362 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Cmpds
Data
Article Title
Organization
32
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
31
Discovery of a Potent, Selective, and Orally Available PI3Kd Inhibitor for the Treatment of Inflammatory Diseases.
RhôNe-Poulenc Rorer
15
6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.
Csir-Indian Institute of Integrative Medicine
16
Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.
Novartis Institutes For Biomedical Research
33
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
23
Discovery and antiplatelet activity of a selective PI3Kß inhibitor (MIPS-9922).
Monash University
2
Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity.
La Trobe University
35
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
1
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
1
Concise SAR Exploration Based on the"Head-to-Tail" Approach: Discovery of PI4KIIIa Inhibitors Bearing Diverse Scaffolds.
Japan Tobacco
26
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.
Infinity Pharmaceuticals
40
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
20
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
23
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
17
Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.
Novartis Institutes For Biomedical Research
20
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
17
Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.
La Trobe University
13
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.
Second Military Medical University
14
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
11
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.
Shandong University
15
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
3
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
18
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
3
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
44
Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).
AstraZeneca
15
Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Ka inhibitors.
Cairo University
7
Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.
AstraZeneca
45
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
17
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.
Vertex Pharmaceuticals
10
Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Glaxosmithkline
22
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.
Pkucare Pharmaceutical R & D Center
7
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.
AstraZeneca
36
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
17
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
11
6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Ka.
Nanjing University
31
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.
University Hospital Hradec Kralove
25
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
28
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
5
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
1
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
22
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
25
Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Sanofi
3
Inhibitors of PI3Kβ as Potential Treatment for Cancer.
Therachem Research Medilab (India)
99
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
19
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.
Novartis Institutes For Biomedical Research
16
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
Novartis Institutes For Biomedical Research
14
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
41
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinaseß isoform.
Genentech
31
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
19
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.
AstraZeneca
43
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
9
Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase.
Monash Institute of Pharmaceutical Sciences
14
L-Aminoacyl-triazine derivatives are isoform-selective PI3Kβ inhibitors that target non-conserved Asp862 of PI3Kβ
Monash University (Parkville Campus)
1
Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Ka.
Celgene Avilomics Research
25
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.
TBA
25
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
22
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.
Amgen
14
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
14
Recent results in protein kinase inhibition for tropical diseases.
Montclair State University
35
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Amgen
20
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
57
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.
Amgen
25
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
37
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.
Exelixis
23
Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kß inhibitors.
Sanofi
19
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.
Novartis Institutes For Biomedical Research
48
SAR studies around a series of triazolopyridines as potent and selective PI3K¿ inhibitors.
Cellzome
44
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
11
Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.
Spanish National Cancer Research Centre (Cnio)
1
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
7
Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.
Nanjing University
12
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
16
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.
TBA
23
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
118
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
6
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.
Novartis Institute For Biomedical Research
18
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.
Astellas Pharma
36
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
4
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
33
Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.
Genentech
1
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
34
Novel pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.
University of Auckland
34
Discovery of pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors.
University of Auckland
11
Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kß) inhibitors with selectivity over PI3Ka.
Institute of Science and Technology (Kaist)
10
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
39
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
42
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
8
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
17
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
61
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
Amgen
18
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.
Korea Advanced Institute of Science and Technology
5
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.
Chugai Pharmaceutical
18
Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors
TBA
48
Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.
The Institute of Cancer Research
19
Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening.
AstraZeneca
26
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
22
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.
Genentech
18
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.
Pfizer
7
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
13
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.
Medical Research Council-Laboratory of Molecular Biology
10
5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.
Wyeth Research
49
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
12
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Genentech
16
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
1
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.
Kudos Pharmaceuticals
27
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.
Wyeth Research
26
Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.
Wyeth Research
8
Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.
University of Auckland
37
Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.
Wyeth Research
36
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.
Ucb Pharma
21
4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.
Ucb Pharma
25
Discovery and Optimization of Potent PROTAC Degraders of Phosphoinositide 3-Kinase with Significant in Vivo Anticancer Efficacy.
Chinese Academy of Medical Sciences and Peking Union Medical College
11
A Perspective on the Strategic Application of Deconstruction-Reconstruction in Drug Discovery.
