427 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.
High Magnetic Field Laboratory
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.
Chugai Pharmaceutical
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.
East China Normal University
Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3.
Eberhard Karls Universit£T T£Bingen
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.
Glaxosmithkline
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
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma.
Sygnature Discovery
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.
High Magnetic Field Laboratory
Fragment-based drug discovery of potent and selective MKK3/6 inhibitors.
Takeda California
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
Tetra-substituted pyridinylimidazoles as dual inhibitors of p38a mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases.
Eberhard Karls Universit£T T£Bingen
Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38aMAPK and ERK1/2 inhibitory activity.
Cairo University
Discovery and characterization of MAPK-activated protein kinase-2 prevention of activation inhibitors.
Astrazeneca
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
Design and synthesis of 5-[(2-chloro-6-fluorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (AKP-001), a novel inhibitor of p38 MAP kinase with reduced side effects based on the antedrug concept.
Aska Pharmaceutical
Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.
Syncom
Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors.
Hanyang University
Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.
Translational Research Institute
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Galapagos
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents.
Zhejiang Academy of Medical Sciences
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.
Takeda Pharmaceutical
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.
East China University of Science and Technology
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.
Emory University
Amino acid derived quinazolines as Rock/PKA inhibitors.
Translational Research Institute
Structure-based discovery of cellular-active allosteric inhibitors of FAK.
Takeda Pharmaceutical
A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.
Peking Union Medical College
Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform.
Cyclofluidic
Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity.
University of T£Bingen
Synthesis and biological activity of pyridopyridazin-6-one p38a MAP kinase inhibitors. Part 2.
Merck Research Laboratories
p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.
Glaxosmithkline
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.
Glaxosmithkline
Development of N-2,4-pyrimidine-N-phenyl-N'-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-alpha) synthesis. Part 1.
Procter and Gamble Pharmaceuticals
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.
Takeda Pharmaceutical
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
Takeda Pharmaceutical
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.
Cellzome
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.
Sichuan University
A frozen analogue approach to aminopyridinylimidazoles leading to novel and promising p38 MAP kinase inhibitors.
University of Tuebingen
Targeting the hinge glycine flip and the activation loop: novel approach to potent p38a inhibitors.
Eberhard Karls University T£Bingen
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.
Teijin Pharma
From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.
TBA
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
TBA
Design, synthesis, and biological evaluation of novel disubstituted dibenzosuberones as highly potent and selective inhibitors of p38 mitogen activated protein kinase.
Eberhard-Karls University
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.
Takeda Pharmaceutical
Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-ß type 1 receptor kinase inhibitors.
Ewha Womans University
Modulation of cofilin phosphorylation by inhibition of the Lim family kinases.
Bristol-Myers Squibb Research and Development
Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.
Korea University
Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.
University of Washington
Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.
Astrazeneca
Design and synthesis of novel p38a MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety.
Toray Industries
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors.
University of Gothenburg
The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38a MAP kinase inhibitor for the treatment of inflammatory diseases.
Astrazeneca
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Amgen
Indolin-2-one p38a inhibitors I: design, profiling and crystallographic binding mode.
RhôNe-Poulenc Rorer
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
Pfizer
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site.
K£Mia
Through the"gatekeeper door": exploiting the active kinase conformation.
Nerviano Medical Sciences
Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.
Pfizer
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
King'S College London
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
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.
Wyeth Research
Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection.
Tulane University School of Medicine
Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.
Eberhard Karls University Tuebingen
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.
Bristol-Myers Squibb
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.
Bristol-Myers Squibb Research and Development
Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors.
Merck Research Laboratories
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.
K£Mia
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.
University of Zurich
Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties.
Eli Lilly
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).
Takeda Pharmaceutical
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.
Amgen
Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors.
Eberhard-Karls-Universit£T
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Astrazeneca
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.
Serono Pharmaceutical Research Institute
Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.
Leo Pharma
SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.
Novartis Institutes For Biomedical Research
Structure-based virtual screening approach to the discovery of p38 MAP kinase inhibitors.
Sejong University
Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.
Amgen
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.
Celgene
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Ludwig-Maximilians University of Munich
Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38a.
Chemical Genomics Centre of The Max Planck Society
Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.
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 novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.
Takeda Pharmaceutical
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
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.
Novartis Institute For Biomedical Research
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Elan Pharmaceuticals
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.
