjing University
22819764 35 Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.EBI Spanish National Cancer Research Centre
22738635 87 Discovery of novel PI3K¿/d inhibitors as potential agents for inflammation.EBI Cellzome Ltd
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd
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
20138514 93 3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI Vertex Pharmaceuticals Inc
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
19297156 43 Exploring the PI3K alpha and gamma binding sites with 2,6-disubstituted isonicotinic derivatives.EBI University of Cincinnati
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18248814 24 Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.EBI Novartis Institute for BioMedical Research
17339109 33 Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.EBI Astellas Pharma Inc.
22361133 148 Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.EBI GlaxoSmithKline
22336246 7 JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs.EBI Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics
22325943 71 Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.EBI Spanish National Cancer Research Centre (CNIO). C/Melchor Fern£ndez Almagro 3
21985639 70 Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.EBI Genentech
22300886 5 Synthesis, molecular docking and biological evaluation of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.EBI Nanjing University
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
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
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.
21925880 14 Fragment based discovery of a novel and selective PI3 kinase inhibitor.EBI Pfizer Inc.
21882832 116 Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).EBI University of Auckland
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
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.
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
21332118 157 Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.EBI Amgen Inc.
21450467 261 Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).EBI National Human Genome Research Institute
21341675 266 Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.EBI GlaxoSmithKline
21322566 61 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 Dana Farber Cancer Institute
21376583 232 Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.EBI Amgen Inc
21353551 23 Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.EBI OSI Pharmaceuticals, 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
21216151 66 Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.EBI The Institute of Cancer Research
21169017 63 Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening.EBI AstraZeneca R&D M£lndal
21062009 70 Design, Synthesis, and Structure−Activity Relationships of 3-Ethynyl-1H-indazoles as Inhibitors of the Phosphatidylinositol 3-Kinase Signaling PathwayEBI TBA
21121631 28 Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal.EBI University of British Columbia
21035331 32 Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.EBI Novartis Institutes for Biomedical Research
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
20822905 28 Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.EBI Genentech
20797855 63 PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.EBI Pfizer Inc.
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20081827 52 The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.EBI Medical Research Council-Laboratory of Molecular Biology
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
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
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
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
19969455 70 Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.EBI Wyeth Research
19954970 64 Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.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
18774713 66 Optimization of a series of multi-isoform PI3 kinase inhibitors.EBI UCB
18644721 131 Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.EBI UCB
18625552 88 4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.EBI UCB
16789742 65 Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.EBI Serono Pharmaceutical Research Institute
28209465 124 Identification of highly potent and selective PI3K? inhibitors.EBI Bristol-Myers Squibb Company
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
28404374 81 Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.EBI Spanish National Cancer Research Centre (CNIO)
28541707 119 Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders.EBI Bristol-Myers Squibb Company
28520415 91 Design and Synthesis of Soluble and Cell-Permeable PI3K? Inhibitors for Long-Acting Inhaled Administration.EBI AstraZeneca
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
22214210 32 Synthesis and binding study of certain 6-arylalkanamides as molecular probes for cannabinoid receptor subtypes.BDB Cairo University
24356970 37 Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.BDB University of Texas Southwestern Medical Center
14573386 17 Comparison of effects of dual transporter inhibitors on monoamine transporters and extracellular levels in rats.BDB Lilly Research Laboratories
1346637 120 Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells.BDB Mayo Clinic Jacksonville
1328199 8 Cloning of a novel somatostatin receptor, SSTR3, coupled to adenylylcyclase.BDB University of Chicago
1325033 19 Receptor occupancy and adenylate cyclase activation in AR 4-2J rat pancreatic acinar cell membranes by analogs of pituitary adenylate cyclase-activating peptides amino-terminally shortened or modified at position 1, 2, 3, 20, or 21.BDB Universit´ Libre de Bruxelles
19090918 33 Inhibitors of tubulin assembly identified through screening a compound library.BDB The Ohio State University
19012568 7 Binding properties of the C-terminal domain of VIAF.BDB The Burnham Institute for Medical Research
18662878 12 4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase.BDB Anadys Pharmaceuticals
19209891 34 New Insights into the Design of Inhibitors of Human S-Adenosylmethionine Decarboxylase: Studies of Adenine C(8) Substitution in Structural Analogues of S-Adenosylmethionine (dagger).BDB Cornell University
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
17095227 26 Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma.BDB Pfizer
14722321 9 A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.BDB Johnson & Johnson Pharmaceutical
18269228 93 Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.BDB Wyeth Research
11520201 10 X-Ray crystal structures of Candida albicans dihydrofolate reductase: high resolution ternary complexes in which the dihydronicotinamide moiety of NADPH is displaced by an inhibitor.BDB GSK
17574423 44 Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.BDB Pfizer
17132624 2 Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors.BDB Johnson & Johnson Pharmaceutical
15734645 4 Structural basis for the highly selective inhibition of MMP-13.BDB Aventis Pharma Deutschland GmbH
15217611 14 Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms.BDB Vernalis (R&D) Ltd
17352464 51 Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.BDB Abbott Laboratories
17149864 69 Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.BDB University of Massachusetts Medical School
16616489 29 Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.BDB Institut Curie
22552008 7 Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.BDB Celgene
8893827 17 Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.BDB Upjohn