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190 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
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 Co.
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University of Sydney
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
27387421 34 Discovery and antiplatelet activity of a selective PI3K▀ inhibitor (MIPS-9922).EBI Monash University
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
27644332 59 Class II Phosphoinositide 3-Kinases as Novel Drug Targets.EBI Curtin University
27575470 12 Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.EBI Novartis Institutes for BioMedical Research
27774129 2 Concise SAR Exploration Based on the"Head-to-Tail" Approach: Discovery of PI4KIIIa Inhibitors Bearing Diverse Scaffolds.EBI Japan Tobacco Inc
27774127 75 Discovery of a Series of 5,11-Dihydro-6EBI Dana-Farber Cancer Institute Inc
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
26951750 59 Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for BioMedical Research
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
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
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
25890698 135 Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.EBI University of Auckland
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
25387153 53 Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.EBI University Hospital Hradec Kralove
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
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
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
24387221 150 Discovery and optimization of pyrimidone indoline amide PI3K▀ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.EBI Sanofi
24900751 6 Inhibitors of PI3K? as Potential Treatment for Cancer.EBI Therachem Research Medilab (India) Pvt. 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 Inc
23375793 26 Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.EBI AstraZeneca
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, Inc.
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
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
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
22765895 72 Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR 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
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 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
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
22819764 35 Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.EBI Spanish National Cancer Research Centre (CNIO)
22738635 87 Discovery of novel PI3K¿/d inhibitors as potential agents for inflammation.EBI Cellzome Ltd
22168626 32 Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.EBI Ambit Biosciences
22520630 21 Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.EBI Nanjing University
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
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
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
21985639 70 Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.EBI Genentech
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
22030027 12 Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kß) inhibitors with selectivity over PI3Ka.EBI Institute of Science and Technology (KAIST)
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
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
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
21636270 27 Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.EBI Genentech Inc
21332118 157 Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.EBI Amgen 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
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
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
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
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
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
19748269 21 Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.EBI University of Auckland
19916508 76 Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.EBI Wyeth Research
18774713 66 Optimization of a series of multi-isoform PI3 kinase inhibitors.EBI UCB Pharma SA
18644721 131 Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.EBI UCB Pharma SA
18625552 88 4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.EBI UCB Pharma SA
17869522 51 Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.EBI University of Auckland
16789742 65 Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.EBI Serono Pharmaceutical Research Institute
28106991 136 Discovery of a Phosphoinositide 3-Kinase (PI3K) ?/? Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3K? Potency in a PI3K?-Selective Template by Targeting Nonconserved Asp856.EBI Gilead Sciences, Inc.
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
26206504 131 Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.EBI Novartis Institutes for BioMedical Research
24900655 165 [3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase ? Inhibitors.EBI GlaxoSmithKline
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
30071408 56 Difuran-substituted quinoxalines as a novel class of PI3K? H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.EBI Chongqing 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
30245395 50 Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3K? H1047R mutant inhibitors.EBI Chongqing University
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
29937355 8 Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3K? inhibitors.EBI Shenyang Pharmaceutical University
29601991 22 Discovery of novel quinazolinone derivatives as high potent and selective PI3K? and PI3K?/? inhibitors.EBI Shandong University
29559278 99 Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.EBI AstraZeneca
29534936 30 Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3K?) inhibitors.EBI Xi'an Jiaotong University
29486969 14 Design and synthesis of 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3K? isoform selective activity.EBI India Academy of Scientific & Innovative Research (AcSIR)
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
29407971 15 Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3K?.EBI Shenyang Pharmaceutical University
28835805 45 Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.EBI Fudan University
28800461 16 Design, synthesis, and biological evaluation of novel 3-substituted imidazo[1,2-a]pyridine and quinazolin-4(3H)-one derivatives as PI3K? inhibitors.EBI Shenyang Pharmaceutical University
30053721 184 Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3K?) inhibitor.EBI Chinese Academy of Sciences
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
29057057 54 From PIM1 to PI3K? via GSK3?: Target Hopping through the Kinome.EBI GlaxoSmithKline
28947947 112 Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.EBI Novartis Institutes for BioMedical Research
29852070 101 Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors.EBI Pharmaron-Beijing Co., Ltd
28835793 32 Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168).EBI University of Michigan
28835784 77 Potential of PI3K? Inhibitors in the Treatment of Cancer and Other Diseases.EBI Therachem Research Medilab (India) Pvt. Ltd.
28128944 96 Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase? (PI3K?) Inhibitors.EBI University Park Nottingham
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
27846451 60 SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3K?) inhibitors.EBI Shanghai Institute of Materia Medica (SIMM)
28526367 30 Discovery of a novel aminopyrazine series as selective PI3K? inhibitors.EBI AstraZeneca
28209465 124 Identification of highly potent and selective PI3K? inhibitors.EBI Bristol-Myers Squibb Co.
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
28541707 119 Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders.EBI Bristol-Myers Squibb Co.
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
23663081 49 Design, synthesis and biological evaluation of novel inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors.BDB Nycomed
20222761 21 Semisynthesis of alpha-methyl-gamma-lactones and in vitro evaluation of their activity on protein farnesyltransferase.BDB UFR des Sciences Pharmaceutiques et IngÚnierie de la SantÚ
12232544 79 [Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine].BDB Emory University
9015795 50 Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.BDB University of Toronto
6271132 14 Prostacyclin receptors of a neuronal hybrid cell line. Divalent citations and ligand-receptor coupling.BDB Royal Postgraduate Medical School
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
16873019 6 MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.BDB GPC Biotech Incorporated
14722321 9 A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.BDB Johnson & Johnson Pharmaceutical
17574423 44 Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.BDB Pfizer Inc
15734645 4 Structural basis for the highly selective inhibition of MMP-13.BDB Aventis Pharma Deutschland GmbH
12014965 38 Homodimeric tacrine congeners as acetylcholinesterase inhibitors.BDB National Defense Medical Center