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312 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28039836 41 Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with inávitro and inávivo antitumor activities.EBI East China Normal University
28006668 1 Design and synthesis of novel 7-aminosubstituted pyrido[2,3-b]pyrazines exhibiting anti-breast cancer activity.EBI Biomedical Research Foundation Academy of Athens (BRFAA)
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.
28129991 2 Identification of allosteric binding sites for PI3Ka oncogenic mutant specific inhibitor design.EBI Johns Hopkins University School of Medicine
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
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
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
27171036 164 Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.EBI University of Nebraska Medical Center
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
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
27217002 96 Discovery of novel 7-azaindoles as PDK1 inhibitors.EBI Merck KGaA
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
27117263 51 Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC┐ inhibitors.EBI Takeda Pharmaceutical Co., Ltd
27084677 16 Computer-aided design, synthesis, and biological evaluation of new indole-2-carboxamide derivatives as PI3Ka/EGFR inhibitors.EBI The University of Jordan
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
26885694 34 Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase III▀.EBI University of California
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
26896709 113 Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.EBI Saarland University
26713102 36 Discovery of Novel and Orally Bioavailable Inhibitors of PI3 Kinase Based on Indazole Substituted Morpholino-Triazines.EBI Sphaera Pharma Pte. Ltd
26741947 24 The Rational Design of Selective Benzoxazepin Inhibitors of thea-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).EBI Genentech
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
26349627 133 Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.EBI The University of Melbourne
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
26119500 22 Discovery of a 6-(pyridin-3-yl)benzo[d]thiazole template for optimization of hedgehog and PI3K/AKT/mTOR dual inhibitors.EBI Soochow University
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
26112437 20 Synthesis and evaluation of pyrrolotriazine based molecules as PI3 kinase inhibitors.EBI Sphaera Pharma Pte. Ltd
26099539 18 Molecular modeling based approach, synthesis, and cytotoxic activity of novel benzoin derivatives targeting phosphoinostide 3-kinase (PI3Ka).EBI Al-Zaytoonah University of Jordan
26087940 287 Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).EBI AstraZeneca
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
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
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
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
25911625 1 Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo.EBI Xi'an Jiaotong 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
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
25765909 1 Design, synthesis and antiproliferative activity evaluation of m-(4-morpholinyl-1,3,5-triazin-2-yl)benzamides in vitro.EBI Xi'an Jiaotong University
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
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
25004409 79 Development and biological evaluation of potent and selective c-KIT(D816V) inhibitors.EBI Korea Advanced Institute of Science and Technology (KAIST)
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
24754609 35 Structural basis for isoform selectivity in a class of benzothiazole inhibitors of phosphoinositide 3-kinase┐.EBI Vertex Pharmaceuticals Inc
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
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)
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
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
25248682 18 Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors.EBI Universit£ de Nantes
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
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
24387221 150 Discovery and optimization of pyrimidone indoline amide PI3K▀ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.EBI Sanofi
24900786 9 Crystal Structures of PI3K? Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design.EBI Shanghai Jiao Tong University
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
23932790 73 A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.EBI Genentech
23867164 27 Identification of GNE-293, a potent and selective PI3Kd inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.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
23414803 9 Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.EBI Celgene Corporation
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
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
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
23265894 40 Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.EBI Genentech Inc
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.
