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107 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28291695 36 Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy.EBI Takeda California Inc
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI AbbVie Bioresearch Center
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck & Co.
27050625 76 Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.EBI Temple University
27089211 38 Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI Zhejiang University
27117263 51 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 Co., Ltd
27080184 3 A review on ROCK-II inhibitors: From molecular modelling to synthesis.EBI Nirma University
26356532 39 Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.EBI Georgia Institute of Technology
26762835 342 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
26318056 25 Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.EBI Universit£ di Pisa
26039570 100 Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.EBI Vertex Pharmaceuticals Inc
26071372 89 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 Inc
25898023 67 Design, synthesis, and biological evaluation of novel, highly active soft ROCK inhibitors.EBI Agoralaan Abis
25621531 114 Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.EBI Translational Research Institute
25589936 36 Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.EBI Lexicon Pharmaceuticals, Inc.
25369270 93 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI Galapagos NV
25248678 66 Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.EBI Novartis Horsham Research Centre
24684843 24 In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.EBI Alcon Laboratories Inc
24044867 86 Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI Califia Bio Inc.
23570561 80 Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.EBI The Scripps Research Institute
23416002 126 Amino acid derived quinazolines as Rock/PKA inhibitors.EBI Translational Research Institute
23394126 170 Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI Exelixis Inc
23394218 159 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
21251828 44 Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.EBI MSD
21145740 41 Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.EBI MSD
19303774 87 1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI GlaxoSmithKline
19349179 47 4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.EBI GlaxoSmithKline
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
22795331 51 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 L.L.C.
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Vertex Pharmaceuticals Inc
22272748 46 Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.EBI H. Lee Moffitt Cancer Center and Research Institute
24900264 106 The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.EBI TBA
22521647 56 Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK).EBI University of Tartu
22465635 95 Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI Abbott Laboratories
24900346 90 Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI TBA
20420387 118 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.EBI GlaxoSmithKline
20138514 93 3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI Vertex Pharmaceuticals Inc
20000469 179 Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.EBI Boehringer Ingelheim Pharmaceuticals Inc
19703774 56 C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.EBI Wyeth Research
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute-Bethesda
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
22310227 89 5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.EBI GlaxoSmithKline
17018693 30 Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.EBI GlaxoSmithKline
22014550 337 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
22018789 73 Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-II).EBI The Scripps Research Institute
22004718 58 Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I).EBI The Scripps Research Institute
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21341675 266 Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.EBI GlaxoSmithKline
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20684608 73 Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.EBI The Scripps Research Institute
20462760 70 Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.EBI Boehringer Ingelheim Pharmaceuticals Inc
20434334 60 Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.EBI Kalypsys Inc
19894727 164 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
20346655 117 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
20223663 100 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
20188552 75 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
19884006 47 Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI Wyeth Research
20166671 85 Selectively nonselective kinase inhibition: striking the right balance.EBI Schering-Plough
19854649 49 Discovery of highly potent and selective type I B-Raf kinase inhibitors.EBI Wyeth Research
19854645 87 Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.EBI Wyeth Research
19837589 52 Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.EBI Translational Research Institute and Department of Molecular Therapeutics
19632115 105 4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.EBI Vertex Pharmaceuticals Inc
20022494 60 2,3-Diaminopyrazines as rho kinase inhibitors.EBI AMRI
20006497 49 2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.EBI GlaxoSmithKline
20005102 34 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.EBI GlaxoSmithKline
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19762237 58 First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.EBI Wyeth Research
19682896 49 C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.EBI Wyeth Research
19831390 54 Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.EBI Lexicon Pharmaceuticals
19800787 27 Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model.EBI Ligand Pharmaceuticals Inc
19361991 80 Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI Vertex Pharmaceuticals Inc
19447612 59 Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.EBI Wyeth Research
19364658 113 Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI Wyeth Research
19285393 90 Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI GlaxoSmithKline
18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
15955699 33 (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
26509640 234 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
23275831 121 Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).EBI Moffitt Cancer Center
29969256 21 Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.EBI Centre Hospitalier Universitaire Vaudois (CHUV) and University of Lausanne (UNIL)
30457335 9 Polyheteroaryl Oxazole/Pyridine-Based Compounds Selected in Vitro as G-Quadruplex Ligands Inhibit Rock Kinase and Exhibit Antiproliferative Activity.EBI University Paris-Sud
30082069 359 ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI Vertex Pharmaceuticals Inc
29945794 193 ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI Vertex Pharmaceuticals, Inc
29266937 36 Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?EBI University of South Australia
28284870 77 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 Co., Ltd
29107425 90 Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI Korea Institute of Science and Technology (KIST)
28539220 198 Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.EBI Bristol-Myers Squibb Research and Development
28533114 91 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 Co., Ltd
22299579 1 Evaluation of a dithiocarbamate derivative as an inhibitor of human glutaredoxin-1.BDB South Dakota State University
1975644 47 Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.BDB U. 109
17581239 25 Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.BDB Pfizer Inc
18804034 9 Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.BDB Duke University Medical Center
10662686 6 Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.BDB University of California San Francisco
10467133 4 Structural basis for selective inhibition of Src family kinases by PP1.BDB Princeton University
16275079 29 4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.BDB Merck Research Laboratories
18457381 36 Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.BDB GSK
16303304 18 Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.BDB Karo Bio AB
17696333 2 Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.BDB University of Tennessee at Knoxville
17055272 30 (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