AstraZeneca
8
Design, Synthesis, and Biological Evaluation of Thieno[3,2-d]pyrimidine Derivatives as the First Bifunctional PI3Kδ Isoform Selective/Bromodomain and Extra-Terminal Inhibitors.
Chongqing University of Arts and Sciences
1
Lysine-Targeted Covalent Strategy Leading to the Discovery of Novel Potent PROTAC-Based PI3Kδ Degraders.
Xi'an Jiaotong University
38
Lysine-Targeted Covalent Inhibitors of PI3Kδ Synthesis and Screening by In Situ Interaction Upgradation.
Xi'an Jiaotong University
10
Nitrogen-containing heterocyclic drug products approved by the FDA in 2023: Synthesis and biological activity.
University of South China
5
Benzothiazole a privileged scaffold for Cutting-Edges anticancer agents: Exploring drug design, structure-activity relationship, and docking studies.
Acharya & BM Reddy College of Pharmacy
28
Design, synthesis, and pharmacological evaluation of triazine-based PI3K/mTOR inhibitors for the potential treatment of non-small cell lung cancer.
Jiujiang University
12
Thienopyrimidine: A promising scaffold in the development of kinase inhibitors with anticancer activities.
Zhengzhou University
25
Discovery of ART0380, a Potent and Selective ATR Kinase Inhibitor Undergoing Phase 2 Clinical Studies for the Treatment of Advanced or Metastatic Solid Cancers.
The University of Texas MD Anderson Cancer Center
10
Recent contributions of pyridazine as a privileged scaffold of anticancer agents in medicinal chemistry: An updated review.
Zhengzhou University
3
Exploring the antiproliferative and proapoptotic activities of new pyridopyrimidine derivatives and their analogs.
Egyptian-Russian University
8
Inhibition of Human Class I vs Class III Phosphatidylinositol 3'-Kinases.
Georgetown University
1
Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase.
University of Dundee
5
Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor.
AstraZeneca
2
Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.
Genentech, Inc and Exelixis
1
Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.
GlaxoSmithKline
1
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.
Eli Lilly
2
Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.
The Institute of Cancer Research
1
Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor.
Japanese Foundation for Cancer Research
17
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.
GlaxoSmithKline
3
Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer.
Moffitt Cancer Center
4
Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors.
University of California
10
ZSTK474, a novel phosphatidylinositol 3-kinase inhibitor identified using the JFCR39 drug discovery system.
Cancer Chemotherapy Center
3
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Johann Wolfgang Goethe University
21
Discovery of benzamide-based PI3K/HDAC dual inhibitors with marked pro-apoptosis activity in lymphoma cells.
Ocean University of China
14
Synthesis and application of small molecules approved for the treatment of lymphoma.
The First Affiliated Hospital of Zhengzhou University
33
Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor.
Chinese Academy of Sciences
28
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs.
Guizhou Medical University
13
Azaindole derivatives as potential kinase inhibitors and their SARs elucidation.
Hunan University of Science and Technology
14
Discovery of N-(2-chloro-5-(3-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide (FD274) as a highly potent PI3K/mTOR dual inhibitor for the treatment of acute myeloid leukemia.
Fudan University
14
Advances in dual-targeting inhibitors of HDAC6 for cancer treatment.
Guizhou Medical University
39
Discovery of Pyrazolo[1,5-a]pyridine Derivatives as Potent and Selective PI3Kγ/δ Inhibitors.
Chinese Academy of Sciences
10
Small Molecular Inhibitors That Target ATM for Drug Discovery: Current Research and Potential Prospective.
Sichuan University
27
Rational Design of a Novel 6H-Benzo[c]chromen Series as Selective PI3Kα Inhibitors.
Xi'an Jiaotong University
31
Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer.
Guizhou Medical University
47
Discovery of Potent and Selective PI3Kδ Inhibitors for the Treatment of Acute Myeloid Leukemia.
Zhejiang University
40
Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia.
Chinese Academy of Medical Sciences & Peking Union Medical College
15
MNK, mTOR or eIF4E-selecting the best anti-tumor target for blocking translation initiation.
