186 articles for thisTarget

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The following articles (labelled with PubMed ID or TBD) are for your review

PMID	Data	Article Title	Organization
28235701	10	Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors.	Peking University
26652969	15	Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.	Xi'An Jiaotong University
28109945	25	Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.	Hangzhou Xixi Hospital
28280261	84	Non-kinase targets of protein kinase inhibitors.	The University Of Sydney
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
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
27994725	107	Imidazopyridazine Inhibitors of PI3Kß.	Dart Neuroscience
27644332	59	Class II Phosphoinositide 3-Kinases as Novel Drug Targets.	Curtin University
27115835	85	Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.	University Of Edinburgh
27353887	9	Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety.	Jiangxi Science & Technology Normal University
27096040	17	Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.	Genentech
27089211	38	Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.	Zhejiang University
27043268	16	Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Ka/mTOR inhibitors.	Jiangxi Science & Technology Normal University
26731167	32	Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.	Sun Yat-Sen University
26819001	29	Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.	Second Military Medical University
26318067	34	Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.	Hanyang 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
26321603	8	Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity.	Xi'An Jiaotong University
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
26162498	1	4-(N-Phenyl-N'-substituted benzenesulfonyl)-6-(4-hydroxyphenyl)quinolines as inhibitors of mammalian target of rapamycin.	India Academy Of Scientific & Innovative Research (Acsir)
25980912	41	Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.	Astrazeneca
26102506	40	Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.	Celgene
26083478	66	Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.	Celgene
25893045	44	Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.	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.	Sichuan University
25659752	16	Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Ka inhibitors.	Jiangxi Science & Technology Normal University
25643210	16	Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.	Astrazeneca
25387153	53	Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.	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.	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.	Shenyang Pharmaceutical University
24893124	4	Development of synthetic lethality anticancer therapeutics.	The University Of Texas M.D. Anderson Cancer Center
25589928	37	Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.	Novartis Institutes For Biomedical Research
25589927	36	Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.	Novartis Institutes For Biomedical Research
25589915	41	Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.	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.	TBA
25466188	21	Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.	Amgen
25440879	13	Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.	Shenyang Pharmaceutical University
24805946	25	Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness.	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.	Development Center For Biotechnology
24433860	60	Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors.	Pkucare Pharmaceutical R & D Center
24393580	6	Virtual screening and biochemical evaluation to identify new inhibitors of mammalian target of rapamycin (mTOR).	Sejong University
24387221	150	Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.	Sanofi
24091081	49	Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.	Merck Research Laboratories
23855836	147	1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.	Newcastle University
23932790	73	A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.	Genentech
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
23506825	71	Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.	Pfizer
23414803	9	Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.	Celgene
23473235	21	Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).	Genentech
23448267	17	Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1.	Glaxosmithkline
23375793	26	Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.	Astrazeneca
24900569	25	Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.	Genentech
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
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.	Astrazeneca
10843203	12	Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.	Glaxo Wellcome
22520259	65	Identification of ETP-46321, a potent and orally bioavailable PI3Ka,d inhibitor.	Spanish National Cancer Research Centre (Cnio)
22832322	40	Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.	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
23199076	28	Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.	Genentech
22946614	9	The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinasea.	Genentech
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
22765895	72	Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.	Amgen
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
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
22765900	24	Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors.	Pfizer
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
22819764	35	Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.	Spanish National Cancer Research Centre (Cnio)
22749419	22	Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Ka and mTOR.	Pfizer
22607682	47	Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor.	Astrazeneca
22475557	75	Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potentß isoform selective phosphatidylinositol 3-kinase inhibitors.	Glaxosmithkline
24900266	24	Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.	TBA
24900269	18	Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.	TBA
21353571	26	Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.	Hanyang University
20166697	71	Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.	Wyeth Research
17350953	3	The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain.	Stanford University
