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414 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors.EBI
Astrazeneca
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kd inhibitors.EBI
Bristol-Myers Squibb
Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.EBI
Hangzhou Xixi Hospital
Non-kinase targets of protein kinase inhibitors.EBI
The University of Sydney
Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110a-selective PI3 kinase inhibitors.EBI
University of Auckland
Discovery of a Potent, Selective, and Orally Available PI3Kd Inhibitor for the Treatment of Inflammatory Diseases.EBI
RhôNe-Poulenc Rorer
6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.EBI
Csir-Indian Institute of Integrative Medicine
Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.EBI
Novartis Institutes For Biomedical Research
Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.EBI
Second Military Medical University
Discovery and antiplatelet activity of a selective PI3Kß inhibitor (MIPS-9922).EBI
Monash University
Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kd.EBI
TBA
Imidazopyridazine Inhibitors of PI3Kß.EBI
Dart Neuroscience
Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity.EBI
La Trobe University
Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase IIIß (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology.EBI
Academy of Sciences of The Czech Republic
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.EBI
Curtin University
Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.EBI
Novartis Institutes For Biomedical Research
Discovery of a Series of 5,11-Dihydro-6EBI
Dana-Farber Cancer Institute
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.EBI
Infinity Pharmaceuticals
Discovery of novel 7-azaindoles as PDK1 inhibitors.EBI
Merck
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kd Selective Inhibitors.EBI
Gilead Sciences
Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIß.EBI
University of California
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI
Novartis Institutes For Biomedical Research
Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.EBI
Novartis Institutes For Biomedical Research
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.EBI
Saarland University
Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.EBI
Sun Yat-Sen University
Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.EBI
La Trobe University
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.EBI
Second Military Medical University
Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.EBI
Novartis Institutes For Biomedical Research
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.EBI
Shandong University
The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.EBI
Amgen
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Ka inhibitor with high PI3K isoform selectivity and potent cellular activity.EBI
Novartis Institutes For Biomedical Research
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.EBI
Novartis Institutes For Biomedical Research
Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea.EBI
Xi'An Jiaotong University
Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).EBI
Astrazeneca
Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Ka inhibitors.EBI
Cairo University
Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.EBI
Astrazeneca
Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.EBI
University of Auckland
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.EBI
Vertex Pharmaceuticals
Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).EBI
Glaxosmithkline
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.EBI
Pkucare Pharmaceutical R & D Center
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.EBI
Astrazeneca
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.EBI
Astrazeneca
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.EBI
Vertex Pharmaceuticals
6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Ka.EBI
Nanjing University
Synthesis and SAR study of potent and selective PI3Kd inhibitors.EBI
Amgen
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.EBI
University Hospital Hradec Kralove
Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kß inhibitors, useful as antiplatelet agents.EBI
Astrazeneca
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.EBI
Astrazeneca
Quinalozinones as Inhibitors of Class I PI3K Kinases.EBI
Dart Neuroscience
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.EBI
Monash University (Parkville Campus)
Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness.EBI
Northeastern University
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.EBI
Sanofi
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).EBI
Icahn School of Medicine At Mount Sinai
Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.EBI
Sanofi
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.EBI
Newcastle University
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.EBI
Novartis Institutes For Biomedical Research
A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.EBI
Genentech
Identification of GNE-293, a potent and selective PI3Kd inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.EBI
Genentech
Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus.EBI
Boehringer Ingelheim (Canada)
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.EBI
Novartis Institutes For Biomedical Research
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.EBI
Genentech
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinaseß isoform.EBI
Genentech
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.EBI
Astrazeneca
Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.EBI
Pfizer
Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.EBI
The University of Arizona
Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase.EBI
Monash Institute of Pharmaceutical Sciences
L-Aminoacyl-triazine derivatives are isoform-selective PI3Kβ inhibitors that target non-conserved Asp862 of PI3KβEBI
Monash University (Parkville Campus)
Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Ka.EBI
Celgene Avilomics Research
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.EBI
TBA
PI3Kd and PI3K¿ as targets for autoimmune and inflammatory diseases.EBI
Amgen
Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines.EBI
La Trobe University
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.EBI
Amgen
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.EBI
Cellzome
Recent results in protein kinase inhibition for tropical diseases.EBI
