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154 articles for thisTarget


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

PMID
Data
Article Title
Organization
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 guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.EBI
Temple University
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI
Zhejiang University
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
A review on ROCK-II inhibitors: From molecular modelling to synthesis.EBI
Nirma University
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.EBI
Georgia Institute of Technology
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£
Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.EBI
Vertex Pharmaceuticals
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 biological evaluation of novel, highly active soft ROCK inhibitors.EBI
Agoralaan Abis
Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.EBI
Translational Research Institute
Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.EBI
Lexicon Pharmaceuticals
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI
Galapagos
Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.EBI
Novartis Horsham Research Centre
In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.EBI
Alcon Laboratories
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI
Califia Bio
Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.EBI
The Scripps Research Institute
Amino acid derived quinazolines as Rock/PKA inhibitors.EBI
Translational Research Institute
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis
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
Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.EBI
Msd
Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.EBI
Msd
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI
Glaxosmithkline
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.EBI
Glaxosmithkline
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.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
Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI
Vertex Pharmaceuticals
Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.EBI
H. Lee Moffitt Cancer Center and Research Institute
The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.EBI
TBA
Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK).EBI
University of Tartu
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI
Abbott Laboratories
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI
TBA
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.EBI
Glaxosmithkline
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI
Vertex Pharmaceuticals
Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.EBI
Boehringer Ingelheim Pharmaceuticals
C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.EBI
Wyeth Research
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI
National Cancer Institute-Bethesda
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University of Oxford
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
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
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
Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-II).EBI
The Scripps Research Institute
Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I).EBI
The Scripps Research Institute
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.EBI
Glaxosmithkline
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.EBI
The Scripps Research Institute
Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.EBI
Boehringer Ingelheim Pharmaceuticals
Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.EBI
Kalypsys
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.EBI
Wyeth Research
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
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.EBI
Wyeth Research
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
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
Discovery of highly potent and selective type I B-Raf kinase inhibitors.EBI
Wyeth Research
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.EBI
Wyeth Research
Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.EBI
Translational Research Institute and Department of Molecular Therapeutics
4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.EBI
Vertex Pharmaceuticals
2,3-Diaminopyrazines as rho kinase inhibitors.EBI
Amri
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
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.EBI
Wyeth Research
C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.EBI
Wyeth Research
Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.EBI
Lexicon Pharmaceuticals
Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model.EBI
Ligand Pharmaceuticals
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI
Vertex Pharmaceuticals
Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.EBI
Wyeth Research
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI
Wyeth Research
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI
Glaxosmithkline
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI
Wyeth Research
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.EBI
Hefei University of Technology
Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities.EBI
Sun Yat-Sen University
Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.EBI
West China Hospital
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.EBI
Glaxosmithkline
Novel anilinopyrimidine derivatives as potential EGFREBI
Southeast University
Medulloblastoma drugs in development: Current leads, trials and drawbacks.EBI
University of Connecticut
Discovery of 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one derivatives as a new class of ROCK inhibitors for the treatment of glaucoma.EBI
Sichuan University
Discovery of EBI
Zhejiang University
Structure-guided optimization of a novel class of ASK1 inhibitors with increased spEBI
Takeda Research In California
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Beijing Normal University
Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor.EBI
Janssen Research & Development
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3K? Inhibitors.EBI
Vertex Pharmaceuticals
ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors.EBI
Vertex Pharmaceuticals
Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors.EBI
Bristol Myers Squibb
Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.EBI
Bristol Myers Squibb
Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye.EBI
Taipei Medical University
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.EBI
China Pharmaceutical University
Discovery of thieno[2,3-d]pyrimidin-4(3H)-one derivatives as a new class of ROCK inhibitors.EBI
Sichuan University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Merck
Discovery of (S)-6-methoxy-chroman-3-carboxylic acid (4-pyridin-4-yl-phenyl)-amide as potent and isoform selective ROCK2 inhibitors.EBI
Shanghai Institute of Technology
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
CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.EBI
Shaoxing University
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
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
Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors.EBI
Purdue University
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.EBI
University of Naples Federico Ii
Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design.EBI
Abbvie Bioresearch Center
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 a Novel, Highly Potent, and Selective Thieno[3,2-EBI
Takeda Pharmaceutical
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
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
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.EBI
Universitaire Vaudois
Polyheteroaryl Oxazole/Pyridine-Based Compounds Selected in Vitro as G-Quadruplex Ligands Inhibit Rock Kinase and Exhibit Antiproliferative Activity.EBI
University Paris-Sud
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
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?EBI
University of South Australia
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.EBI
Takeda Pharmaceutical
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute of Science & Technology (Kist)
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.EBI
Bristol-Myers Squibb Research and Development
2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase.EBI
Takeda Pharmaceutical
Evaluation of a dithiocarbamate derivative as an inhibitor of human glutaredoxin-1.BDB
South Dakota State University
Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.BDB
U. 109
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.BDB
Pfizer
Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.BDB
Duke University Medical Center
Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.BDB
University of California San Francisco
Structural basis for selective inhibition of Src family kinases by PP1.BDB
Princeton University
4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.BDB
Merck Research Laboratories
Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.BDB
Gsk
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.BDB
Karo Bio
Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.BDB
University of Tennessee At Knoxville
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.BDB
Merck Research Laboratories