The Institute of Cancer Research
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.
Bristol-Myers Squibb
Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.
Pfizer
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.
Pfizer
Molecular modeling studies of phenoxypyrimidinyl imidazoles as p38 kinase inhibitors using QSAR and docking.
University College of Pharmaceutical Sciences
3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.
Roche Palo Alto
Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.
Korea Institute of Science and Technology
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
Chiral sulfoxides as metabolites of 2-thioimidazole-based p38a mitogen-activated protein kinase inhibitors: enantioselective synthesis and biological evaluation.
Eberhard-Karls-University Tu£Bingen
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors
Roche Palo Alto
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Millennium Pharmaceuticals
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Elan Pharmaceuticals
Catechin derivatives from Parapiptadenia rigida with in vitro wound-healing properties.
Albert-Ludwigs-University of Freiburg
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.
Elan Pharmaceuticals
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Elan Pharmaceuticals
5-amino-pyrazoles as potent and selective p38a inhibitors.
Bristol-Myers Squibb Research and Development
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.
Martin-Luther-University Halle-Wittenberg
Identification of potent ITK inhibitors through focused compound library design including structural information.
Nycomed
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
Pfizer
Tri- and tetrasubstituted imidazoles as p38a mitogen-activated protein kinase inhibitors.
Eberhard-Karls University of TüBingen
5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidines as novel class of potent and highly selective CaMKII inhibitors.
Dainippon Sumitomo Pharma
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region.
Deciphera Pharmaceuticals
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
Nerviano Medical Sciences Oncology
Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38a MAP kinase inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Biochemical and biophysical characterization of unique switch pocket inhibitors of p38a.
Abbott Laboratories
Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38a MAP kinase inhibitor for the treatment of inflammatory diseases.
Bristol-Myers Squibb Research and Development
Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors.
Amgen
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Amgen
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Rational design of inhibitors that bind to inactive kinase conformations.
Novartis Research Foundation
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
University of Dundee
Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.
Daiichi Sankyo
X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.
Roche Palo Alto
The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.
The University of Arizona
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.
Daiichi Sankyo
Unexpected reaction of 2-alkylsulfanylimidazoles to imidazol-2-ones: pyridinylimidazol-2-ones as novel potent p38alpha mitogen-activated protein kinase inhibitors.
Eberhard Karls University of Tubingen
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.
Cyclacel
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
Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors.
Merck Research Laboratories
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.
Wyeth Research
Amide-based inhibitors of p38alpha MAP kinase. Part 2: design, synthesis and SAR of potent N-pyrimidyl amides.
Scios
Amide-based inhibitors of p38alpha MAP kinase. Part 1: discovery of novel N-pyridyl amide lead molecules.
Scios
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.
Wyeth Research
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
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).
Wyeth Research
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
Roche Palo Alto
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
Wyeth Research
Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Wyeth Research
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.
Wyeth Research
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
Novartis Institutes For Biomedical Research
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.
Institute For Medical Research
Piperidine-based heterocyclic oxalyl amides as potent p38alpha MAP kinase inhibitors.
Scios
Application of a novel [3+2] cycloaddition reaction to prepare substituted imidazoles and their use in the design of potent DFG-out allosteric B-Raf inhibitors.
The University of Arizona
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.
The Institute of Cancer Research
Design and synthesis of piperazine-indole p38alpha MAP kinase inhibitors with improved pharmacokinetic profiles.
Scios
Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition.
Pfizer
Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38 alpha mitogen-activated protein kinase inhibitors.
Eberhard-Karls-University of T£Bingen
Displacement assay for the detection of stabilizers of inactive kinase conformations.
Chemical Genomics Centre of The Max Planck Society
Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.
Memorial Sloan-Kettering Cancer Center
Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles.
The University of Texas At Austin
3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta.
Eberhard-Karls University
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.
Takeda Pharmaceutical
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.
Vertex Pharmaceuticals
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.
Vertex Pharmaceuticals
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Wyeth Research
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.
Boehringer Ingelheim Pharmaceuticals
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
Pfizer
Role of the hydrogen bonding heteroatom-Lys53 interaction between the p38alpha mitogen-activated protein (MAP) kinase and pyridinyl-substituted 5-membered heterocyclic ring inhibitors.
Islamic University of Gaza
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.
Glaxosmithkline
Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors.
