The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28591512 |
114 |
Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines. |
Glaxosmithkline |
28017532 |
140 |
Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors. |
Astrazeneca |
26652969 |
15 |
Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety. |
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. |
Bristol-Myers Squibb |
28109945 |
25 |
Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. |
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. |
National University Of Singapore |
28105286 |
65 |
Discovery of a Potent, Selective, and Orally Available PI3Kd Inhibitor for the Treatment of Inflammatory Diseases. |
RhôNe-Poulenc Rorer |
27479483 |
61 |
6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. |
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. |
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. |
Second Military Medical University |
27994757 |
41 |
Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kd. |
TBA |
27994725 |
107 |
Imidazopyridazine Inhibitors of PI3Kß. |
Dart Neuroscience |
27765510 |
8 |
Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity. |
La Trobe University |
28004945 |
52 |
Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase IIIß (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology. |
Academy Of Sciences Of The Czech Republic |
27391133 |
76 |
Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening. |
University Of Berne |
27644332 |
59 |
Class II Phosphoinositide 3-Kinases as Novel Drug Targets. |
Curtin University |
27774127 |
75 |
Discovery of a Series of 5,11-Dihydro-6 |
Dana-Farber Cancer Institute |
27660692 |
70 |
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. |
Infinity Pharmaceuticals |
27186676 |
186 |
Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
West China Hospital Of Sichuan University |
27217002 |
96 |
Discovery of novel 7-azaindoles as PDK1 inhibitors. |
Merck |
27043133 |
16 |
A Prospective Virtual Screening Study: Enriching Hit Rates and Designing Focus Libraries To Find Inhibitors of PI3Kd and PI3K¿. |
Janssen Pharmaceutica |
26885694 |
34 |
Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIß. |
University Of California |
26951753 |
336 |
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
26819669 |
39 |
Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo. |
Novartis Institutes For Biomedical Research |
26896709 |
113 |
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
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. |
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. |
La Trobe University |
26819001 |
29 |
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. |
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. |
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. |
Anhui Agricultural University |
26086931 |
38 |
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators. |
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. |
Amgen |
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. |
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. |
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. |
Xi'An Jiaotong University |
26087940 |
287 |
Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa). |
Astrazeneca |
26037808 |
75 |
Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Ka inhibitors. |
Cairo University |
25980912 |
41 |
Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold. |
Astrazeneca |
25890697 |
6 |
Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions. |
Punjabi University |
26121481 |
37 |
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿. |
Vertex Pharmaceuticals |
26005528 |
41 |
Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT). |
Glaxosmithkline |
25893045 |
44 |
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors. |
Pkucare Pharmaceutical R & D Center |
25643210 |
16 |
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2. |
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 PI3Kß and PI3Kd for the treatment of PTEN-deficient cancers. |
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. |
Vertex Pharmaceuticals |
25693787 |
44 |
6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Ka. |
Nanjing University |
25666823 |
90 |
Synthesis and SAR study of potent and selective PI3Kd inhibitors. |
Amgen |
25415535 |
118 |
Inhibitors of c-Jun N-terminal kinases: an update. |
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. |
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. |
The University Of Jordan |
25042253 |
52 |
Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kß inhibitors, useful as antiplatelet agents. |
Astrazeneca |
24992874 |
58 |
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kß/d inhibitors for the treatment of PTEN-deficient tumours. |
Astrazeneca |
24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
24754609 |
35 |
Structural basis for isoform selectivity in a class of benzothiazole inhibitors of phosphoinositide 3-kinase¿. |
Vertex Pharmaceuticals |
25589920 |
72 |
Quinalozinones as Inhibitors of Class I PI3K Kinases. |
Dart Neuroscience |
25589915 |
41 |
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
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. |
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 PI3Kß inhibitors. |
Sanofi |
23944386 |
55 |
Discovery of selective small molecule type III phosphatidylinositol 4-kinase alpha (PI4KIIIa) inhibitors as anti hepatitis C (HCV) agents. |
Glaxosmithkline |
24387221 |
150 |
Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. |