23265889 31 Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation.EBI Chugai Pharmaceutical Co. Ltd
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
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
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
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 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
22575050 40 Design, synthesis, and evaluation of 3,5-disubstituted 7-azaindoles as Trk inhibitors with anticancer and antiangiogenic activities.EBI Korea Advanced Institute of Science and Technology (KAIST)
23063566 70 Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Ka inhibitors.EBI Universit£ de Nantes
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
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)
22771009 9 Discovery of MEK/PI3K dual inhibitor via structure-based virtual screening.EBI Sejong University
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 Vertex Pharmaceuticals Inc
22607682 47 Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor.EBI AstraZeneca
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
22480851 6 Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinasea (PI3Ka) inhibitors.EBI Zhejiang 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
24900269 18 Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.EBI TBA
21067921 13 Discovery of new azaindole-based PI3Ka inhibitors: apoptotic and antiangiogenic effect on cancer cells.EBI Institute of Science and Technology (KAIST)
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
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
19081716 57 Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.EBI GlaxoSmithKline
19297156 43 Exploring the PI3K alpha and gamma binding sites with 2,6-disubstituted isonicotinic derivatives.EBI University of Cincinnati
14593182 34 Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI Pfizer Inc
18501601 1 Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway.EBI Nicholas Piramal Research Centre
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
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
22130133 9 Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.EBI Chinese Academy of Sciences
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
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
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
21945250 5 Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Ka inhibitors.EBI Zhejiang University
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
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
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 Inc
21376583 232 Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.EBI Amgen Inc
21354792 4 Structure-based virtual screening approach to the discovery of phosphoinositide 3-kinase alpha inhibitors.EBI Sejong University
24900229 41 Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.EBI TBA
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
21216595 38 DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.EBI Newcastle University
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 Inc
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
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
20223664 36 Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha.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
19864136 45 Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.EBI Wyeth Research
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
19523825 6 A stabilized demethoxyviridin derivative inhibits PI3 kinase.EBI Harvard Medical School
19362830 47 Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.EBI Wyeth Research
18815050 34 4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.EBI Wyeth Research
18774713 66 Optimization of a series of multi-isoform PI3 kinase inhibitors.EBI UCB Pharma SA
18682324 33 Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.EBI Amgen Inc
18644721 131 Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.EBI UCB Pharma SA
18630894 10 Slow self-activation enhances the potency of viridin prodrugs.EBI Harvard Medical School
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
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
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
26613634 11 Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability.EBI Chugai Pharmaceutical Co. Ltd
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
24345273 111 Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors.EBI Universit£ d'Orl£ans
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
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
30245395 50 Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3K? H1047R mutant inhibitors.EBI Chongqing University
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
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
29631787 21 Discovery and biological evaluation of novel pyrazolopyridine derivatives as potent and orally available PI3K? inhibitors.EBI Astellas Pharma Inc.
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
30034607 60 Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.EBI Shanghai Haiyan Pharmaceutical Technology Co. Ltd.
29407971 15 Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3K?.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
29625382 8 Phthalimide conjugations for the degradation of oncogenic PI3K.EBI Tsinghua University
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.
28633896 13 Design, synthesis and biological evaluation of novel 3H-imidazole [4,5-b] pyridine derivatives as selective mTOR inhibitors.EBI China Pharmaceutical University
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
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
28341403 57 Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.EBI University of Oxford
28462836 4 Iodine catalyzed three component synthesis of 1-((2-hydroxy naphthalen-1-yl)(phenyl)(methyl))pyrrolidin-2-one derivatives: Rationale as potent PI3K inhibitors and anticancer agents.EBI VIT University
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
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
20030517 18 Synthesis and activity of amides of tripeptides as potential urokinase inhibitors.BDB Medical University of Bialystok
20030504 38 Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1.BDB Dublin City University
 42 Ellagitannin and flavonoid constituents from Agrimonia pilosa Ledeb. with their protein tyrosine phosphatase and acetylcholinesterase inhibitory activitiesBDB Catholic University of Daegu
 15 Rational design, synthesis, pharmacophore modeling, and docking studies for identification of novel potent DNA-PK inhibitorsBDB Taibah University
20879713 6 Kinetics and inhibition of nicotinamidase from Mycobacterium tuberculosis.BDB Albert Einstein College of Medicine
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
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
15734645 4 Structural basis for the highly selective inhibition of MMP-13.BDB Aventis Pharma Deutschland GmbH
14741294 72 Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.BDB Merck Frosst Canada & Co.
8027985 66 Tyrosine kinase inhibitors. 3. Structure-activity relationships for inhibition of protein tyrosine kinases by nuclear-substituted derivatives of 2,2'-dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamide).BDB University of Auckland
1552513 36 Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity.BDB Roche Products Limited