Institute For Medical Research
Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors: design, synthesis, and biological data of inhibitors with improved physicochemical properties.
Eberhard-Karls-UniversitäT
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Glaxosmithkline
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.
Astrazeneca R&D Boston
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.
Glaxosmithkline
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.
Amgen
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
Targeting the ribose and phosphate binding site of p38 mitogen-activated protein (MAP) kinase: synthesis and biological testing of 2-alkylsulfanyl-, 4(5)-aryl-, 5(4)-heteroaryl-substituted imidazoles.
Eberhard-Karls University of TüBingen
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.
Amgen
Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.
Piramal Life Sciences
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.
Glaxosmithkline
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.
Wyeth Research
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Glaxosmithkline
Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase.
Ewha Womans University
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.
Amgen
Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.
Cardiff University
Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.
Merck Research Laboratories
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.
Wyeth Research
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Bristol-Myers Squibb
Benzothiazole based inhibitors of p38alpha MAP kinase.
Bristol-Myers Squibb Research and Development
Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors.
Eberhard-Karls University
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.
Bristol-Myers Squibb Pharmaceutical Research Institute
The structure-based optimization of 3-substituted indolin-2-one derivatives as potent and isoform-selective c-Jun N-terminal kinase 3 (JNK3) inhibitors and biological evaluation.
Peking University
Novel 1,4,5,6-tetrahydrocyclopenta[d]imidazole-5-carboxamide-based JNK3 inhibitors: Design, synthesis, molecular docking, and therapeutic potential in neurodegenerative diseases.
Hanyang University
Discovery of novel imidazole chemotypes as isoform-selective JNK3 inhibitors for the treatment of Alzheimer's disease.
Hanyang University
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Pfizer
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Glaxosmithkline
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Amgen
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
Biocon-Bristol Myers Squibb Research and Development Center
From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors.
Eberhard-Karls-University TüBingen
Structure-Based Optimization of Selective and Brain Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions.
Janssen Research and Development
Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1.
Stanford University
Benzophenone: a ubiquitous scaffold in medicinal chemistry.
National Institute of Pharmaceutical Education and Research
Design, synthesis, broad-spectrum antiproliferative activity, and kinase inhibitory effect of triarylpyrazole derivatives possessing arylamides or arylureas moieties.
Korea Institute of Science and Technology
Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective.
University of Modena and Reggio Emilia
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Bristol-Myers Squibb Research & Development
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-
Biocon-Bristol Myers Squibb Research and Development Center
Progress in the development of domain selective inhibitors of the bromo and extra terminal domain family (BET) proteins.
China Pharmaceutical University
Inhibitors of unactivated p38 MAP kinase.
Johnson and Johnson Pharmaceutical Research and Development
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
The Emerging Landscape of Small-Molecule Therapeutics for the Treatment of Huntington's Disease.
Aligarh Muslim University
Design, Synthesis, and Biological Characterization of Inhaled p38α/β MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases.
Chiesi Farmaceutici
High-Throughput Screening Platform in Postnatal Heart Cells and Chemical Probe Toolbox to Assess Cardiomyocyte Proliferation.
Christian-Albrechts University of Kiel
Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3.
Astrazeneca R&D SöDertäLje
Unraveling the Design and Discovery of c-Jun N-Terminal Kinase Inhibitors and Their Therapeutic Potential in Human Diseases.
National Clinical Research Center For Geriatrics
Fast small molecule similarity searching with multiple alignment profiles of molecules represented in one-dimension.
Pharmacopeia
Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.
Novartis Institutes For Biomedical Research
p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones.
Merck
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.
Abbott Laboratories
Two classes of p38alpha MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes.
Locus Pharmaceuticals
Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.
Takeda Pharmaceutical
The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold.
University College London
Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3.
Astrazeneca R&D SöDertäLje
New dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Bristol-Myers Squibb Pharmaceutical Research Institute
The molecular basis for coxib inhibition of p38alpha MAP kinase.
Universidade Federal Do Rio De Janeiro (Ufrj)
Rapid computational identification of the targets of protein kinase inhibitors.
University of Iowa
A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia.
Newcastle University
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
Procter and Gamble Pharmaceuticals
Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.
Eli Lilly
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position.
Eberhard-Karls-University TüBingen
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Bristol-Myers Squibb
Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.
Johann Wolfgang Goethe University
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.
