263 articles for thisTarget
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Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.
East China Normal University
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.
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.
East China Normal University
Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors.
Kasetsart University
3-Cyano-6-(5-methyl-3-pyrazoloamino) pyridines (Part 2): A dual inhibitor of Aurora kinase and tubulin polymerization.
Cxs
Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design.
Taiwan National Health Research Institutes
Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening.
University Of Berne
Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.
Entremed
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.
Southeast University
Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors.
Sookmyung Women'S University
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.
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.
Nerviano Medical Sciences
Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors.
Ewha Womans University
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
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).
Icahn School Of Medicine At Mount Sinai
Identification of Substituted Naphthotriazolediones as Novel Tryptophan 2,3-Dioxygenase (TDO) Inhibitors through Structure-Based Virtual Screening.
National Health Research Institutes
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.
Universit£
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.
Sichuan University
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Novartis Institutes For Biomedical Research
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.
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.
Nerviano Medical Sciences
Fluorescent photoaffinity probes for mitotic protein kinase Aurora A.
University Of Tartu
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.
Christian-Albrechts-University Of Kiel
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.
Takeda Pharmaceutical
Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.
Shanghai Chempartner
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.
Genentech
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.
National Health Research Institutes
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.
Sichuan University
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.
Entremed
Synthesis and biological evaluation of 2,4-diaminopyrimidines as selective Aurora A kinase inhibitors.
Lanzhou University
Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.
Zhengzhou University
The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.
TBA
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold.
Zhejiang University
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.
University Health Network
Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors.
Ewha Womans University
Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.
Zhejiang University
Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor.
National Taiwan University
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
Biased and unbiased strategies to identify biologically active small molecules.
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.
Fudan University
Discovery of 4-aminoquinazoline--urea derivatives as Aurora kinase inhibitors with antiproliferative activity.
Southeast University
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.
Genentech
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.
Novartis Institutes For Biomedical Research
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.
Development Center For Biotechnology
Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
Sun Yat-Sen University
Polyphenols bearing cinnamaldehyde scaffold showing cell growth inhibitory effects on the cisplatin-resistant A2780/Cis ovarian cancer cells.
Konkuk University
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.
Zhejiang University
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).
The Institute Of Cancer Research
Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3ß (GSK-3ß) inhibitors.
Zhejiang University
Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.
The Institute Of Cancer Research
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Nerviano Medical Sciences
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
Califia Bio
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.
The Institute Of Cancer Research
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
Entremed
Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.
Takeda Pharmaceutical
A thienopyrimidine derivative induces growth inhibition and apoptosis in human cancer cell lines via inhibiting Aurora B kinase activity.
Fudan University
Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine Aurora kinase inhibitor.
National Health Research Institutes
Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors.
Xuzhou Medical College
Structure-based optimization of oxadiazole-based GSK-3 inhibitors.
Technische Universit£T Darmstadt
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
National Health Research Institutes
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors.
Emd-Serono Research Institute
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.
Sichuan University
Trimeric hemibastadin congener from the marine sponge Ianthella basta.
Heinrich-Heine University
Design and synthesis of tricyclic cores for kinase inhibition.
Abbott Bioresearch Center
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
Hoffmann-La Roche
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Pfizer
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß.
Glaxosmithkline
Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.
The Institute Of Cancer Research
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.
Cellzome
Crystal structure of human aurora B in complex with INCENP and VX-680.
University Of Oxford
Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.
Ambit Biosciences
Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents.
Nanjing University
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Abbott Laboratories
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.
Janssen Pharmaceutical Companies Of Johnson & Johnson
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.
Abbott Laboratories
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
National Health Research Institutes
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a.
Technische Universit£T Darmstadt
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.
Sichuan University
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.
The Institute Of Cancer Research
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
Hanmi Research Center
Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors.
Biogen Idec
Synthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors.
Korea Research Institute Of Chemical Technology
Synthesis, biological evaluation, and molecular docking studies of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives as anticancer agents.
Nanjing University
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Amgen
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Ambit Biosciences
Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.
TBA
Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.
Amri
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Abbott Laboratories
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
TBA
Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1.
Biogen Idec
Unbiased binding assays for discovering small-molecule probes and drugs.
Broad Institute Of Harvard And Mit
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c
Cephalon
Single step synthesis of new fused pyrimidine derivatives and their evaluation as potent Aurora-A kinase inhibitors.
Umm Al-Qura University
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Merck Research Laboratories
Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase.
Evotec (Uk)
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.
Nerviano Medical Sciences Oncology
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.
National Taiwan University
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.
The Institute Of Cancer Research
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.
Glaxosmithkline
Through the"gatekeeper door": exploiting the active kinase conformation.
Nerviano Medical Sciences
Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.
Institute Of Science And Technology
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
Nerviano Medical Sciences
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.
Schering-Plough Research Institute
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
National Cancer Institute-Bethesda
Discovery and development of aurora kinase inhibitors as anticancer agents.
Vertex Pharmaceuticals
2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3).
Kemia
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.
Millennium Pharmaceuticals
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
Amgen
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
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.
Osi Pharmaceuticals
Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.
National Health Research Institutes
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.
Pfizer
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Astrazeneca
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.
Westf£Lische Wilhelms-Universit£T M£Nster
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Glaxosmithkline
Selection of cyclic-peptide inhibitors targeting Aurora kinase A: problems and solutions.