Shandong University
30
Design, Synthesis, and Bioevaluation of Novel Reversibly Photoswitchable PI3K Inhibitors Based on Phenylazopyridine Derivatives toward Light-Controlled Cancer Treatment.
Chinese Academy of Medical Sciences and Peking Union Medical College
41
Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.
Sichuan University
17
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.
University of Auckland
57
Targeting autophagy drug discovery: Targets, indications and development trends.
China Jiliang University
30
Discovery of Novel Azaindoles as Potent and Selective PI3Kδ Inhibitors for Treatment of Multiple Sclerosis.
Zhejiang University
95
Identification of 6-Anilino Imidazo[4,5-c]pyridin-2-ones as Selective DNA-Dependent Protein Kinase Inhibitors and Their Application as Radiosensitizers.
University of Auckland
14
Designing Small Molecule PI3Kγ Inhibitors: A Review of Structure-Based Methods and Computational Approaches.
Hebei University of Science & Technology
2
Discovery and Optimization of Pyridazinones as PI3Kδ Selective Inhibitors for Administration by Inhalation.
Chiesi Farmaceutici S.p.A
1
Facile Synthesis and First Antifungal Exploration of Tetracyclic Meroterpenoids: (+)-Aureol, (-)-Pelorol, and Its Analogs.
Guizhou University
26
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
Mirati Therapeutics
4
Design, synthesis and biological evaluation of novel morpholinopyrimidine-5-carbonitrile derivatives as dual PI3K/mTOR inhibitors.
Health Affairs Directorate - Giza
34
Design and Synthesis of 1,3,5-Triazines or Pyrimidines Containing Dithiocarbamate Moiety as PI3Kα Selective Inhibitors.
Shenyang Pharmaceutical University
2
Discovery of a photosensitizing PI3K inhibitor for tumor therapy: Design, synthesis and in vitro biological evaluation.
Fudan University
30
Function-oriented synthesis of Imidazo[1,2-a]pyrazine and Imidazo[1,2-b]pyridazine derivatives as potent PI3K/mTOR dual inhibitors.
East China Normal University
36
Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents.
University of Calabria
17
Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.
Novartis Institutes for Biomedical Research
34
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
China Pharmaceutical University
22
Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor.
University of Basel
48
Discovery of 4-oxo-4,5-dihydropyrazolo[1,5-a]quinoxaline-7-carboxamide derivatives as PI3Kα inhibitors via virtual screening and docking-based structure optimization.
Zhejiang University
1
Design, synthesis and bioactivity evaluation of a series of quinazolinone derivatives as potent PI3Kγ antagonist.
Southern Medical University
3
Developing a Naïve Bayesian Classification Model with PI3Kγ structural features for virtual screening against PI3Kγ: Combining molecular docking and pharmacophore based on multiple PI3Kγ conformations.
Jiangnan University
25
Design, synthesis and in vitro biological evaluation of 2-aminopyridine derivatives as novel PI3Kδ inhibitors for hematological cancer.
Fudan University
34
4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.
Yangtze University
31
Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.
Universite de Tours
37
Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.
Al-Azhar University
30
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.
Sichuan University
29
Targeting the PI3K/AKT/mTOR Signaling Pathway in the Treatment of Human Diseases: Current Status, Trends, and Solutions.
South China University of Technology
33
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.
Serono Pharmaceutical Research Institute
103
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).
University of Hradec Kralove
68
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Menoufia University
30
Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies.
Peking Union Medical College
27
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.
Zhejiang University
53
Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase γ (PI3Kγ).
Arcus Biosciences
36
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
Genentech
19
Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases.
National Clinical Research Center For Geriatrics
40
Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer.
China Pharmaceutical University
33
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.
Hefei University of Technology
33
Identification and optimization of a novel series of selective PIP5K inhibitors.
AstraZeneca
37
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Novartis Institutes For Biomedical Research
50
Kinase Inhibitors as Underexplored Antiviral Agents.
Complutense University of Madrid
91
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
Csir-Indian Institute of Integrative Medicine
20
Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review.
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)
8
Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies.
West China Hospital
15
Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy.