Montclair State University
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.EBI
Genentech
Discovery and in vivo evaluation of dual PI3Kß/d inhibitors.EBI
Amgen
Discovery of phosphoinositide 3-kinases (PI3K) p110ß isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance.EBI
Astrazeneca
Discovery of novel PI3-kinased specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.EBI
Genentech
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.EBI
Amgen
Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110ß isoform inhibitors through structure-based fragment optimisation.EBI
Astrazeneca
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI
Exelixis
Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kß inhibitors.EBI
Sanofi
Potent and selective inhibitors of PI3Kd: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.EBI
Genentech
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.EBI
Novartis Institutes For Biomedical Research
SAR studies around a series of triazolopyridines as potent and selective PI3K¿ inhibitors.EBI
Cellzome
Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kß inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.EBI
Sanofi Research & Development
Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.EBI
Spanish National Cancer Research Centre (Cnio)
Discovery of novel PI3K¿/d inhibitors as potential agents for inflammation.EBI
Cellzome
Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.EBI
Nanjing University
Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potentß isoform selective phosphatidylinositol 3-kinase inhibitors.EBI
Glaxosmithkline
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.EBI
TBA
Features of selective kinase inhibitors.EBI
University of California San Francisco
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.EBI
Wyeth Research
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.EBI
Novartis Institute For Biomedical Research
Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.EBI
Glaxosmithkline
JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs.EBI
Tianjin Key Laboratory On Technologies Enabling Development of Clinical Therapeutics and Diagnostics
Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.EBI
Genentech
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.EBI
Ludwig-Maximilians University of Munich
Novel pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.EBI
University of Auckland
Discovery of pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors.EBI
University of Auckland
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.EBI
Genentech
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.EBI
Amgen
Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).EBI
University of Auckland
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.EBI
Novartis Institute For Biomedical Research
Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.EBI
Amgen
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.EBI
Genentech
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.EBI
Amgen
Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.EBI
Amgen
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.EBI
Chugai Pharmaceutical
Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase InhibitorsEBI
TBA
Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening.EBI
Astrazeneca R & D M£Lndal
Design, Synthesis, and Structure−Activity Relationships of 3-Ethynyl-1H-indazoles as Inhibitors of the Phosphatidylinositol 3-Kinase Signaling PathwayEBI
TBA
Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.EBI
Novartis Institutes For Biomedical Research
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.EBI
Genentech
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.EBI
Pfizer
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.EBI
Medical Research Council-Laboratory of Molecular Biology
5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.EBI
Wyeth Research
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.EBI
Wyeth Research
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.EBI
Genentech
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.EBI
Genentech
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.EBI
Kudos Pharmaceuticals
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.EBI
Wyeth Research
Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.EBI
Wyeth Research
Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.EBI
University of Auckland
Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.EBI
Wyeth Research
Optimization of a series of multi-isoform PI3 kinase inhibitors.EBI
Ucb Pharma
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.EBI
Ucb Pharma
4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.EBI
Ucb Pharma
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.EBI
University of Auckland
Design, synthesis and biological evaluation of novel morpholinopyrimidine-5-carbonitrile derivatives as dual PI3K/mTOR inhibitors.EBI
Health Affairs Directorate - Giza
Targeting VPS34 in autophagy: An update on pharmacological small-molecule compounds.EBI
Southwest Jiaotong University
Design and Synthesis of 1,3,5-Triazines or Pyrimidines Containing Dithiocarbamate Moiety as PI3Kα Selective Inhibitors.EBI
Shenyang Pharmaceutical University
Discovery of (S)-NEBI
Zhejiang Chinese Medical University
Discovery of a photosensitizing PI3K inhibitor for tumor therapy: Design, synthesis and in vitro biological evaluation.EBI
Fudan University
Discovery of Highly Selective and Orally Bioavailable PI3Kδ Inhibitors with Anti-Inflammatory Activity for Treatment of Acute Lung Injury.EBI
Zhejiang University
Function-oriented synthesis of Imidazo[1,2-a]pyrazine and Imidazo[1,2-b]pyridazine derivatives as potent PI3K/mTOR dual inhibitors.EBI
East China Normal University
Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents.EBI
University of Calabria
The Role of Allylic Strain for Conformational Control in Medicinal Chemistry.EBI
Astrazeneca
Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.EBI
Novartis Institutes for Biomedical Research
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.EBI
China Pharmaceutical University
Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor.EBI
University of Basel
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.EBI
Zhejiang University
Design, synthesis and bioactivity evaluation of a series of quinazolinone derivatives as potent PI3Kγ antagonist.EBI
Southern Medical University
Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective.EBI
University of Modena and Reggio Emilia
Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors.EBI
Guru Nanak Dev University
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.EBI
Jiangnan University
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.EBI
Astrazeneca
Design, synthesis and in vitro biological evaluation of 2-aminopyridine derivatives as novel PI3Kδ inhibitors for hematological cancer.EBI
Fudan University
4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.EBI
Yangtze University
Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.EBI
Universite de Tours
4-(3H)-quinazolinones N-3 substituted with a five membered heterocycle: A promising scaffold towards bioactive molecules.EBI
Universita Degli Studi di Palermo
Research progress of mTOR inhibitors.EBI
Jilin University
Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.EBI
Al-Azhar University
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.EBI
Sichuan University
Targeting the PI3K/AKT/mTOR Signaling Pathway in the Treatment of Human Diseases: Current Status, Trends, and Solutions.EBI
South China University of Technology
Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.EBI
Anhui University of Chinese Medicine
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.EBI
Serono Pharmaceutical Research Institute
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).EBI
University of Hradec Kralove
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.EBI
Menoufia University
Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies.EBI
Peking Union Medical College
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.EBI
Zhejiang University
Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase γ (PI3Kγ).EBI
Arcus Biosciences
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.EBI
Genentech
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.EBI
Tianjin University
Discovery, Optimization, and Evaluation of Quinazolinone Derivatives with Novel Linkers as Orally Efficacious Phosphoinositide-3-Kinase Delta Inhibitors for Treatment of Inflammatory Diseases.EBI
National Clinical Research Center For Geriatrics
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.EBI
Zhengzhou University
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.EBI
Hefei University of Technology
Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer.EBI
China Pharmaceutical University
Identification and optimization of a novel series of selective PIP5K inhibitors.EBI
Astrazeneca
Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8EBI
Astrazeneca
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.EBI
Novartis Institutes For Biomedical Research
Kinase Inhibitors as Underexplored Antiviral Agents.EBI
Complutense University of Madrid
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.EBI
Csir-Indian Institute of Integrative Medicine
Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review.EBI
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)
Discovery, Optimization, and Evaluation of Potent and Selective PI3Kδ-γ Dual Inhibitors for the Treatment of B-cell Malignancies.EBI
West China Hospital
Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy.EBI
Zhuhai Campus of Zunyi Medical University
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.EBI
Peking Union Medical College
Discovery of 2-Methyl-2-(4-(2-methyl-8-(1EBI
West China Hospital of Sichuan University
Phenotypic Discovery of Triazolo[1,5-EBI
Technical University Dortmund
Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Fluorinated Candidates as PI3K Inhibitors: Targeting Fluorophilic Binding Sites.EBI
Huazhong Agricultural University
Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer.EBI
Guizhou Medical University
Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors.EBI
The University of Michigan Medical School
Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment.EBI
TBA
Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma.EBI
Astrazeneca
Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation.EBI
Fudan University
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.EBI
Merck
Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ.EBI
Novartis Institutes For Biomedical Research
Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.EBI
Glaxosmithkline R&D
Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity.EBI
Fudan University
Discovery of a new series of PI3K-δ inhibitors from Virtual Screening.EBI
Merck
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.EBI
Guangzhou Institutes of Biomedicine and Health
Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.EBI
Southern Medical University
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.EBI
China Pharmaceutical University
Synthetic Lethality through the Lens of Medicinal Chemistry.EBI
Istituto Italiano Di Tecnologia
Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors.EBI
Guizhou Medical University
Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability.EBI
Gilead Sciences
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.EBI
Jiaxing University
Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer.EBI
China Pharmaceutical University
Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors.EBI
Southwest Jiaotong University
Discovery of a Potent and Selective PI3Kδ Inhibitor (EBI
Lupin
Discovery of 2-(5-(quinolin-6-yl)-1,3,4-oxadiazol-2-yl)acetamide derivatives as novel PI3Kα inhibitors via docking-based virtual screening.EBI
Zhejiang University
4-(Difluoromethyl)-5-(4-((3EBI
University of Basel
Research advances on selective phosphatidylinositol 3 kinase δ (PI3Kδ) inhibitors.EBI
Xi'An Jiaotong University
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.EBI
Amgen
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).EBI
Pfizer
Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity.EBI
China Pharmaceutical University
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.EBI
A*Star
Discovery of (EBI
Hefei Institutes of Physical Science
Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.EBI
Maternal and Child Health Hospital of Hubei Province
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.EBI
Chinese Academy of Sciences
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors.EBI
Peking Union Medical College
Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-EBI
University of Edinburgh
Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors.EBI
Merck
Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors.EBI
Shenyang Pharmaceutical University
Discovery of 3-Quinazolin-4(3EBI
Luoxin Pharmaceutical (Shanghai) Co.
Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase δ.EBI
Gsk Medicines Research Centre
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.EBI
Central South University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.EBI
Merck
Synthesis and antitumor activity evaluation of 4,6-disubstituted quinazoline derivatives as novel PI3K inhibitors.EBI
Xi'An Jiaotong University
Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.EBI
Glaxosmithkline R&D
Development of single and mixed isoform selectivity PI3Kδ inhibitors by targeting Asn836 of PI3Kδ.EBI
Monash University
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.EBI
Novartis Institutes For Biomedical Research
Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors.EBI
Bristol-Myers Squibb
Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ.EBI
China Pharmaceutical University
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of EBI
University of Nottingham
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).EBI
Incyte
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.EBI
National Center For Advancing Translational Sciences
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-EBI
Astrazeneca
Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3Kδ inhibitors.EBI
Xi'An Jiaotong University
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.EBI
University Park Nottingham
Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.EBI
Zydus Research Centre
Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow.EBI
Merck
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach.EBI
Glaxosmithkline R&D
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.EBI
Novartis Institutes For Biomedical Research
Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.EBI
TBA
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.EBI
Ain Shams University
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.EBI
Chengdu University
Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3Kδ inhibitor.EBI
Astellas Pharma
Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα.EBI
School of Traditional Chinese Pharmacy
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.EBI
Hutchison Medipharma
Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases.EBI
Astrazeneca
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.EBI
Eberhard Karls University T£Bingen
Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.EBI
TBA
Design, synthesis and biological evaluation of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates containing sulfonamido as potential PI3Kα inhibitors.EBI
School of Traditional Chinese Pharmacy
Targeting the immunity protein kinases for immuno-oncology.EBI
China Pharmaceutical University
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.EBI
Glaxosmithkline
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor.EBI
University of Basel
Why Some Targets Benefit from beyond Rule of Five Drugs.EBI
Boston University
Discovery of 3-Oxabicyclo[4.1.0]heptane, a Non-nitrogen Containing Morpholine Isostere, and Its Application in Novel Inhibitors of the PI3K-AKT-mTOR Pathway.EBI
Glaxosmithkline R&D
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.EBI
China Pharmaceutical University
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.EBI
Astrazeneca
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.EBI
Novartis Institutes For Biomedical Research
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.EBI
Zhejiang University
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.EBI
Novartis Institutes For Biomedical Research
Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors.EBI
Orleans University
[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors.EBI
Glaxosmithkline
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.EBI
Xi'An Jiaotong University
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.EBI
University of Basel
Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.EBI
Chongqing University
Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.EBI
University of California San Diego
Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors.EBI
Chongqing University
Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ.EBI
China Pharmaceutical University
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.EBI