University Of Arizona
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Ludwig-Maximilians University Of Munich
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Pfizer
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.
Shenyang Pharmaceutical University
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.
Nerviano Medical Sciences
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
Shionogi
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Design and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors.
Korea Research Institute Of Chemical Technology
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.
Vertex Pharmaceuticals
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Novartis Institute For Biomedical Research
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.
Technische Universit£T Darmstadt
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Ambit Biosciences
Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
Biogen Idec
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.
The Institute Of Cancer Research
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.
Nerviano Medical Sciences
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
National Health Research Institutes
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.
Pfizer
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.
Mitsubishi Tanabe Pharma
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.
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.
Vertex Pharmaceuticals
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Glaxosmithkline
8-Hydroxynaphthalene-1,4-dione derivative as novel compound for glioma treatment.
University Of Padova
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
Amgen
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
TBA
Molecular modeling studies on imidazo[4,5-b]pyridine derivatives as Aurora A kinase inhibitors using 3D-QSAR and docking approaches.
Jinan University
Computational approach to the identification of novel Aurora-A inhibitors.
Korea Institute Of Science And Technology
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.
Martin-Luther-University Halle-Wittenberg
Identification of potent ITK inhibitors through focused compound library design including structural information.
Nycomed
Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine and benzo[4,5]imidazo[1,2-a]pyrimidine compounds as dual KSP and Aurora-A kinase inhibitors for anti-cancer agents.
China Pharmaceutical University
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.
The Institute Of Cancer Research
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
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.
Takeda Pharmaceutical
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Rational design of inhibitors that bind to inactive kinase conformations.
Novartis Research Foundation
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.
Université
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile.
Development Center For Biotechnology
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.
National Health Research Institutes
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.
Cyclacel
Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.
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.
Nerviano Medical Sciences
5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.
Institute Of Science And Technology
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.
Abbott Laboratories
Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors.
S*Bio
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
Genentech
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.
Chugai Pharmaceutical
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.
Zhejiang University
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.
Vertex Pharmaceuticals
N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.
4Sc
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Glaxosmithkline
Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.
Amgen
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Glaxosmithkline
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?
Pfizer
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.
Johnson & Johnson Pharmaceutical Research And Development
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.
Amgen
A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.
Johnson & Johnson Pharmaceutical Research And Development
Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry.
Sunesis Pharmaceuticals
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
Eberhard-Karls University
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.
The Institute Of Cancer Research
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.
University Of Athens
Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.
Abbott Laboratories
Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors.
Activesight
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.
Eberhard-Karls University
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors.
Valeant Pharmaceuticals Research & Development
Accurate prediction of the relative potencies of members of a series of kinase inhibitors using molecular docking and MM-GBSA scoring.
Astrazeneca R&D Boston
Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases.
Imclone Systems
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.
Nankai University
Structure-based virtual screening toward the discovery of novel inhibitors of the DNA repair activity of the human apurinic/apyrimidinic endonuclease 1.
Universidade De Lisboa
Long residence times revealed by Aurora A kinase-targeting fluorescent probes derived from inhibitors MLN8237 and VX-689.
University Of Tartu
Spiro[9,10-dihydroanthracene]-9,3'-pyrrolidine-a structurally unique tetracyclic 5-HT2A receptor antagonist.
Virginia Commonwealth University
Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands.
Universit&Aagrove
Agonist, antagonist, and inverse agonist characteristics of TIPP (H-Tyr-Tic-Phe-Phe-OH), a selective delta-opioid receptor ligand.
University Of Arkansas
Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R).
National Institute Of Diabetes And Digestive And Kidney Diseases
Pharmacological characterization of the constitutively activated state of the serotonin 5-HT2C receptor.
Albany Medical College
Expression of recombinant homo-oligomeric 5-hydroxytryptamine3 receptors provides new insights into their maturation and structure.
Medical Research Council Centre
Antiproliferative activity against MCF-7 breast cancer cells by diamino-triazaspirodiene antifolates.
National University Of Singapore
The binding of [3H]-prostacyclin to membranes of a neuronal somatic hybrid.
Royal Postgraduate Medical School
Molecular cloning and expression of a dopamine D2 receptor from human retina.
National Institute Of Neurological Disorders And Stroke
Carbonic anhydrase inhibitors: inhibition of cytosolic carbonic anhydrase isozymes II and VII with simple aromatic sulfonamides and some azo dyes.
Universita Degli Studi Di Firenze
Sequential mechanism of assembly of multidrug efflux pump AcrAB-TolC.
University Of Oklahoma
Characterization of the binding of [3H]muscimol, a potent gamma-aminobutyric acid agonist, to rat brain synaptosomal membranes using a filtration assay.
TBA
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
The Scripps Research Institute
Identification and Biological Evaluation of a Series of 1H-Benzo[de]isoquinoline-1,3(2H)-diones as Hepatitis C Virus NS5B Polymerase Inhibitors.
Irbm, Mrl Rome
Flaviviral protease inhibitors identified by fragment-based library docking into a structure generated by molecular dynamics.
University Of Zurich
A structure-based approach to ligand discovery for 2C-methyl-D-erythritol-2,4-cyclodiphosphate synthase: a target for antimicrobial therapy.
University Of Dundee
Structural insight into the inhibition of human kynurenine aminotransferase I/glutamine transaminase K.
Virginia Tech
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
Gsk
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
Vernalis (R&D)
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.
Abbott Laboratories