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382 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.EBI
East China Normal University
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.EBI
Sichuan University And Collaborative Innovation Center For Biotherapy
Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.EBI
Carna Biosciences
Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy.EBI
Takeda California
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.EBI
East China Normal University
Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.EBI
Comenius University In Bratislava
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Identification of lead small molecule inhibitors of glycogen synthase kinase-3 beta using a fragment-linking strategy.EBI
Institute For Basic Science (Ibs)
3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents.EBI
Egyptian Russian University
Design, synthesis and biological evaluation of 5-benzylidene-2-iminothiazolidin-4-ones as selective GSK-3ß inhibitors.EBI
National Institute Of Pharmaceutical Education And Research
Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3ß.EBI
Institute Of Harvard And Mit
Synthesis of benzimidazole based thiadiazole and carbohydrazide conjugates as glycogen synthase kinase-3ß inhibitors with anti-depressant activity.EBI
Jamia Hamdard (Hamdard University)
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI
Southeast University
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI
Zhejiang University
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.EBI
Nerviano Medical Sciences
New applications for known drugs: Human glycogen synthase kinase 3 inhibitors as modulators of Aspergillus fumigatus growth.EBI
Centro De Investigaciones Biologicas (Cib, Csic)
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.EBI
Takeda Pharmaceutical
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI
Novartis Institutes For Biomedical Research
Versatility of the Curcumin Scaffold: Discovery of Potent and Balanced Dual BACE-1 and GSK-3ß Inhibitors.EBI
Alma Mater Studiorum-University Of Bologna
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.EBI
Central University
Hit Optimization of 5-Substituted-N-(piperidin-4-ylmethyl)-1H-indazole-3-carboxamides: Potent Glycogen Synthase Kinase-3 (GSK-3) Inhibitors with in Vivo Activity in Model of Mood Disorders.EBI
Angelini
Evaluation of Improved Glycogen Synthase Kinase-3a Inhibitors in Models of Acute Myeloid Leukemia.EBI
Technische Universit£T Darmstadt
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).EBI
Wuxi Apptec
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI
Sichuan University
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI
Hanyang University
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.EBI
Nerviano Medical Sciences
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.EBI
Eli Lilly
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.EBI
Zhejiang University
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI
Astellas Pharma
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.EBI
Vertex Pharmaceuticals
9-Hydroxycanthin-6-one, aß-Carboline Alkaloid from Eurycoma longifolia, Is the First Wnt Signal Inhibitor through Activation of Glycogen Synthase Kinase 3ß without Depending on Casein Kinase 1a.EBI
Chiba University
Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure.EBI
Eli Lilly
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.EBI
Sichuan University
Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.EBI
Bristol-Myers Squibb Research And Development
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.EBI
The Institute Of Cancer Research
Discovery of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally-active GSK-3ß inhibitors for Alzheimer's disease.EBI
Mitsubishi Tanabe Pharma
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.EBI
Vertex Pharmaceuticals
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI
Nerviano Medical Sciences
Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3ß of substituted quinolines.EBI
Kansas State University
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.EBI
Merck Research Laboratories
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI
Glaxosmithkline
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.EBI
Lexicon Pharmaceuticals
Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3ß (GSK-3ß) with cellular activity of promoting glucose uptake.EBI
Fudan University
In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.EBI
Fudan University
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI
Galapagos
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI
Merck Research Laboratories
Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.EBI
Technische Universit£T Darmstadt
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI
Nerviano Medical Sciences
Guanidinium-based derivatives: searching for new kinase inhibitors.EBI
Trinity College
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI
Bristol-Myers Squibb Research And Development
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.EBI
Martin-Luther-University Halle-Wittenberg
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI
Takeda Pharmaceutical
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.EBI