16134928	34	Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.	The Scripps Research Institute
15369399	3	A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma.	Novartis Institutes For Biomedical Research And Novartis Pharma Development
22325943	71	Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.	Spanish National Cancer Research Centre (Cnio)
22136433	67	7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.	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.	Celgene
22197143	17	Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors.	S*Bio
22040023	63	Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).	Pfizer
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
22014755	36	Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.	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.	Amgen
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	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.	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.	Amgen
21763134	57	Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.	Pfizer
20561789	6	Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.	Sanofi-Aventis
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
21495671	95	Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.	Genentech
21438579	4	Isolation and structure of homotemsirolimuses A, B, and C.	Wyeth Research
21332118	157	Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.	Amgen
21413798	174	Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.	Vertex Pharmaceuticals
21388141	22	Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.	Korea Advanced Institute Of Science And Technology
21376583	232	Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.	Amgen
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
21269826	39	Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.	Pfizer
21062009	70	Design, Synthesis, and Structure−Activity Relationships of 3-Ethynyl-1H-indazoles as Inhibitors of the Phosphatidylinositol 3-Kinase Signaling Pathway	TBA
20860370	83	Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.	Dana-Farber Cancer Institute
20822905	28	Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.	Genentech
20817449	19	4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.	Pfizer
20797855	63	PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.	Pfizer
20483602	23	5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.	Wyeth Research
20363128	42	Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.	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
20334367	78	Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.	Wyeth Research
20307980	22	B-Raf kinase inhibitors: hit enrichment through scaffold hopping.	Wyeth Research
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
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).	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).	Wyeth Research
19884006	47	Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.	Wyeth Research
20166671	85	Selectively nonselective kinase inhibition: striking the right balance.	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.	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
20089401	46	Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.	Wyeth Research
19969455	70	Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.	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).	Wyeth Research
19954970	64	Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.	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.	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
19733066	25	Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.	Kudos Pharmaceuticals
19916508	76	Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.	Wyeth Research
19362830	47	Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.	Wyeth Research
19317452	155	Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.	Wyeth Research
18815050	34	4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.	Wyeth Research
18644721	131	Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.	Ucb Pharma
17562705	6	Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.	Stony Brook University
16185865	4	Rapamycin analogs with reduced systemic exposure.	Abbott Laboratories
16143526	1	Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases.	Chinese Academy Of Sciences
15658870	104	Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.	Newcastle University
15546735	25	Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.	University Of Newcastle
10411471	19	Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.	Abbott Laboratories
29308895	24	Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer.	Nankai University
28571824	65	Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3K?/mTOR inhibitors.	Temple University
28829592	109	5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.	University Of Basel
28347666	45	Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours.	Astrazeneca
22957724	30	Synthesis and characterization of metal complexes of heterocyclic sulfonamide as carbonic anhydrase inhibitors.	Dumlupinar University
22188522	45	Sulfapyridine-like benzenesulfonamide derivatives as inhibitors of carbonic anhydrase isoenzymes I, II and VI.	Ataturk University
21635211	12	Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products.	Atatürk University
20030504	38	Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1.	Dublin City University
27595330	6	Small-molecule WNK inhibition regulates cardiovascular and renal function.	Novartis Institutes
12815170	15	[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding.	Abbott Laboratories
11907190	4	4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A): a potent and selective corticotrophin-releasing factor(1) receptor antagonist. I. Biochemical and pharmacological characterization.	Sanofi Synthelabo
11882920	41	Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols.	Institut De Recherches Servier
19012568	7	Binding properties of the C-terminal domain of VIAF.	The Burnham Institute For Medical Research
18849971	56	Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.	University Of California San Francisco
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
17574423	44	Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.	Pfizer
17352464	51	Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.	Abbott Laboratories
8879560	22	Structure-activity relationships of HIV-1 PR inhibitors containing AHPBA--II. Modification of pyrrolidine ring at P1' proline.	Sankyo
8893827	17	Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.	Upjohn