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. |
Taisho Pharmaceutical |
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. |
Newcastle University |
23820386 |
32 |
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K. |
Novartis Institutes For Biomedical Research |
23726034 |
117 |
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. |
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): aß-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. |
Genentech |
23540645 |
140 |
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinaseß isoform. |
Genentech |
23394126 |
170 |
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). |
Exelixis |
23375793 |
26 |
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014. |
Astrazeneca |
24900568 |
27 |
Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. |
Pfizer |
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. |
The University Of Arizona |
23265896 |
36 |
Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase. |
Monash Institute Of Pharmaceutical Sciences |
23795239 |
62 |
L-Aminoacyl-triazine derivatives are isoform-selective PI3K? inhibitors that target non-conserved Asp862 of PI3K? |
Monash University (Parkville Campus) |
23360348 |
11 |
Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Ka. |
Celgene Avilomics Research |
22520259 |
65 |
Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor. |
Spanish National Cancer Research Centre (Cnio) |
24900504 |
107 |
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors. |
TBA |
22924688 |
128 |
PI3Kd and PI3K¿ as targets for autoimmune and inflammatory diseases. |
Amgen |
23122859 |
43 |
Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase¿ inhibitors. |
Taisho Pharmaceutical |
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. |
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. |
Amgen |
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. |
Cellzome |
23063403 |
21 |
Recent results in protein kinase inhibition for tropical diseases. |
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. |
Amgen |
22877085 |
33 |
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta. |
Genentech |
22876881 |
72 |
Discovery and in vivo evaluation of dual PI3Kß/d inhibitors. |
Amgen |
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. |
Astrazeneca |
22548365 |
293 |
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases. |
Amgen |
23021994 |
108 |
Identification of pyrimidine derivatives as hSMG-1 inhibitors. |
Pfizer |
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. |
Astrazeneca |
22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
22981333 |
103 |
Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kß inhibitors. |
Sanofi |
22863202 |
94 |
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway. |
Novartis Institutes For Biomedical Research |
22819766 |
173 |
SAR studies around a series of triazolopyridines as potent and selective PI3K¿ inhibitors. |
Cellzome |
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. |
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. |
Nanjing University |
22819764 |
35 |
Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR. |
Spanish National Cancer Research Centre (Cnio) |
22738635 |
87 |
Discovery of novel PI3K¿/d inhibitors as potential agents for inflammation. |
Cellzome |
22738630 |
76 |
Structure-based optimization of aminopyridines as PKC¿ inhibitors. |
Vertex Pharmaceuticals |
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. |
Glaxosmithkline |
24900266 |
24 |
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. |
TBA |
20138514 |
93 |
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta. |
Vertex Pharmaceuticals |
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. |
Wyeth Research |
19297156 |
43 |
Exploring the PI3K alpha and gamma binding sites with 2,6-disubstituted isonicotinic derivatives. |
University Of Cincinnati |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University Of Oxford |
18248814 |
24 |
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. |
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. |
Astellas Pharma |
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. |
Glaxosmithkline |
22336246 |
7 |
JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. |
Tianjin Key Laboratory On Technologies Enabling Development Of Clinical Therapeutics And Diagnostics |
22325943 |
71 |
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. |
Spanish National Cancer Research Centre (Cnio) |
21985639 |
70 |
Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform. |
Genentech |
22300886 |
5 |
Synthesis, molecular docking and biological evaluation of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents. |
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. |
Ludwig-Maximilians University Of Munich |
22177407 |
104 |
Novel pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR. |
University Of Auckland |
22177405 |
104 |
Discovery of pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors. |
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. |
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. |
Amgen |
21925880 |
14 |
Fragment based discovery of a novel and selective PI3 kinase inhibitor. |
Pfizer |
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). |
University Of Auckland |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
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. |
Amgen |
21763134 |
57 |
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors. |
Pfizer |
21636270 |
27 |
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase. |