Shenyang Pharmaceutical University
Optimization and in vivo evaluation of pyrazolopyridines as a potent and selective PI3Kδ inhibitor.EBI
Astellas Pharma
Discovery of novel quinazolinone derivatives as high potent and selective PI3Kδ and PI3Kδ/γ inhibitors.EBI
Shandong University
Discovery and biological evaluation of novel pyrazolopyridine derivatives as potent and orally available PI3Kδ inhibitors.EBI
Astellas Pharma
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.EBI
Astrazeneca
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.EBI
Xi'An Jiaotong University
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.EBI
India Academy of Scientific & Innovative Research (Acsir)
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.EBI
Peking Union Medical College
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.EBI
Astrazeneca
Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα.EBI
Shenyang Pharmaceutical University
Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR).EBI
Integral Biosciences
Discovery of a Novel Inhaled PI3Kδ Inhibitor for the Treatment of Respiratory Diseases.EBI
TBA
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.EBI
Chinese Academy of Sciences
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).EBI
Astrazeneca
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.EBI
Peking Union Medical College
From PIM1 to PI3Kδ via GSK3β: Target Hopping through the Kinome.EBI
Glaxosmithkline
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.EBI
Novartis Institutes For Biomedical Research
Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.EBI
Genentech
Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors.EBI
Pharmaron-Beijing
Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168).EBI
University of Michigan
Potential of PI3Kβ Inhibitors in the Treatment of Cancer and Other Diseases.EBI
Therachem Research Medilab (India)
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.EBI
University Park Nottingham
Synthesis and biological evaluation of 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones against DNA-PK, PI3K, PDE3A enzymes and platelet aggregation.EBI
La Trobe University
SAR study of 5-alkynyl substituted quinazolin-4(3H)-ones as phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.EBI
Shanghai Institute of Materia Medica (Simm)
Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors.EBI
Astrazeneca
Identification of highly potent and selective PI3Kδ inhibitors.EBI
Bristol-Myers Squibb
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.EBI
University of Basel
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinaseδ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.EBI
Bristol-Myers Squibb
Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration.EBI
Astrazeneca
Atropisomerism and Conformational Equilibria: Impact on PI3Kδ Inhibition of 2-((6-Amino-9H-purin-9-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one (IC87114) and Its Conformationally Restricted Analogs.EBI
University of Parma
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.EBI
Astrazeneca
DELIVERY OF THERAPEUTIC ALKALOID COMPOUNDSBDB
Sensorium Therapeutics
Benzimidazolone derived inhibitors of BCL6BDB
Cancer Research Technology
Diarylpyrazole compound, composition comprising same, and use thereofBDB
Shenzhen Targetrx
2,4,6-TRISUBSTITUTED 1,3,5-TRIAZINES AS MODULATORS OF CX3CR1BDB
Astrazeneca
19-nor neuroactive steroids and methods of use thereofBDB
Sage Therpeutics
Bicyclic urea kinase inhibitors and uses thereofBDB
The General Hospital
Substituted amino triazoles useful as chitinase inhibitorsBDB
Molecure
JAK1 pathway inhibitors for the treatment of gastrointestinal diseaseBDB
Incyte
BTK inhibitor compoundsBDB
Eli Lilly
Heterocyclic inhibitors of ATR kinaseBDB
University Of Texas
Immunomodulator compoundsBDB
Chemocentryx
Aryl-phosphorus-oxygen compound as EGFR kinase inhibitorBDB
Chia Tai Tianqing Pharmaceutical Group
Heterocyclic compound as CSF-1R inhibitor and use thereofBDB
Medshine Discovery
2-substituted pyrazole amino-4-substituted amino-5-pyrimidine formamide compound, composition, and application thereofBDB
Beijing Scitech Mq Pharmaceuticals
Potent Inhibition of SARS-CoV-2 nsp14 BDB
University of Montpellier
Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereofBDB
La Jolla Institute of Allergy & Immunology
Compound, compositions, and methodsBDB
Denali Therapeutics
Substituted heterocyclyl derivatives as CDK inhibitorsBDB
Aurigene Discovery Technologies
Pyridylamino substituted heterotricyclic compounds, and preparation method and pharmaceutical use thereofBDB
TBA
Heterocyclic derivatives as PI3K inhibitorsBDB
Incyte
Substituted N-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereofBDB
Sanofi
Fused piperidinyl bicyclic and related compounds as modulators of C5A receptorBDB
Inflarx
Oxazolidinones as taro inhibitorsBDB
Merck Sharp & Dohme
COMPOUNDSBDB
Enterprise Therapeutics
Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptidesBDB
Arvinas Operations
2,6-disubstituted pyridine derivativeBDB
Sumitomo Dainippon Pharma
Biaryltriazole inhibitors of macrophage migration inhibitory factorBDB
Yale University
Heterocyclic compounds for the inhibition of paskBDB
Bioenergenix
DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 MBDB
Baylor College of Medicine
Azetidine derivativesBDB
Vernalis (R&D)
Inhibitors of phosphatidylinositol 3-kinase gammaBDB
Astrazeneca
Compositions and methods for treating KIT- and PDGFRA-mediated diseasesBDB
Blueprint Medicines
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-amineBDB
Kronos Bio
Heterocyclic compounds for the inhibition of PASKBDB
Bioenergenix
Nitrogen-containing heteroaryl compound and pharmaceutical use thereofBDB
Japan Tobacco
Cyanoindazole compounds and uses thereofBDB
Incyte
Rho kinase inhibitorsBDB
Kadmon
Therapeutic compounds and uses thereofBDB
Genentech
Bicyclic heterocycles as FGFR4 inhibitorsBDB
Incyte
Imidazopyridazine compounds and their useBDB
Hutchison Medipharma
Substituted (4'-hydroxyphenyl)cyclohexane compounds and uses thereof as selective agonists of the estrogen receptor beta isoformBDB
Marquette University
Treatment of relapsed and/or refractory solid tumors and non-hodgkin's lymphomasBDB
Celgene Quanticel Research
IBAT inhibitors for the treatment of liver diseasesBDB
Albireo
Positive allosteric modulators of the GLP-1 receptorBDB
Vanderbilt University
Substituted indoles as modulators of ROR-gammaBDB
Vitae Pharmaceuticals
3-amino-1,5,6,7-tetrahydro-4H-indol-4-onesBDB
Bayer Pharma Aktiengesellschaft
Quinazoline derivative and preparation method thereforBDB
Chia Tai Tianqing Pharmaceutical Group
Cycloalkane derivativesBDB
Daiichi Sankyo
Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitorsBDB
Acetylon Pharmaceuticals
Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.BDB
King Fahd University of Petroleum & Minerals
Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitorsBDB
Tolero Pharmaceuticals
Dimeric compoundsBDB
Hoffmann-La Roche
Kinetic and in silico analysis of thiazolidin-based inhibitors of a-carbonic anhydrase isoenzymes.BDB
Ondokuz Mayis University
Pyrimidinyl-pyridazinone derivatives for treating a disease which is influenced by inhibition of met kinaseBDB
Merck Patent
Pharmaceutical uses of 6-amino quinazoline or 3-cyano quinoline derivativesBDB
Jiangsu Hengrui Medicine
Rational design of broad spectrum antibacterial activity based on a clinically relevant enoyl-acyl carrier protein (ACP) reductase inhibitor.BDB
University of Wuerzburg
Substituted quinolines as bruton's tyrosine kinases inhibitorsBDB
Hangzhouderenyucheng Biotechnology
Hydroxylated aminotriazole derivatives as ALX receptor agonistsBDB
Actelion Pharmaceuticals
Pharmacologically active compoundsBDB
Cancer Research Technology
Method for dual inhibition of SGLT1 and SGLT2 using diphenylmethane derivativesBDB
Green Cross
Beta-alanine derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical composition comprising same as active ingredientBDB
Korea Research Institute of Chemical Technology
Acid addition salt of substituted pyridine compoundBDB
Daiichi Sankyo
Facile dimethyl amino group triggered cyclic sulfonamides synthesis and evaluation as alkaline phosphatase inhibitors.BDB
University of Karachi
Methylene linked quinolinyl modulators of RORγtBDB
Janssen Pharmaceutica
An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms.BDB
Universitätsklinikum Frankfurt
Bicyclic sulfonamide compounds as sodium channel inhibitorsBDB
Amgen
