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282 articles for thisTarget


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

PMID
Data
Article Title
Organization
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.EBI
Chugai Pharmaceutical
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
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Synthetic sulfoglycolipids targeting the serine-threonine protein kinase Akt.EBI
University Of Milano-Bicocca
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
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI
Novartis Institutes For Biomedical Research
Synthesis and evaluation of the cytotoxic activity of novel ethyl 4-[4-(4-substitutedpiperidin-1-yl)]benzyl-phenylpyrrolo[1,2-a]quinoxaline-carboxylate derivatives in myeloid and lymphoid leukemia cell lines.EBI
University Of Bordeaux
3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1.EBI
Baylor College Of Medicine
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).EBI
Icahn School Of Medicine At Mount Sinai
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.EBI
Universit£
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI
Hanyang University
Design, synthesis and biological characterization of selective LIMK inhibitors.EBI
Amakem Therapeutics
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
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
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.EBI
Christian-Albrechts-University Of Kiel
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
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
Exploitation of the ability of¿-tocopherol to facilitate membrane co-localization of Akt and PHLPP1 to develop PHLPP1-targeted Akt inhibitors.EBI
The Ohio State University
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI
Nerviano Medical Sciences
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
Biased and unbiased strategies to identify biologically active small molecules.EBI
Institut De Chimie Des Substances Naturelles
In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.EBI
Fudan University
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.EBI
Zhejiang University
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI
Merck Research Laboratories
2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.EBI
Vanderbilt University Medical Center
Phenylalanine-Based Inactivator of AKT Kinase: Design, Synthesis, and Biological Evaluation.EBI
Virginia Commonwealth University
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI
Nerviano Medical Sciences
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.EBI
Martin-Luther-University Halle-Wittenberg
Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors.EBI
Zhejiang University
Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl)-sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III.EBI
Shandong University
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.EBI
Zhejiang University
Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.EBI
Heinrich Heine Universit£T
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.EBI
Heinrich-Heine-Universit£T D£Sseldorf
Preparation and evaluation of deconstruction analogues of 7-deoxykalafungin as AKT kinase inhibitors.EBI
Virginia Commonwealth University
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI
Nerviano Medical Sciences
Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II.EBI
Shandong University
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.EBI
The Institute Of Cancer Research
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.EBI
Merck Research Laboratories
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.EBI
Merck Research Laboratories
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.EBI
Merck Research Laboratories
Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.EBI
Pfizer
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
Synthesis, characterization and Akt phosphorylation inhibitory activity of cyclopentanecarboxylate-substituted alkylphosphocholines.EBI
Kyung Hee University
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.EBI
University Of Nottingham
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.EBI
Emory University
Structure-based discovery of cellular-active allosteric inhibitors of FAK.EBI
Takeda Pharmaceutical
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis
Trimeric hemibastadin congener from the marine sponge Ianthella basta.EBI
Heinrich-Heine University
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.EBI
Astrazeneca
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
Irreversible protein kinase inhibitors: balancing the benefits and risks.EBI
Covalution Pharma
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
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
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.EBI
Array Biopharma
Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.EBI
Arqule
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI
Exelixis
Synthesis, cytotoxicity of new 4-arylidene curcumin analogues and their multi-functions in inhibition of both NF-¿B and Akt signalling.EBI
Sun Yat-Sen University
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
2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.EBI
Technische Universit£T Braunschweig
Diverse heterocyclic scaffolds as allosteric inhibitors of AKT.EBI
Astrazeneca
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI
Amgen
Pyrazolopyrimidines as dual Akt/p70S6K inhibitors.EBI
Exelixis
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.EBI
TBA
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI
TBA
Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors.EBI
Exelixis
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.EBI
Merck Research Laboratories
Development of chemical probes: toward the mode of action of a methylene-linked di(aryl acetate) E1.EBI
University College London
Features of selective kinase inhibitors.EBI
University Of California San Francisco
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI
Nerviano Medical Sciences Oncology
Through the"gatekeeper door": exploiting the active kinase conformation.EBI
Nerviano Medical Sciences
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
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.EBI
Schering-Plough Research Institute
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI
National Cancer Institute-Bethesda
Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.EBI
Glaxosmithkline
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI
Pfizer
Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.EBI
Wyeth Research
Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.EBI
