302 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
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
28280261	84	Non-kinase targets of protein kinase inhibitors.	The University of Sydney
27923617	70	Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110a-selective PI3 kinase inhibitors.	University of Auckland
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
27387421	34	Discovery and antiplatelet activity of a selective PI3Kß inhibitor (MIPS-9922).	Monash University
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
27644332	59	Class II Phosphoinositide 3-Kinases as Novel Drug Targets.	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.	Novartis Institutes For Biomedical Research
27774129	2	Concise SAR Exploration Based on the"Head-to-Tail" Approach: Discovery of PI4KIIIa Inhibitors Bearing Diverse Scaffolds.	Japan Tobacco
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
27189888	11	Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents.	Chugai Pharmaceutical
26951750	59	Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.	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.	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
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
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
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
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.	University of Auckland
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
25387153	53	Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.	University Hospital Hradec Kralove
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
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
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
24387221	150	Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.	Sanofi
24900751	6	Inhibitors of PI3K? as Potential Treatment for Cancer.	Therachem Research Medilab (India)
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
23644197	51	Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).	University of Auckland
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
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
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
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
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
22765895	72	Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR 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
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
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
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.	Ambit Biosciences
22520630	21	Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.	Nanjing University
22475557	75	Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potentß isoform selective phosphatidylinositol 3-kinase inhibitors.	Glaxosmithkline
24900266	24	Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.	TBA
20166697	71	Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.	Wyeth Research
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
21985639	70	Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.	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.	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
22030027	12	Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kß) inhibitors with selectivity over PI3Ka.	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.	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
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
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
21636270	27	Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.	Genentech
21332118	157	Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.	Amgen
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
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
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
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
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
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
19748269	21	Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.	University of Auckland
19916508	76	Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.	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
17869522	51	Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.	University of Auckland
16789742	65	Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.	Serono Pharmaceutical Research Institute
32676155	54	Discovery of 3-Quinazolin-4(3	Luoxin Pharmaceutical (Shanghai) Co.
32676144	34	Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase ?.	Gsk Medicines Research Centre
32317209	8	Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.	Central South University
32551006	134	Discovery of an Atropisomeric PI3K? Selective Inhibitor through Optimization of the Hinge Binding Motif.	Gilead Sciences
32502336	79	Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.	Bayer
30850264	108	Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.	University of Auckland
27544401	10	Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors.	Xi'An Jiaotong University
27429068	54	Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.	Glaxosmithkline R&D
27259031	191	Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.	Astrazeneca
27561716	95	Development of single and mixed isoform selectivity PI3K? inhibitors by targeting Asn836 of PI3K?.	Monash University
27563400	133	Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.	Novartis Institutes For Biomedical Research
30605829	24	Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3K?.	China Pharmaceutical University
31647659	576	Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of	University of Nottingham
31749910	26	INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3K?).	Incyte
32212730	206	Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.	National Center For Advancing Translational Sciences
31851518	61	The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-	Astrazeneca
31434616	32	Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3K? inhibitors.	Xi'An Jiaotong University
30582807	22	Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.	University Park Nottingham
30975623	34	Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3K? selective inhibitors.	Zydus Research Centre
30878826	45	Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3K?-selective inhibitors for treating B-cell-mediated malignancies.	Zhejiang University
30532965	81	Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.	Glaxosmithkline R&D
31955578	37	Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.	Novartis Institutes For Biomedical Research
31846325	46	Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.	TBA
31693351	473	Discovery of 4	TBA
31581005	29	Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.	Ain Shams University
31381325	46	Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.	Chengdu University
30755348	45	Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3K? inhibitor.	Astellas Pharma
31228810	162	Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.	West China Hospital of Sichuan University
31446244	70	Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3K?.	School of Traditional Chinese Pharmacy
32069401	27	Design, Synthesis, and Biological Evaluation of Imidazo[1,2-	East China Normal University
31550151	17	The Exploration of Chirality for Improved Druggability within the Human Kinome.	University of Arkansas For Medical Sciences
31033293	77	Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3K?-PI3K? Dual Inhibitors.	Hutchison Medipharma
31029551	64	Design, synthesis and biological evaluation of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates containing sulfonamido as potential PI3K? inhibitors.	School of Traditional Chinese Pharmacy
30418766	35	Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.	Qingdao University
30530193	64	Targeting the immunity protein kinases for immuno-oncology.	China Pharmaceutical University
30015489	16	Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) ? Inhibitor.	Gilead Sciences
31855425	224	Optimization of Orally Bioavailable PI3K? Inhibitors and Identification of Vps34 as a Key Selectivity Target.	Glaxosmithkline
31465220	139	A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor.	University of Basel
31335136	29	Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis.	TBA
31117517	103	Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.	TBA
29211480	64	Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.	China Pharmaceutical University
28106991	136	Discovery of a Phosphoinositide 3-Kinase (PI3K) ?/? Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3K? Potency in a PI3K?-Selective Template by Targeting Nonconserved Asp856.	Gilead Sciences
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.	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.	Novartis Institutes For Biomedical Research
26596710	27	Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.	Zhejiang University
26206504	131	Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.	Novartis Institutes For Biomedical Research
24900655	165	[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase ? Inhibitors.	Glaxosmithkline
31176568	34	Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.	Xi'An Jiaotong University
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.	University of Basel
30071408	56	Difuran-substituted quinoxalines as a novel class of PI3K? H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.	Chongqing University
30380865	19	Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.	University of California San Diego
30245395	50	Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3K? H1047R mutant inhibitors.	Chongqing University
30237123	12	Piperidinyl-embeded chalcones possessing anti PI3K? inhibitory properties exhibit anti-atopic properties in preclinical models.	Inserm 1052/Cnrs 5286/University of Lyon
29541370	41	Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.	Wuxi Apptec (Shanghai) Co.