Astrazeneca
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.
Astrazeneca
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.
University of Minnesota
Design and Synthesis of Highly Selective Brain Penetrant p38α Mitogen-Activated Protein Kinase Inhibitors.
Eberhard Karls Universit£T T£Bingen
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors.
Procter and Gamble Pharmaceuticals
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
Novartis Institutes For Biomedical Research
Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines.
Eli Lilly
Improved potency of pyridin-2(1H)one derivatives for the treatment of mechanical allodynia.
University of Clermont Auvergne
Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.
Glaxosmithkline
Discovery of novel 2,3,5-trisubstituted pyridine analogs as potent inhibitors of IL-1β via modulation of the p38 MAPK signaling pathway.
Allinky Biopharma
-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors.
Reaction Biology
Rapid Evaluation of Small Molecule Cellular Target Engagement with a Luminescent Thermal Shift Assay.
Merck
A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors.
Novartis Institute For Biomedical Research
Developments of small molecules as inhibitors for carbonic anhydrase isoforms.
Georgia State University
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
Identification of an allosteric and Smad3-selective inhibitor of p38αMAPK using a substrate-based approach.
Carna Biosciences
The kinetics of binding to p38MAP kinase by analogues of BIRB 796.
Boehringer Ingelheim Pharmaceuticals
Indole-based heterocyclic inhibitors of p38alpha MAP kinase: designing a conformationally restricted analogue.
Scios
Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors.
China Pharmaceutical University
From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.
Sichuan University
Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors.
Yanbian University
Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF
Korea Institute of Science & Technology (Kist)
N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors.
Glaxosmithkline
Imidazopyrimidines, potent inhibitors of p38 MAP kinase.
Johnson & Johnson Pharmaceutical Research and Development
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.
Merck Research Laboratories
The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors.
Astrazeneca
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
Merck Research Laboratories
Advances in the Development of Phosphodiesterase-4 Inhibitors.
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors.
Reaction Biology
Imidazole inhibitors of cytokine release: probing substituents in the 2 position.
Eberhard-Karls-University TüBingen
Selective targeting of the αC and DFG-out pocket in p38 MAPK.
Johann Wolfgang Goethe University
Pyridin-2(1H)one derivatives: A possible new class of therapeutics for mechanical allodynia.
University of Clermont Auvergne
SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors.
Novartis Pharma
Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.
Bayer Research Center
Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38α/MAPK14 inhibitor.
University of Science & Technology (Ust)
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
China Pharmaceutical University
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Bayer
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.
Glaxosmithkline
Phenoxypyrimidine inhibitors of p38alpha kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles.
Glaxosmithkline
Mining the PDB for Tractable Cases Where X-ray Crystallography Combined with Fragment Screens Can Be Used to Systematically Design Protein-Protein Inhibitors: Two Test Cases Illustrated by IL1β-IL1R and p38α-TAB1 Complexes.
King'S College London
Bioisosteric Replacement of Arylamide-Linked Spine Residues with
Federal University of Rio De Janeiro (Ufrj)
Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5.
Yanbian University
p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas.
Bayer Research Center
Kinase-Inhibitory Nucleoside Derivatives from the Pacific Bryozoan
Victoria University of Wellington
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.
Glaxosmithkline R&D
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.
Bayer Research Center
Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors.
Yanbian University
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.
Novartis Pharma
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.
Japan Tobacco
Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.
Shanghai Jiao-Tong University School of Medicine
Kinase Atlas: Druggability Analysis of Potential Allosteric Sites in Kinases.
University of California
Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors.
Eberhard Karls Universit£T T£Bingen
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach.
Glaxosmithkline R&D
Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors.
University of Minnesota Twin Cities
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.
Newcastle University
Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives.
Yanbian University
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.
University of Naples Federico Ii
Discovery of potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation.
University of Perugia
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.
University of Florida
Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.
Eppley Institute For Research In Cancer and Allied Diseases
Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors.
Johann Wolfgang Goethe-University
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.
Cresset
Discovery of a potent p38α/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies.
University of Sharjah
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
University of Minnesota
Pyridinylimidazoles as GSK3β Inhibitors: The Impact of Tautomerism on Compound Activity via Water Networks.
Eberhard Karls Universit£T T£Bingen
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
Novartis Institutes For Biomedical Research
Syntheses and structure-activity relationships for some triazolyl p38α MAPK inhibitors.