Abbott Laboratories
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI
Bristol-Myers Squibb Research And Development
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.EBI
Osi Pharmaceuticals
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.EBI
Merck
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.EBI
Merck Research Laboratories
Rapid assembly of diverse and potent allosteric Akt inhibitors.EBI
Merck Research Laboratories
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.EBI
Novartis Institute For Biomedical Research
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.EBI
Pfizer
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
Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells.EBI
University Of Pune
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.EBI
Hoffmann-La Roche
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.EBI
Serono Pharmaceutical Research Institute
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
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.EBI
Westf£Lische Wilhelms-Universit£T M£Nster
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.EBI
Glaxosmithkline
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.EBI
Glaxosmithkline
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
Synthesis and biological activity of novel organoselenium derivatives targeting multiple kinases and capable of inhibiting cancer progression to metastases.EBI
Institute Of The Sir Mortimer Jewish General Hospital
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
Synthesis of GSK3ß mimetic inhibitors of Akt featuring a novel extended dipeptide surrogate.EBI
H. Lee Moffitt Cancer Center And Research Institute
9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.EBI
Peking University
Pharmacophore identification, virtual screening and biological evaluation of prenylated flavonoids derivatives as PKB/Akt1 inhibitors.EBI
Zhejiang University
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
Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.EBI
Amgen
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.EBI
Chugai Pharmaceutical
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
Selectivity of kinase inhibitor fragments.EBI
Glaxosmithkline
Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.EBI
Heinrich Heine Universit£T
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.EBI
Bristol-Myers Squibb
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI
Merck Research Laboratories
Backbone cyclic peptide inhibitors of protein kinase B (PKB/Akt).EBI
The Hebrew University Of Jerusalem
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.EBI
Chugai Pharmaceutical
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 optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.EBI
Amgen
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
Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.EBI
Array Biopharma
Discovery and SAR of spirochromane Akt inhibitors.EBI
Array Biopharma
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.EBI
TBA
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.EBI
TBA
Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.EBI
Array Biopharma
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.EBI
Novartis Institutes For Biomedical Research
5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidines as novel class of potent and highly selective CaMKII inhibitors.EBI
Dainippon Sumitomo Pharma
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI
Nerviano Medical Sciences
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI
Merck Research Laboratories
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI
Nerviano Medical Sciences Oncology
4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.EBI
Pfizer
Discovery of pyrrolopyrimidine inhibitors of Akt.EBI
Array Biopharma
Inhibitor hijacking of Akt activation.EBI
University Of California
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI
Amgen
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
Design of selective, ATP-competitive inhibitors of Akt.EBI
Pfizer
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI
Novartis Institute Of Biomedical Research
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI
Cyclacel
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
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.EBI
Wyeth Research
The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).EBI
Wyeth Research
Aminofurazans as potent inhibitors of AKT kinase.EBI
Glaxosmithkline
Synthesis and structure-activity relationship studies of peptidomimetic PKB/Akt inhibitors: the significance of backbone interactions.EBI
The Hebrew University Of Jerusalem
B-Raf kinase inhibitors: hit enrichment through scaffold hopping.EBI
Wyeth Research
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI
Wyeth Research
Selectively nonselective kinase inhibition: striking the right balance.EBI
Schering-Plough
Azole-based inhibitors of AKT/PKB for the treatment of cancer.EBI
Amgen
2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.EBI
Amgen
5-Substituted [1]pyrindine derivatives with antiproliferative activity.EBI
University Of Paris
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI
Cgi Pharmaceuticals
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.EBI
Institute For Medical Research
Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).EBI
The Institute Of Cancer Research
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI
Nerviano Medical Sciences
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.EBI
Chugai Pharmaceutical
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 I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.EBI
Glaxosmithkline
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.EBI
Glaxosmithkline
Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR.EBI
Taisho Pharmaceutical
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.EBI
Taisho Pharmaceutical
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.EBI
The University Of Texas
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.EBI
Hanmi Research Center
QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine.EBI
Zhejiang University
Discovery of a novel protein kinase B inhibitor by structure-based virtual screening.EBI
Torrey Pines Institute For Molecular Studies
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.EBI
Wyeth Research
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.EBI
Boehringer Ingelheim Pharmaceuticals
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.EBI
Wyeth Research
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI
Glaxosmithkline
Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.EBI