East China University Of Science And Technology
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis
Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3ß (GSK-3ß).EBI
Fudan University
Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.EBI
Abbott Laboratories
Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.EBI
Universitat De Barcelona
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI
Pfizer
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI
Pfizer
3,6-Diamino-4-(2-halophenyl)-2-benzoylthieno[2,3-b]pyridine-5-carbonitriles are selective inhibitors of Plasmodium falciparum glycogen synthase kinase-3.EBI
Technische Universit£T Braunschweig
Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine.EBI
TBA
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3ß inhibitors.EBI
Glaxosmithkline
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI
Glaxosmithkline
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.EBI
Glaxosmithkline
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI
Glaxosmithkline
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.EBI
Takeda Pharmaceutical
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.EBI
Takeda Pharmaceutical
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3ß inhibitors through virtual screening.EBI
Fudan University
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.EBI
Takeda Pharmaceutical
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
Structure-Based Design of Potent and Selective CK1¿ Inhibitors.EBI
TBA
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.EBI
Sichuan University
Novel 3-Azaindolyl-4-arylmaleimides exhibiting potent antiangiogenic efficacy, protein kinase inhibition, and antiproliferative activity.EBI
Johannes Gutenberg University Of Mainz
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.EBI
Cnrs
Discovery of novel potent and highly selective glycogen synthase kinase-3ß (GSK3ß) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.EBI
Astrazeneca
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.EBI
Martin-Luther-University Halle-Wittenberg
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.EBI
Teijin Pharma
Identification of pyrimidine derivatives as hSMG-1 inhibitors.EBI
Pfizer
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.EBI
Takeda Pharmaceutical
2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1¿) inhibitors.EBI
Amgen
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.EBI
Abbott Laboratories
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.EBI
Janssen Pharmaceutical Companies Of Johnson & Johnson
Langkolide, a 32-membered macrolactone antibiotic produced by Streptomyces sp. Acta 3062.EBI
Technische Universit£T Berlin
Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.EBI
Pfizer
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a.EBI
Technische Universit£T Darmstadt
Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.EBI
TBA
Design, synthesis and biological evaluation of novel imidazopyridines as potential antidiabetic GSK3ß inhibitors.EBI
Crystalgenomics
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.EBI
Takeda Pharmaceutical
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.EBI
The Institute Of Cancer Research
Exploring the binding sites of glycogen synthase kinase 3. Identification and characterization of allosteric modulation cavities.EBI
Instituto De Quimica Medica-Csic
Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.EBI
TBA
5-imino-1,2,4-thiadiazoles: first small molecules as substrate competitive inhibitors of glycogen synthase kinase 3.EBI
Instituto De Qu£Mica M£Dica-Csic
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI
TBA
Towards the preparation of radiolabeled 1-aryl-3-benzyl ureas: Radiosynthesis of [(11)C-carbonyl] AR-A014418 by [(11)C]CO(2) fixation.EBI
University Of Toronto
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.EBI
Hanyang University
Eutypoids B-E produced by a Penicillium sp. strain from the North Sea.EBI
Institute Of Marine Sciences (Ifm-Geomar)
Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.EBI
Novartis Institutes For Biomedical Research
Pharmacological inhibitors of glycogen synthase kinase 3.EBI
The Rockefeller University
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI
Nerviano Medical Sciences Oncology
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.EBI
The Institute Of Cancer Research
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI
Vertex Pharmaceuticals
Discovery of potent and bioavailable GSK-3beta inhibitors.EBI
Roche Palo Alto
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.EBI
Nerviano Medical Sciences
Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode.EBI
Peking University
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).EBI
Technische Universit£T Braunschweig
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
The selectivity of protein kinase inhibitors: a further update.EBI
University Of Dundee
The marine natural-derived inhibitors of glycogen synthase kinase-3beta phenylmethylene hydantoins: In vitro and in vivo activities and pharmacophore modeling.EBI
University Of Louisiana At Monroe
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI
National Cancer Institute-Bethesda