Zhuhai Campus of Zunyi Medical University
21
Synthesis and biological evaluation of 4H-benzo[e][1,3]oxazin-4-ones analogues of TGX-221 as inhibitors of PI3Kβ.
La Trobe University
4
From lab to clinic: The discovery and optimization journey of PI3K inhibitors.
China Medical University
1
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
Peking Union Medical College
34
Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions.
National Institute of Pharmaceutical Education and Research (NIPER)
4
Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Fluorinated Candidates as PI3K Inhibitors: Targeting Fluorophilic Binding Sites.
Huazhong Agricultural University
29
Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer.
Guizhou Medical University
19
Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors.
The University of Michigan Medical School
2
Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment.
TBA
22
Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation.
Fudan University
30
BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.
Bayer
16
Synthesis and biological evaluation of novel purinyl quinazolinone derivatives as PI3Kδ-specific inhibitors for the treatment of hematologic malignancies.
Sungkyunkwan University
28
Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ.
Novartis Institutes For Biomedical Research
27
Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity.
Fudan University
9
Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.
Southern Medical University
18
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.
China Pharmaceutical University
30
Synthetic Lethality through the Lens of Medicinal Chemistry.
Istituto Italiano Di Tecnologia
15
Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors.
Guizhou Medical University
19
Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability.
Gilead Sciences
8
Structural optimization towards promising β-methyl-4-acrylamido quinoline derivatives as PI3K/mTOR dual inhibitors for anti-cancer therapy: The in vitro and in vivo biological evaluation.
Jiaxing University
4
Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer.
China Pharmaceutical University
44
Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors.
Southwest Jiaotong University
14
Discovery of 2-(5-(quinolin-6-yl)-1,3,4-oxadiazol-2-yl)acetamide derivatives as novel PI3Kα inhibitors via docking-based virtual screening.
Zhejiang University
25
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).
Pfizer
8
Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity.
China Pharmaceutical University
42
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
A*Star
20
Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.
Maternal and Child Health Hospital of Hubei Province
2
Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.
Chinese Academy of Sciences
23
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors.
Peking Union Medical College
9
Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-
University of Edinburgh
3
Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors.
Shenyang Pharmaceutical University
24
Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase δ.
Gsk Medicines Research Centre
2
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.
Central South University
20
Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
Gilead Sciences
50
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
4
Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors.
Xi'An Jiaotong University
11
Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
Glaxosmithkline R&D
46
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
AstraZeneca
20
Development of single and mixed isoform selectivity PI3Kδ inhibitors by targeting Asn836 of PI3Kδ.
Monash University
16
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
Novartis Institutes For Biomedical Research
14
Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ.
China Pharmaceutical University
72
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of
University of Nottingham
19
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).
Incyte
39
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
National Center For Advancing Translational Sciences
17
Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3Kδ inhibitors.
Xi'An Jiaotong University
9
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.
University Park Nottingham
13
Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.
Zydus Research Centre
30
Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies.
Zhejiang University
16
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach.
Glaxosmithkline R&D
14
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.
Novartis Institutes For Biomedical Research
20
Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.
TBA
8
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.
Ain Shams University
3
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.
Chengdu University
21
Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3Kδ inhibitor.
Astellas Pharma
14
Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα.
School of Traditional Chinese Pharmacy
9
The Exploration of Chirality for Improved Druggability within the Human Kinome.
University of Arkansas For Medical Sciences
16
Design, synthesis and biological evaluation of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates containing sulfonamido as potential PI3Kα inhibitors.
School of Traditional Chinese Pharmacy
28
Targeting the immunity protein kinases for immuno-oncology.
China Pharmaceutical University
39
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
Glaxosmithkline
29
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor.
University of Basel
38
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
TBA
28
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.
China Pharmaceutical University
31
Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
Gilead Sciences
17
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
AstraZeneca
16
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
18
Synthetic approaches and application of representative clinically approved fluorine-enriched anti-cancer medications.
Shengjing Hospital of China Medical University
19
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.
Zhejiang University
29
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Novartis Institutes For Biomedical Research
28
[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors.
Glaxosmithkline
20
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.
Xi'An Jiaotong University
38
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
40
Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.
Chongqing University
2
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
34
Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors.
