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43 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
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
25353650 111 Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.EBI Pfizer
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
25313996 91 Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI Merck Research Laboratories
23602398 43 Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive 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
23312943 166 Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
22726925 216 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.EBI Cellzome
24900358 69 Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.EBI TBA
22148921 48 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-cEBI Cephalon
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
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
17850214 99 The selectivity of protein kinase inhibitors: a further update.EBI University of Dundee
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute-Bethesda
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
20674350 63 Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
21620699 51 Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI Pfizer
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
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
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
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19053756 27 Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).EBI National Human Genome Research Institute
19035792 85 Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI Glaxosmithkline
19019675 52 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?EBI Pfizer
31757666 314 Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI Merck
31693351 473 Discovery of 4EBI TBA
31400941 4 Discovery of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo signaling pathway inhibitors.EBI Sichuan University
30384048 365 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
31526603 379 Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI Takeda Pharmaceutical
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
30480444 85 Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.EBI Sichuan University/Collaborative Innovation Center of Biotherapy
30082069 359 ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI Vertex Pharmaceuticals
29545102 159 Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.EBI Merck
29107425 90 Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI Korea Institute of Science & Technology (Kist)
15169829 3 Ligand-directed functional heterogeneity of histamine H1 receptors: novel dual-function ligands selectively activate and block H1-mediated phospholipase C and adenylyl cyclase signaling.BDB University of North Carolina At Chapel Hill
17630989 9 Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.BDB Abbott Laboratories