Discovery and development of aurora kinase inhibitors as anticancer agents.EBI
Vertex Pharmaceuticals
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.EBI
University Of California
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI
Pfizer
Kinetic studies and bioactivity of potential manzamine prodrugs.EBI
The University Of Mississippi
2-N-Methyl modifications and SAR studies of manzamine A.EBI
The University Of Mississippi
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI
Harvard Medical School
2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3).EBI
Kemia
Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors.EBI
Chemical Diversity Research Institute
Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.EBI
The Institute Of Cancer Research
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Pyrazinoindolone inhibitors of MAPKAP-K2.EBI
Boehringer Ingelheim Pharmaceuticals
Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin.EBI
University Of Jordan
Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors.EBI
Glaxosmithkline
Novel GSK-3beta inhibitors from sequential virtual screening.EBI
Korea Institute Of Science And Technology
Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease.EBI
University Of Mississippi
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.EBI
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.EBI
Eli Lilly
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.EBI
Johnson And Johnson Pharmaceutical Research And Development
Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors.EBI
Novo Nordisk
Structure-activity relationship of the 7-hydroxy benzimidazole analogs as glycogen synthase kinase 3ß inhibitor.EBI
Crystalgenomics
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.EBI
Glaxosmithkline
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI
Glaxosmithkline
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.EBI
Chugai Pharmaceutical
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
Quinolone derivatives containing strained spirocycle as orally active glycogen synthase kinase 3ß (GSK-3ß) inhibitors for type 2 diabetics.EBI
Kyorin Pharmaceutical
6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3ß: discovery of nitrile derivatives with picomolar potency.EBI
Activx Biosciences
Design and combinatorial synthesis of a novel kinase-focused library using click chemistry-based fragment assembly.EBI
Carna Biosciences
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).EBI
Pfizer
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.EBI
Nerviano Medical Sciences
Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI
Pfizer
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI
Ansaris
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.EBI
Takeda Pharmaceutical
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI
RhôNe-Poulenc Rorer
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
Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3ß.EBI
Activx Biosciences
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.EBI
University Of South Florida
Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.EBI
Technische Universit£T Darmstadt
Selectivity of kinase inhibitor fragments.EBI
Glaxosmithkline
Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds.EBI
Instituto De Qui£?Mica Medica-Csic
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.EBI
Nerviano Medical Sciences
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.EBI
Vertex Pharmaceuticals
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.EBI
Glaxosmithkline
Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors.EBI
Harvard Medical School
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.EBI
TBA
6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3ß inhibitors.EBI
Pfizer
Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.EBI
Abbott Laboratories
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.EBI
Abbott Laboratories
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.EBI
National University Of Ireland
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI
TBA
Discovery of novel GSK-3ß inhibitors with potent in vitro and in vivo activities and excellent brain permeability using combined ligand- and structure-based virtual screening.EBI
University Of Louisiana At Monroe
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.EBI
Novartis Institutes For Biomedical Research
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI
Nerviano Medical Sciences
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI
Nerviano Medical Sciences Oncology
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.EBI
Takeda Pharmaceutical
Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells.EBI
University Of Rostock
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Specificity and mechanism of action of some commonly used protein kinase inhibitors.EBI
University Of Dundee
Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.EBI
Daiichi Sankyo
Novel 8-arylated purines as inhibitors of glycogen synthase kinase.EBI
Institut Curie
Synthesis and cytotoxicity of novel indirubin-5-carboxamides.EBI
University Of Kaiserslautern
Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).EBI
Nycomed Pharma
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI
Cyclacel