Syncom
KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space.
Vu University Amsterdam
Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood.
Eberhard-Karls-University T£Bingen
The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.
Bristol-Myers Squibb Pharmaceutical Research Institute
Tri-substituted imidazole analogues of SB203580 as inducers for cardiomyogenesis of human embryonic stem cells.
Institute of Chemical and Engineering Sciences
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.
Northwestern University
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.
Universitaire Vaudois
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF
Nanjing University
Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.
Bristol-Myers Squibb Research and Development
Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis.
Montclair State University
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.
Takeda Pharmaceutical
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
Glaxosmithkline
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.
Korea Institute of Science & Technology (Kist)
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping.
Eberhard Karls Universit£T T£Bingen
Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases.
C-A-I-R Biosciences
In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.
National Institute of Biological Sciences, Beijing
Design, Synthesis, and Biological Evaluation of Novel Type I
Eberhard-Karls-Universitaet Tuebingen
Protacs targeting coronavirus 3CL protease and preparation method and application thereof
Shaanxi Panlong Pharmaceutical
Heterocyclic compound as Syk inhibitor and/or Syk-HDAC dual inhibitor
Hangzhou Innogate Pharma
Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CL
Cleveland Clinic
Thienopyrazine carboxamides as ubiquitin-specific protease inhibitors
Valo Early Discovery
Methods of treatment using pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds
Array Biopharma
1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
Angelini Acraf
Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors
Array Biopharma
Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Fused bicylic pyridine compounds and their use as AMPA receptor modulators
Janssen Pharmaceutica
Benzofurans substituted with secondary benzamide as HCV inhibitors
Bristol-Myers Squibb
Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
Boehringer Ingelheim International
Selective CYP11B1 inhibitors for the treatment of cortisol dependent diseases
Universitaet Des Saarlandes Campus Saarbruecken
Proline sulfonamide derivatives as orexin receptor antagonists
Actelion Pharmaceuticals
Multifunctional radical quenchers and their uses
Arizona Board of Regents, A Body Corporate of The State of Arizona Acting For and On Behalf of Arizona State University
Structure-based design and solid-phase parallel synthesis of phosphorylated nonpeptides to explore hydrophobic binding at the Src SH2 domain.
Ariad Pharmaceuticals
26- and 27-Methyl groups of 2-substituted, 19-nor-1a,25-dihydroxylated vitamin D compounds are essential for calcium mobilization in vivo.
University of Wisconsin-Madison
Steady-state kinetic mechanism of Ras farnesyl:protein transferase.
Merck Research Laboratories
Reaction of the molybdenum- and copper-containing carbon monoxide dehydrogenase from Oligotropha carboxydovorans with quinones.
University of California Riverside
The first selective agonist for the neuropeptide YY5 receptor increases food intake in rats.
Federal Institute of Technology of Zurich
N-(3-lodoprop-2E-enyl)-2beta-carbomethoxy-3beta-(3',4'-dichloro phenyl)nortropane (beta-CDIT), a tropane derivative: pharmacological characterization as a specific ligand for the dopamine transporter in the rodent brain.
University of Tours
Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes.
Warner-Lambert/Parke-Davis Pharmaceutical Research
Displacement of DL-[3H]-2-amino-4-phosphonobutanoic acid ( [3H]APB) binding with methyl-substituted APB analogues and glutamate agonists.
University of Minnesota
Characterization and autoradiographic localization of multiple tachykinin binding sites in gastrointestinal tract and bladder.
National Institutes of Health
Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties.
Novo Nordisk
Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.
Consiglio Nazionale Delle Ricerche
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).
Amgen
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.
Incyte
The structural basis for the selectivity of benzotriazole inhibitors of PTP1B.
Merck Research Laboratories
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
F. Hoffmann-La Roche
A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
Griffith University
Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: synthesis and biological evaluation.
Cardiff University
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.
Technische Universitat Braunschweig
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.
Avenida De La Industria
Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases.
University of Auckland
8-Anilinoimidazo[4,5-g]quinoline-7-carbonitriles as Src kinase inhibitors.
Wyeth-Ayerst Research
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2.
University of Newcastle
Stereospecific synthesis of a GS 4104 metabolite: determination of absolute stereochemistry and influenza neuraminidase inhibitory activity.
Gilead Sciences