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81 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck & Co.
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
26774655 32 Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.EBI Novartis Institutes for BioMedical Research
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
26403930 56 Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications.EBI Merck Research Laboratories
26288698 38 Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.EBI Merck Research Laboratories
26115573 67 Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4.EBI Merck Research Laboratories
25262942 189 Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI AstraZeneca
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
26101574 30 Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.EBI Merck & Co.
26101573 32 Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.EBI Merck Research Laboratories
25870132 37 Discovery and hit-to-lead optimization of 2,6-diaminopyrimidine inhibitors of interleukin-1 receptor-associated kinase 4.EBI Merck Research Laboratories
25827523 275 Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.EBI Vertex Pharmaceuticals Inc
24913714 53 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
25589930 62 Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.EBI Lexicon Pharmaceuticals, Inc.
25479567 50 Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders.EBI Nimbus Discovery
25313996 91 Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI Merck Research Laboratories
24685542 67 Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI Bristol-Myers Squibb Research and Development
24900590 55 Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.EBI GlaxoSmithKline
23602398 43 Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.EBI Merck Research Laboratories
23587425 37 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
23535330 83 Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.EBI Merck Research Laboratories
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
23116168 42 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
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.
22727637 85 Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI Abbott Laboratories
22503250 128 Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.EBI AMRI
24900358 69 Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.EBI TBA
24900346 90 Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI TBA
21128646 88 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
20138514 93 3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI Vertex Pharmaceuticals Inc
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute-Bethesda
18501603 48 IRAK-4 inhibitors. Part III: a series of imidazo[1,2-a]pyridines.EBI UCB Pharma SA
18474425 27 IRAK-4 inhibitors. Part 1: a series of amides.EBI UCB Pharma SA
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
22136433 67 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
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
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21970471 66 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.EBI Vertex Pharmaceuticals Inc
21936542 143 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
20674350 63 Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
21391610 139 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 Inc
20855207 26 Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
19039322 50 Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.EBI Center for Molecular Medicine of the Austrian Academy of Sciences
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19414255 58 Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI Vertex Pharmaceuticals Inc
18482836 14 IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding.EBI UCB Pharma SA
16563752 38 Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.EBI Amgen Inc
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
28947151 62 Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.EBI Bristol-Myers Squibb Co.
29172502 96 Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88EBI AstraZeneca
28501511 23 Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.EBI AstraZeneca
28498658 47 Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.EBI Pfizer Inc
19245211 9 Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.BDB Intervet Innovation GmbH
18713665 23 Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.BDB Deltagen Research Laboratories
14766749 2 Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.BDB Vertex Pharmaceuticals Inc
18636690 11 Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacids.BDB University of Tennessee Health Science Center
17656360 16 Structural basis of enantioselective inhibition of cyclooxygenase-1 by S-alpha-substituted indomethacin ethanolamides.BDB Michigan State University
16580202 21 Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.BDB GSK
17132625 21 Protein engineering of the colony-stimulating factor-1 receptor kinase domain for structural studies.BDB Johnson & Johnson Pharmaceutical
15715490 145 8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors.BDB Purdue Pharma LP
17028182 47 Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.BDB Incyte Corporation
28892605 20 Inhibitors of the Diadenosine Tetraphosphate Phosphorylase Rv2613c of Mycobacterium tuberculosis.BDB University of Konstanz
17064068 36 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.BDB Palacky University
11563919 20 A structure-based design approach to the development of novel, reversible AChE inhibitors.BDB Syngenta
28440616 7 Discovery and Characterization of a Eukaryotic Initiation Factor 4A-3-Selective Inhibitor That Suppresses Nonsense-Mediated mRNA Decay.BDB BC Cancer Agency