30077608	24	Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3K?.	China Pharmaceutical University
29937355	8	Design, synthesis and biological evaluation of novel series of 2H-benzo[b][1,4]oxazin-3(4H)-one and 2H-benzo[b][1,4]oxazine scaffold derivatives as PI3K? inhibitors.	Shenyang Pharmaceutical University
29601991	22	Discovery of novel quinazolinone derivatives as high potent and selective PI3K? and PI3K?/? inhibitors.	Shandong University
29631787	21	Discovery and biological evaluation of novel pyrazolopyridine derivatives as potent and orally available PI3K? inhibitors.	Astellas Pharma
29559278	99	Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.	Astrazeneca
29534936	30	Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3K?) inhibitors.	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.	India Academy of Scientific & Innovative Research (Acsir)
29475582	8	Novel 4-aminoquinazoline derivatives induce growth inhibition, cell cycle arrest and apoptosis via PI3K? inhibition.	Shenyang Pharmaceutical University
29305298	28	Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.	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.	Astrazeneca
30034607	60	Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.	Shanghai Haiyan Pharmaceutical Technology
29407971	15	Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3K?.	Shenyang Pharmaceutical University
28835805	45	Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.	Fudan University
28800461	16	Design, synthesis, and biological evaluation of novel 3-substituted imidazo[1,2-a]pyridine and quinazolin-4(3H)-one derivatives as PI3K? inhibitors.	Shenyang Pharmaceutical University
29017786	35	Identification of novel PI3K inhibitors through a scaffold hopping strategy.	Spanish National Cancer Research Centre (Cnio)
28958845	147	Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.	University of Auckland
30351000	119	Discovery of a Novel Inhaled PI3K? Inhibitor for the Treatment of Respiratory Diseases.	TBA
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.	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).	Astrazeneca
29927604	90	Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.	Chinese Academy of Medical Sciences and Peking Union Medical College
28494256	11	Designing multi-targeted agents: An emerging anticancer drug discovery paradigm.	Hunan University of Chinese Medicine
29057057	54	From PIM1 to PI3K? via GSK3?: Target Hopping through the Kinome.	Glaxosmithkline
28947947	112	Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.	Novartis Institutes For Biomedical Research
29852070	101	Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors.	Pharmaron-Beijing
28835793	32	Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168).	University of Michigan
28835784	77	Potential of PI3K? Inhibitors in the Treatment of Cancer and Other Diseases.	Therachem Research Medilab (India)
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.	University Park Nottingham
28409639	83	Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.	West China Hospital of Sichuan University
28259529	31	Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.	The Ohio State University
27846451	60	SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3K?) inhibitors.	Shanghai Institute of Materia Medica (Simm)
28526367	30	Discovery of a novel aminopyrazine series as selective PI3K? inhibitors.	Astrazeneca
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
23663081	49	Design, synthesis and biological evaluation of novel inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors.	Nycomed
20222761	21	Semisynthesis of alpha-methyl-gamma-lactones and in vitro evaluation of their activity on protein farnesyltransferase.	Ufr Des Sciences Pharmaceutiques Et Ingenierie De La Sante
12232544	79	[Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine].	Emory University
9015795	50	Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.	University of Toronto
6271132	14	Prostacyclin receptors of a neuronal hybrid cell line. Divalent citations and ligand-receptor coupling.	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.	Universit&Acute
19090918	33	Inhibitors of tubulin assembly identified through screening a compound library.	The Ohio State University
16873019	6	MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.	Gpc Biotech
18849971	56	Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.	University of California San Francisco
17685602	33	Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.	Targegen
17172449	20	Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.	Targegen
18754654	19	The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .	Piramed Pharma
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
17574423	44	Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.	Pfizer
15734645	4	Structural basis for the highly selective inhibition of MMP-13.	Aventis Pharma Deutschland
12014965	38	Homodimeric tacrine congeners as acetylcholinesterase inhibitors.	National Defense Medical Center