Emerging targets in osteoporosis disease modification.EBI
Amgen
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.EBI
Nerviano Medical Sciences
Aminofurazans as potent inhibitors of AKT kinase.EBI
Glaxosmithkline
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.EBI
Abbott Laboratories
Design of potent and selective GSK3beta inhibitors with acceptable safety profile and pharmacokinetics.EBI
Sanofi-Aventis
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI
Wyeth Research
Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.EBI
Sanofi-Aventis
Selectively nonselective kinase inhibition: striking the right balance.EBI
Schering-Plough
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI
Cgi Pharmaceuticals
4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.EBI
Vertex Pharmaceuticals
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI
Nerviano Medical Sciences
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.EBI
Glaxosmithkline
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.EBI
Glaxosmithkline
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Thienylhalomethylketones: Irreversible glycogen synthase kinase 3 inhibitors as useful pharmacological tools.EBI
Instituto De Qu£Mica M£Dica-Csic
(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.EBI
Wyeth Research
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.EBI
Takeda Pharmaceutical
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI
Vertex Pharmaceuticals
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.EBI
Zhejiang University
The discovery of the potent aurora inhibitor MK-0457 (VX-680).EBI
Vertex Pharmaceuticals
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.EBI
Sterling Road
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.EBI
Glaxosmithkline
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI
Vertex Pharmaceuticals
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.EBI
University Of Illinois At Chicago
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI
Pfizer
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI
Glaxosmithkline
Synthesis and cytotoxic activity of new azepino[3',4':4,5]pyrrolo[2,1-a]isoquinolin-12-ones.EBI
Universidad Nacional AutóNoma De MéXico
Identification of small molecules that inhibit GSK-3beta through virtual screening.EBI
Korea Research Institute Of Chemical Technology
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI
Glaxosmithkline
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.EBI
Glaxosmithkline
Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors.EBI
Université
Cellular characterization of a novel focal adhesion kinase inhibitor.EBI
University Of Virginia
Novel heterocycle-substituted pyrimidines as inhibitors of NF-kappaB transcription regulation related to TNF-alpha cytokine release.EBI
Seoul National University
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.EBI
Schering-Plough Research Institute
Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.EBI
Crystalgenomics
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.EBI
Abbott Laboratories
Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.EBI
Eberhard-Karls University
Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.EBI
Glaxosmithkline
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.EBI
Università
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.EBI
Astrazeneca
Structural basis for the GSK-3beta binding affinity and selectivity against CDK-2 of 1-(4-aminofurazan-3yl)-5-dialkylaminomethyl-1H-[1,2,3] triazole-4-carboxylic acid derivatives.EBI
Universidade Do Porto
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.EBI
Johnson & Johnson Pharmaceutical Research & Development
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold.EBI
University Of Campinas (Unicamp)
Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3? inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in the brain without affecting that in intestine.EBI
China Pharmaceutical University
Discovery of EBI
China Pharmaceutical University
Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3?/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.EBI
Shenyang Pharmaceutical University
A novel GSK-3 inhibitor binds to GSK-3? via a reversible, time and Cys-199-dependent mechanism.EBI
Ohio University
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.EBI
Eli Lilly
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.EBI
University Paris-Saclay
Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.EBI
University Of South Australia
Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3?.EBI
University Of Central Lancashire
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI
Boehringer Ingelheim Pharmaceuticals
PROTACs suppression of GSK-3?, a crucial kinase in neurodegenerative diseases.EBI
China Pharmaceutical University
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.EBI
Novartis Institutes For Biomedical Research
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Beijing Normal University
An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.EBI
University Of Oxford
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.EBI
Genomics Institute Of The Novartis Research Foundation