Chemotype-selective modes of action of ¿-opioid receptor agonists.BDB
University of North Carolina
Crystal structure and pharmacological characterization of a novel N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site.BDB
University of Copenhagen
N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamidesBDB
Novartis
Amino-substituted imidazopyridazinesBDB
Bayer Pharma Aktiengesellschaft
Substituted amide compoundsBDB
Pfizer
Nitrogen-containing compounds and pharmaceutical compositions thereof for the treatment of atrial fibrillationBDB
Otsuka Pharmaceutical
Treatment of respiratory disorders using TRPA1 antagonistsBDB
Glenmark Pharmaceuticals
Design, synthesis and antitumor activity of novel pyrazolo[3,4-d]pyrimidine derivatives as EGFR-TK inhibitors.BDB
Beni-Suef University
ß-Hydroxyacyl-acyl Carrier Protein Dehydratase (FabZ) from Francisella tularensis and Yersinia pestis: Structure Determination, Enzymatic Characterization, and Cross-Inhibition Studies.BDB
Brookhaven National Laboratory
Pyrazolone derivatives as PDE4 inhibitorsBDB
Takeda
Dihydropyrano [2,3-c] pyrazole: Novel in vitro inhibitors of yeast a-glucosidase.BDB
King Abdulaziz University
Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.BDB
Government College University
Design, synthesis and biological screening of new 4-thiazolidinone derivatives with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.BDB
Beni-Suef University
Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductaseBDB
National Taiwan University
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated pathologiesBDB
Galderma Research & Development
Complement pathway modulators and uses thereofBDB
Novartis
Heterocyclic compounds containing a pyrrolopyridine or benzimidazole coreBDB
Boehringer Ingelheim International
Substituted isoquinolinones and quinazolinonesBDB
Novartis
Inhibitors of the renal outer medullary potassium channelBDB
Merck Sharp & Dohme
Structure-guided design of a high affinity inhibitor to human CtBP.BDB
University of Massachusetts Medical School
Biochemical and structural analysis of inhibitors targeting the ADC-7 cephalosporinase of Acinetobacter baumannii.BDB
Grand Valley State University
Resorcinol derivatives as HSP90 inhibitorsBDB
Nerviano Medical Sciences
Substituted imidazo[1,2-a]pyrimidines and —pyridinesBDB
Bayer Intellectual Property
Inhibitors of STAT3BDB
University of Central Florida Research Foundation
Thiophenecarboxamide derivatives as EP4 receptor ligandsBDB
Merck Frosst Canada
Discovery of orally active, potent, and selective benzotriazole-based PTP1B inhibitors.BDB
Zydus Research Centre
Benzodioxole piperidine compoundsBDB
Hoffmann-La Roche
Aminomethyl quinolone compoundsBDB
Hoffmann-La Roche
Targeting Tumour Proliferation with a Small-Molecule Inhibitor of AICAR Transformylase Homodimerization.BDB
University of Southampton
Inhibition of bacterial virulence: drug-like molecules targeting the Salmonella enterica PhoP response regulator.BDB
Washington University
Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor.BDB
University of Kansas
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.BDB
Abbott Laboratories
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.BDB
Institut De Recherches Servier
Pharmacological characterization of KUR-1246, a selective uterine relaxant.BDB
Kissei Pharmaceutical
Potential of pyrazolooxadiazinone derivatives as serine protease inhibitors.BDB
UniversitÀ
Design and synthesis of conformationally constrained cyclophilin inhibitors showing a cyclosporin-A phenotype in C. elegans.BDB
The University of Edinburgh
Biochemical and pharmacological characterization of L-659,989: an extremely potent, selective and competitive receptor antagonist of platelet-activating factor.BDB
Merck Sharp & Dohme Research Laboratories
Agonist activity of 2- and 5'-substituted adenosine analogs and their N6-cycloalkyl derivatives at A1- and A2-adenosine receptors coupled to adenylate cyclase.BDB
National Institutes of Diabetes and Digestive and Kidney Diseases
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.BDB
Bristol-Myers Squibb
Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase.BDB
Rheinische Friedrich-Wilhelms-Universitat Bonn
 
Human Plasma Lecithin-Cholesterol AcyltransferaseBDB
Dalhousie University