110 articles for thisTarget
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Article Title
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Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Synthesis, anticancer, and docking studies of salicyl-hydrazone analogues: A novel series of small potent tropomyosin receptor kinase A inhibitors.
Dongguk University
Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain.
Eli Lilly
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
St. John'S University
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.
Southeast 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
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.
Takeda Pharmaceutical
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit.
The University Of Tokyo
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
Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors.
Institute For Basic Science (Ibs)
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
Wuxi Apptec
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
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.
Astellas Pharma
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.
Vertex Pharmaceuticals
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Genomics Institute Of The Novartis Research Foundation
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
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
Design and nuclear magnetic resonance (NMR) structure determination of the second extracellular immunoglobulin tyrosine kinase A (TrkAIg2) domain construct for binding site elucidation in drug discovery.
Southmead Hospital
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.
University Of North Carolina At Chapel Hill
Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.
Universit£
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain.
Merck Research Laboratories
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expo
Pfizer
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Pfizer
Inhibitors of Tropomyosin-Receptor Kinases (Trk's): Potential Pain Therapy and More.
Therachem Research Medilab (India)
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, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase
Genomics Institute Of The Novartis Research Foundation
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors.
Emd-Serono Research Institute
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.
Universite£
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Genentech
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Glaxosmithkline
Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).
Johnson & Johnson Pharmaceutical Research & Development
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
TBA
Design, synthesis, and evaluation of 3,5-disubstituted 7-azaindoles as Trk inhibitors with anticancer and antiangiogenic activities.
Korea Advanced Institute Of Science And Technology (Kaist)
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
Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.
TBA
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
TBA
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
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
Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.
Astrazeneca R&D
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.
Nerviano Medical Sciences Oncology
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
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.
Boehringer Ingelheim Pharmaceuticals
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
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
TrkA kinase inhibitors from a library of modified and isosteric Staurosporine aglycone.
Cephalon
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
Inhibition of protein-protein association by small molecules: approaches and progress.
Pfizer
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.
Glaxosmithkline
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Pfizer
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 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
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
Pfizer
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.
Astrazeneca R&D Boston
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
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
Nerviano Medical Sciences Oncology
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.
Center For Molecular Medicine Of The Austrian Academy Of Sciences
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.
Université
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
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.
Bristol-Myers Squibb Research And Development
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
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.
Astrazeneca R&D Boston
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.
Bristol-Myers Squibb Research And Development
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.
Johnson & Johnson Pharmaceutical Research & Development
Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.
Bristol-Myers Squibb Research And Development
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.
Cephalon
Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.
Cephalon
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin
Cephalon
Neurotrophic 3,9-bis[(alkylthio)methyl]-and-bis(alkoxymethyl)-K-252a derivatives.
Kyowa Hakko Kogyo
Structure-activity relationships of bergenin derivatives effect on a-glucosidase inhibition.
Kinki University
Interaction of superoxide dismutase with the glycine zipper regions of ß-amyloid peptides: is there an implication towards Alzheimer's disease and oxidative stress?
Rhodes University
Roles of phosphate recognition in inositol 1,3,4,5,6-pentakisphosphate 2-kinase (IPK1) substrate binding and activation.
Mcgill University
Design and synthesis of new 2-anilinoquinolines bearing N-methylpicolinamide moiety as potential antiproliferative agents.
Korea Institute Of Science And Technology
Vectorial transport of the peptide CCK-8 by double-transfected MDCKII cells stably expressing the organic anion transporter OATP1B3 (OATP8) and the export pump ABCC2.
German Cancer Research Center
Pharmacological characterization of the constitutively activated state of the serotonin 5-HT2C receptor.
Albany Medical College
Substituted 1,4-benzodiazepine-2,5-diones as alpha-helix mimetic antagonists of the HDM2-p53 protein-protein interaction.
Johnson & Johnson Pharmaceutical Research & Development
Virtual screening for potential inhibitors of homology modeled Leptospira interrogans MurD ligase.
Svims University
Characterization of a novel 5-HT4 receptor antagonist of the azabicycloalkyl benzimidazolone class: DAU 6285.
Centre De Pharmacologie-Endocrinologie (Montpellier, France)