Design and synthesis of 3-(4-pyridyl)-5-(4-sulfamido-phenyl)-1,2,4-oxadiazole derivatives as novel GSK-3? inhibitors and evaluation of their potential as multifunctional anti-Alzheimer agents.EBI
Anhui Medical University
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.EBI
China Pharmaceutical University
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.EBI
China Pharmaceutical University
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.EBI
Newcastle University
1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3?.EBI
Charles University
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.EBI
China Pharmaceutical University
Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1).EBI
Shanghai Institute Of Materia Medica
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3K? Inhibitors.EBI
Vertex Pharmaceuticals
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor.EBI
Dana-Farber Cancer Institute
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.EBI
Astrazeneca
Novel CDK2 Inhibitors for Treating Cancer.EBI
Smith, Gambrell & Russell
A novel indirubin derivative that increases somatic cell plasticity and inhibits tumorigenicity.EBI
Gwangju Institute Of Science And Technology
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and EBI
Angelini Pharma
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.EBI
Genomics Institute Of The Novartis Research Foundation (Gnf)
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.EBI
Glaxosmithkline R&D
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.EBI
Astrazeneca
Discovery of the First-in-Class GSK-3?/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.EBI
Alma Mater Studiorum-University Of Bologna
Application of Fragment-Based de Novo Design to the Discovery of Selective Picomolar Inhibitors of Glycogen Synthase Kinase-3 Beta.EBI
Sejong University
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.EBI
Japan Tobacco
Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3? for Alzheimer's disease treatment.EBI
Alma Mater Studiorum-University Of Bologna
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.EBI
Vertex Pharmaceuticals
Pyridinylimidazoles as dual glycogen synthase kinase 3?/p38? mitogen-activated protein kinase inhibitors.EBI
Eberhard Karls Universit£T T£Bingen
Synthesis and biological evaluation of 3-substituted 2-oxindole derivatives as new glycogen synthase kinase 3? inhibitors.EBI
Lomonosov Moscow State University
1-Aryl-3-(4-methoxybenzyl)ureas as potentially irreversible glycogen synthase kinase 3 inhibitors: Synthesis and biological evaluation.EBI
Stellenbosch University
Advancement of multi-target drug discoveries and promising applications in the field of Alzheimer's disease.EBI
Jining Medical University
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.EBI
Glaxosmithkline R&D
Discovery of 4EBI
TBA
Triazole-Based Inhibitors of the Wnt/?-Catenin Signaling Pathway Improve Glucose and Lipid Metabolisms in Diet-Induced Obese Mice.EBI
University Of Maryland
Multi-target design strategies for the improved treatment of Alzheimer's disease.EBI
China Pharmaceutical University
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.EBI
Vertex Pharmaceuticals (Europe)
An insight into medicinal chemistry of anticancer quinoxalines.EBI
India
Synthesis and evaluation of novel GSK-3? inhibitors as multifunctional agents against Alzheimer's disease.EBI
Shandong University
Discovery of novel glycogen synthase kinase-3? inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.EBI
Peking University
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI
University Of Florida
Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-EBI
Northeastern University
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.EBI
Genentech
Pyridinylimidazoles as GSK3? Inhibitors: The Impact of Tautomerism on Compound Activity via Water Networks.EBI
Eberhard Karls Universit£T T£Bingen
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 A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI
Abbvie Bioresearch Center
Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.EBI
The University Of Tokyo
Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme.EBI
University Of Pisa
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).EBI
Moffitt Cancer Center
Discovery of 1,3,4-oxidiazole scaffold compounds as inhibitors of superoxide dismutase expression.EBI
Northwestern University
6-(4-Pyridyl)pyrimidin-4(3H)-ones as CNS penetrant glycogen synthase kinase-3? inhibitors.EBI
Mitsubishi Tanabe Pharma
Characterization of maleimide-based glycogen synthase kinase-3 (GSK-3) inhibitors as stimulators of steroidogenesis.EBI
University Of Illinois At Chicago
Structure-activity relationship (SAR) studies of synthetic glycogen synthase kinase-3? inhibitors: A critical review.EBI
Wuhan Institute Of Technology
The development of potent and selective bisarylmaleimide GSK3 inhibitors.EBI
Lilly Research Laboratories
Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3? (GSK-3?).EBI
Fudan University
Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.EBI
Glaxosmithkline R&D
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.EBI
Yunnan University
Dual GSK-3?/AChE Inhibitors as a New Strategy for Multitargeting Anti-Alzheimer's Disease Drug Discovery.EBI
China Pharmaceutical University
CaEBI
Iwate University