Genentech |
21621413 |
24 |
Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability. |
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. |
Amgen |
21450467 |
261 |
Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk). |
National Human Genome Research Institute |
21341675 |
266 |
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors. |
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. |
Dana-Farber Cancer Institute |
21376583 |
232 |
Discovery of triazine-benzimidazoles as selective inhibitors of mTOR. |
Amgen |
21353551 |
23 |
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2. |
Osi Pharmaceuticals |
21316229 |
12 |
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. |
Chugai Pharmaceutical |
24900252 |
33 |
Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors |
TBA |
21216151 |
66 |
Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements. |
The Institute Of Cancer Research |
21169017 |
63 |
Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening. |
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 Pathway |
TBA |
21121631 |
28 |
Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal. |
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. |
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. |
Dana-Farber Cancer Institute |
20822905 |
28 |
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase. |
Genentech |
20797855 |
63 |
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. |
Pfizer |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
20081827 |
52 |
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. |
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. |
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. |
Wyeth Research |
20346656 |
25 |
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor. |
Genentech |
20303263 |
87 |
Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies. |
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. |
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. |
Genentech |
19762236 |
9 |
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase. |
Kudos Pharmaceuticals |
19968288 |
83 |
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402. |
Wyeth Research |
19969455 |
70 |
Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies. |
Wyeth Research |
19954970 |
64 |
Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors. |
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. |
Wyeth Research |
18774713 |
66 |
Optimization of a series of multi-isoform PI3 kinase inhibitors. |
Ucb Pharma |
18644721 |
131 |
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines. |
Ucb Pharma |
18625552 |
88 |
4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase. |
Ucb Pharma |
16789742 |
65 |
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. |
Serono Pharmaceutical Research Institute |
28209465 |
124 |
Identification of highly potent and selective PI3K? inhibitors. |
Bristol-Myers Squibb |
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. |
University Of Basel |
28404374 |
81 |
Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
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. |
Bristol-Myers Squibb |
28520415 |
91 |
Design and Synthesis of Soluble and Cell-Permeable PI3K? Inhibitors for Long-Acting Inhaled Administration. |
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. |
Astrazeneca |
22214210 |
32 |
Synthesis and binding study of certain 6-arylalkanamides as molecular probes for cannabinoid receptor subtypes. |
Cairo University |
24356970 |
37 |
Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket. |
University Of Texas Southwestern Medical Center |
14573386 |
17 |
Comparison of effects of dual transporter inhibitors on monoamine transporters and extracellular levels in rats. |
Eli Lilly |
1346637 |
120 |
Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells. |
Mayo Clinic |
1328199 |
8 |
Cloning of a novel somatostatin receptor, SSTR3, coupled to adenylylcyclase. |
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. |
Universit&Acute |
19090918 |
33 |
Inhibitors of tubulin assembly identified through screening a compound library. |
The Ohio State University |
19012568 |
7 |
Binding properties of the C-terminal domain of VIAF. |
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. |
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). |
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. |
Abbott Laboratories |
17095227 |
26 |
Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma. |
Pfizer |
14722321 |
9 |
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. |
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. |
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. |
Gsk |
17574423 |
44 |
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors. |
Pfizer |
17132624 |
2 |
Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors. |
Johnson & Johnson Pharmaceutical |
15734645 |
4 |
Structural basis for the highly selective inhibition of MMP-13. |
Aventis Pharma Deutschland |
15217611 |
14 |
Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms. |
Vernalis (R&D) |
17352464 |
51 |
Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors. |
Abbott Laboratories |
17149864 |
69 |
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
University Of Massachusetts Medical School |
16616489 |
29 |
Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors. |
Institut Curie |
22552008 |
7 |
Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. |
Celgene |
8893827 |
17 |
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors. |
Upjohn |