Chongqing University
12
Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ.
China Pharmaceutical University
2
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 PI3Kα inhibitors.
Shenyang Pharmaceutical University
13
Discovery of novel quinazolinone derivatives as high potent and selective PI3Kδ and PI3Kδ/γ inhibitors.
Shandong University
32
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
AstraZeneca
17
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.
Xi'An Jiaotong University
4
Design and synthesis of 1,4-substituted 1H-1,2,3-triazolo-quinazolin-4(3H)-ones by Huisgen 1,3-dipolar cycloaddition with PI3Kγ isoform selective activity.
India Academy of Scientific & Innovative Research (Acsir)
20
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.
Peking Union Medical College
18
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
AstraZeneca
4
Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα.
Shenyang Pharmaceutical University
21
Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.
Fudan University
4
Design, synthesis, and biological evaluation of novel 3-substituted imidazo[1,2-a]pyridine and quinazolin-4(3H)-one derivatives as PI3Kα inhibitors.
Shenyang Pharmaceutical University
39
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 (PI3Kδ) inhibitor.
Chinese Academy of Sciences
41
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
42
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.
Peking Union Medical College
12
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Novartis Institutes For Biomedical Research
18
Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors.
Pharmaron-Beijing
9
Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168).
University of Michigan
11
Potential of PI3Kβ Inhibitors in the Treatment of Cancer and Other Diseases.
Therachem Research Medilab (India)
35
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 Kinaseδ (PI3Kδ) Inhibitors.
University Park Nottingham
37
Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.
West China Hospital of Sichuan University
7
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.
The Ohio State University
36
SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.
Shanghai Institute of Materia Medica (Simm)
35
Identification of highly potent and selective PI3Kδ inhibitors.
Bristol Myers Squibb
19
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
39
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinaseδ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Bristol Myers Squibb
11
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
AstraZeneca
467
HETEROCYCLIC INHIBITORS OF IGF-1R FOR TREATMENT OF DISEASE
Horizon Therapeutics Ireland Dac
1
Diarylpyrazole compound, composition comprising same, and use thereof
Shenzhen Targetrx
21
Aryl-phosphorus-oxygen compound as EGFR kinase inhibitor
Chia Tai Tianqing Pharmaceutical Group
35
Fused piperidinyl bicyclic and related compounds as modulators of C5A receptor
Inflarx
35
Biaryltriazole inhibitors of macrophage migration inhibitory factor
Yale University
7
Crystalline monomesylate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
Kronos Bio
152
Nitrogen-containing heteroaryl compound and pharmaceutical use thereof
Japan Tobacco
118
2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides
Pfizer
16
Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.
King Fahd University of Petroleum & Minerals
7
Pharmaceutical uses of 6-amino quinazoline or 3-cyano quinoline derivatives
Jiangsu Hengrui Medicine
16
Facile dimethyl amino group triggered cyclic sulfonamides synthesis and evaluation as alkaline phosphatase inhibitors.
University of Karachi
102
Treatment of respiratory disorders using TRPA1 antagonists
Glenmark Pharmaceuticals
4
ß-Hydroxyacyl-acyl Carrier Protein Dehydratase (FabZ) from Francisella tularensis and Yersinia pestis: Structure Determination, Enzymatic Characterization, and Cross-Inhibition Studies.
Brookhaven National Laboratory
6
Dihydropyrano [2,3-c] pyrazole: Novel in vitro inhibitors of yeast a-glucosidase.
King Abdulaziz University
9
Targeting Tumour Proliferation with a Small-Molecule Inhibitor of AICAR Transformylase Homodimerization.
University of Southampton
8
Inhibition of bacterial virulence: drug-like molecules targeting the Salmonella enterica PhoP response regulator.
Washington University
10
Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.
University of Kansas
7
Affinities of fluoxetine, its enantiomers, and other inhibitors of serotonin uptake for subtypes of serotonin receptors.
Eli Lilly
80
COMPOUND FOR REGULATING AND CONTROLLING ACTIVITY OF 15-PGDH AND PREPARATION METHOD THEREFOR
Scinnohub Pharmaceutical
19
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.
Bristol Myers Squibb