Merck Research Laboratories
Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles.EBI
Institute Of General Genetics
Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.EBI
The Scripps Research Institute-Florida
Chroman-3-amides as potent Rho kinase inhibitors.EBI
The Scripps Research Institute
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.EBI
Wyeth Research
The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.EBI
Merck Research Laboratories
Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors.EBI
Merck Research Laboratories
Recent developments in fragment-based drug discovery.EBI
Astex Therapeutics
A phthalide with in vitro growth inhibitory activity from an oidiodendron strain.EBI
Cetek
Entry into a new class of protein kinase inhibitors by pseudo ring design.EBI
Novartis Institutes For Biomedical Research
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI
Glaxosmithkline
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
SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.EBI
Bayer Research Center
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.EBI
Abbott Laboratories
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.EBI
Roche Research Center
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.EBI
Abbott Laboratories
Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics.EBI
Yale University
Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927.EBI
Wyeth Research
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
Synthesis and biological evaluation of 5-arylamino-6-chloro-1H-indazole-4,7-diones as inhibitors of protein kinase B/Akt.EBI
Ildong Pharmaceutical
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI
Amgen
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.EBI
Chiron
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.EBI
Abbott Laboratories
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade.EBI
Wyeth Research
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI
Boehringer Ingelheim Pharmaceuticals
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth.EBI
Georgetown University Medical Center
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.EBI
Arqule
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
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.EBI
Chinese Academy Of Sciences
Pharmaceutical significance of azepane based motifs for drug discovery: A critical review.EBI
Wuhan Institute Of Technology
Coumarin-containing hybrids and their anticancer activities.EBI
Tsinghua University
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.EBI
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital
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
Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors.EBI
Hangzhou Institute Of Innovative Medicine
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
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).EBI
Moffitt Cancer Center
Benzofuran derivatives as a novel class of inhibitors of mTOR signaling.EBI
Cnrs/Universit£
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.EBI
Shanghai Pharmaceuticals Holding
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium.EBI
Heinrich-Heine-Universitat
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense.EBI
Heinrich-Heine-Universit£T
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.EBI
Georgetown University Medical Center
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.EBI
Yunnan 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
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.EBI
Universit£
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.EBI
Merck
Structural optimization elaborates novel potent Akt inhibitors with promising anticancer activity.EBI
Shandong University
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.EBI
University Of Edinburgh
Design, synthesis, in vitro and in silico evaluation of a new series of oxadiazole-based anticancer agents as potential Akt and FAK inhibitors.EBI
Anadolu University
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.EBI
Chinese Academy Of Medical Sciences And Peking Union Medical College
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute Of Science And Technology (Kist)
Acridone-pyrimidine hybrids- design, synthesis, cytotoxicity studies in resistant and sensitive cancer cells and molecular docking studies.EBI
Svkm'S Dr. Bhanuben Nanavati College Of Pharmacy
Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.EBI
Eli Lilly
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.EBI
The Ohio State University
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
Recent progress towards clinically relevant ATP-competitive Akt inhibitors.EBI
Merck
One-Bead-Two-Compound Thioether Bridged Macrocyclic?-AApeptide Screening Library against EphA2.EBI
University Of South Florida
Price for Opening the Transient Specificity Pocket in Human Aldose Reductase upon Ligand Binding: Structural, Thermodynamic, Kinetic, and Computational Analysis.BDB
Philipps-Universität Marburg
Electrostatic Interactions as Mediators in the Allosteric Activation of Protein Kinase A RIa.BDB
University Of California San Diego
Small-Molecule Chemical Probe Rescues Cells from Mono-ADP-Ribosyltransferase ARTD10/PARP10-Induced Apoptosis and Sensitizes Cancer Cells to DNA Damage.BDB
University Of Oulu
Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases.BDB
University Of Anterwerp
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.BDB
Pfizer
SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.BDB
Smithkline Beecham Pharmaceuticals
Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.BDB
University Of Toronto
Affinity and selectivity of PD156707, a novel nonpeptide endothelin antagonist, for human ET(A) and ET(B) receptors.BDB
University Of Cambridge
Characteristics of 125I-iodocyanopindolol binding to beta-adrenergic and serotonin-1B receptors of rat brain: selectivity of beta-adrenergic agents.BDB
Niigata College Of Pharmacy
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.BDB
Pfizer
Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility.BDB
University Of Pittsburgh
Di-, tri- and tetra-5'-O-phosphorothioadenosyl substituted polyols as inhibitors of Fhit: Importance of the alpha-beta bridging oxygen and beta phosphorus replacement.BDB
Kimmel Cancer Center
Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-Type Cannabinoid CB(2) Receptor Inverse Agonists.BDB
University Of Bern
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.BDB
University Of Michigan
Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.BDB
University Of Michigan
Beta-lactam congeners of orlistat as inhibitors of fatty acid synthase.BDB
Texas A&M University