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI
Vertex Pharmaceuticals
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.EBI
Astrazeneca
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.EBI
Merck
First dual AK/GSK-3? inhibitors endowed with antioxidant properties as multifunctional, potential neuroprotective agents.EBI
Universit£
Discovery of new GSK-3? inhibitors through structure-based virtual screening.EBI
Peking University
Tau-Centric Multitarget Approach for Alzheimer's Disease: Development of First-in-Class Dual Glycogen Synthase Kinase 3? and Tau-Aggregation Inhibitors.EBI
Alma Mater Studiorum-University Of Bologna
Glycogen synthase kinase-3 and its inhibitors: Potential target for various therapeutic conditions.EBI
National Institute Of Pharmaceutical Education And Research (Niper)
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute Of Science And Technology (Kist)
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.EBI
Vertex Pharmaceuticals
From PIM1 to PI3K? via GSK3?: Target Hopping through the Kinome.EBI
Glaxosmithkline
Hydroxy-substituted trans-cinnamoyl derivatives as multifunctional tools in the context of Alzheimer's disease.EBI
Alma Mater Studiorum-University Of Bologna
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.EBI
Glaxosmithkline
Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3? inhibitors.EBI
Mitsubishi Tanabe Pharma
Discovery of novel 2-(4-aryl-2-methylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3? inhibitors.EBI
Mitsubishi Tanabe Pharma
The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3? inhibitors for the treatment of ovarian cancer.EBI
Fudan University
Natural and synthetic bioactive inhibitors of glycogen synthase kinase.EBI
Jamia Hamdard (Hamdard University)
Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.EBI
Sanford Burnham Prebys Medical Discovery Institute
Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus.EBI
Rigel Pharmaceuticals
BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease.EBI
University Of Dundee
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.EBI
Novartis Institutes For Biomedical Research
Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.EBI
University Of Kaiserslautern
Subtly Modulating Glycogen Synthase Kinase 3?: Allosteric Inhibitor Development and Their Potential for the Treatment of Chronic Diseases.EBI
Centro De Investigaciones Biol�Gicas-Csic
Designing modulators of dimethylarginine dimethylaminohydrolase (DDAH): a focus on selectivity over arginase.BDB
Christian-Albrechts-University
Effects of some drugs on human erythrocyte glucose 6-phosphate dehydrogenase: an in vitro study.BDB
Ataturk University
Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.BDB
Shandong University
Dihydropyrano [2,3-c] pyrazole: Novel in vitro inhibitors of yeast a-glucosidase.BDB
King Abdulaziz University
Identification of Novel Selective Lysine-Specific Demethylase 1 (LSD1) Inhibitors Using a Pharmacophore-Based Virtual Screening Combined with Docking.BDB
China Pharmaceutical University
Structure-guided design of a selective BCL-X(L) inhibitor.BDB
Walter And Eliza Hall Institute Of Medical Research
New tryptophanase inhibitors: towards prevention of bacterial biofilm formation.BDB
Ben-Gurion University Of The Negev
Comparison of effects of dual transporter inhibitors on monoamine transporters and extracellular levels in rats.BDB
Eli Lilly
Agonist, antagonist, and inverse agonist characteristics of TIPP (H-Tyr-Tic-Phe-Phe-OH), a selective delta-opioid receptor ligand.BDB
University Of Arkansas
Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.BDB
Schering-Plough Research Institute
Characterisation of the specific binding of the histamine H3 receptor antagonist radioligand [3H]GR168320.BDB
Glaxo Research & Development
Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo.BDB
Merck Sharp And Dohme Research Laboratories
Comparison of the pharmacological characteristics of [3H]raclopride and [3H]SCH 23390 binding to dopamine receptors in vivo in mouse brain.BDB
Novo Industri
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.BDB
Abbott Laboratories
Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors.BDB
University Of California Berkeley
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.BDB
Gsk
Structure-based design and synthesis of N(omega)-nitro-L-arginine-containing peptidomimetics as selective inhibitors of neuronal nitric oxide synthase. Displacement of the heme structural water.BDB
Northwestern University
New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation.BDB
Amgen
Antibacterial activity and mechanism of action of a novel anilinouracil-fluoroquinolone hybrid compound.BDB
Microbiotix
Structural variation and inhibitor binding in polypeptide deformylase from four different bacterial species.BDB
Gsk
7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors.BDB
Conforma Therapeutics
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.BDB
Novartis Pharmaceuticals
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.BDB
Amgen
Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.BDB
Abbott Laboratories
Structural basis for Chk1 inhibition by UCN-01.BDB
Glaxosmithkline
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase.BDB
Elan Pharmaceuticals