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344 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28140585 52 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.EBI High Magnetic Field Laboratory
28109791 44 Identification of a selective inhibitor of transforming growth factor▀-activated kinase 1 by biosensor-based screening of focused libraries.EBI Chugai Pharmaceutical Co., Ltd.
28039836 41 Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with inávitro and inávivo antitumor activities.EBI East China Normal University
27977190 42 Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3.EBI Eberhard Karls Universit£t T£bingen
12565952 26 p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.EBI Merck& Co.
12482438 50 p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.EBI Merck Research Laboratories
9873730 27 Potent inhibitors of the MAP kinase p38.EBI R. W. Johnson Pharmaceutical Research Institute
9873686 18 Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.EBI SmithKline Beecham Pharmaceuticals
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University of Sydney
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
27746002 2 Phenylindenone isomers as divergent modulators of p38a MAP kinase.EBI Universit£ degli Studi di Siena
27109867 48 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.EBI GlaxoSmithKline
27288183 130 Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI Southeast University
27003761 120 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.EBI Nerviano Medical Sciences Srl
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 Company, Ltd
26951753 336 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for BioMedical Research
26800309 90 Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma.EBI Sygnature Discovery Limited
26789553 10 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.EBI High Magnetic Field Laboratory
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
26704264 10 Fragment-based drug discovery of potent and selective MKK3/6 inhibitors.EBI Takeda California Inc.
26483198 30 Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-▀ type I receptor kinase.EBI Ewha Womans University
26259807 21 Structure-based de novo design and synthesis of aminothiazole-based p38 MAP kinase inhibitors.EBI Sejong University
26222319 192 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.EBI Nerviano Medical Sciences Srl
25475894 68 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.EBI Eberhard Karls Universit£t T£bingen
25965804 80 Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.EBI Eli Lilly and Company
25893042 65 Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.EBI Translational Research Institute
25778995 63 Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38aMAPK and ERK1/2 inhibitory activity.EBI Cairo University
25415535 118 Inhibitors of c-Jun N-terminal kinases: an update.EBI Eberhard Karls Universit£t T£bingen
25369539 116 SAR156497, an exquisitely selective inhibitor of aurora kinases.EBI Sanofi
25255283 88 Discovery and characterization of MAPK-activated protein kinase-2 prevention of activation inhibitors.EBI AstraZeneca
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
24938496 32 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.EBI ASKA Pharmaceutical Co., Ltd
24930833 136 Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.EBI Syncom B.V.
24913411 13 Elements and modulation of functional dynamics.EBI Janssen Pharmaceutical Research and Development, LLC
24878193 8 Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors.EBI Hanyang University
25393557 83 Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.EBI Translational Research Institute
25369270 93 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI Galapagos NV
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24786585 200 Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-▀ type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.EBI Ewha Womans University
24704197 32 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-▀ type I receptor kinase.EBI Ewha Womans University
24332090 6 Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents.EBI Zhejiang Academy of Medical Sciences
23490150 48 Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI Takeda Pharmaceutical Co., Ltd
23434140 35 Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.EBI East China University of Science and Technology
23550937 72 Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.EBI Emory University
23416002 126 Amino acid derived quinazolines as Rock/PKA inhibitors.EBI Translational Research Institute
23414845 44 Structure-based discovery of cellular-active allosteric inhibitors of FAK.EBI Takeda Pharmaceutical Company Ltd
23442188 4 A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.EBI Graduate School of Peking Union Medical College and Chinese Academy of Medical Sciences
23441572 55 Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform.EBI Cyclofluidic Ltd
23270382 100 Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity.EBI University of T£bingen
19772287 67 p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.EBI GlaxoSmithKline
19303774 87 1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI GlaxoSmithKline R&D
17194588 92 N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI GlaxoSmithKline R&D
16632356 22 Development of N-2,4-pyrimidine-N-phenyl-N'-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-alpha) synthesis. Part 1.EBI Procter and Gamble Pharmaceuticals
23147077 23 Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.EBI Takeda Pharmaceutical Company Limited
22883026 34 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.EBI Takeda Pharmaceutical Company Limited
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 Ltd
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
22951114 16 A frozen analogue approach to aminopyridinylimidazoles leading to novel and promising p38 MAP kinase inhibitors.EBI University of Tuebingen
22897496 69 Targeting the hinge glycine flip and the activation loop: novel approach to potent p38a inhibitors.EBI Eberhard-Karls-University T£bingen
22746295 91 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.EBI Teijin Pharma Ltd.
23002419 30 From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.EBI TBA
24900538 27 Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.EBI TBA
22676210 116 Design, synthesis, and biological evaluation of novel disubstituted dibenzosuberones as highly potent and selective inhibitors of p38 mitogen activated protein kinase.EBI Eberhard-Karls-University
22980219 55 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.EBI Takeda Pharmaceutical Co. Ltd
23047226 72 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.EBI Ewha Womans University
22902653 99 Modulation of cofilin phosphorylation by inhibition of the Lim family kinases.EBI Bristol-Myers Squibb Research and Development
22858099 52 Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.EBI Korea University
22320388 116 Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.EBI University of Washington
22704236 64 Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.EBI AstraZeneca
22749282 12 Design and synthesis of novel p38a MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety.EBI Toray Industries, Inc.
22439974 79 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.EBI Takeda Pharmaceutical Company Limited
21905739 9 Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors.EBI University of Gothenburg
22608965 186 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.EBI AstraZeneca
22320327 250 Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI Amgen Inc.
24900264 106 The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.EBI TBA
21696951 21 Indolin-2-one p38a inhibitors I: design, profiling and crystallographic binding mode.EBI Rhône-Poulenc Rorer
21641211 14 Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.EBI Pfizer Inc.
20684563 176 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.EBI H. Lundbeck A/S
15975507 13 Features of selective kinase inhibitors.EBI University of California-San Francisco
20663667 31 Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site.EBI K£mia, Inc.
20000735 12 Through the"gatekeeper door": exploiting the active kinase conformation.EBI Nerviano Medical Sciences
19751974 81 Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.EBI Pfizer Corporation
20188577 23 In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.EBI King's College London
20153204 109 Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.EBI Nerviano Medical Sciences Srl
20038108 19 Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.EBI Wyeth Research
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
17923491 5 Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection.EBI Tulane University School of Medicine
14593182 34 Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI Pfizer Global Researchand Development
18789685 172 Kinase array design, back to front: biaryl amides.EBI GlaxoSmithKline R&D
18578517 93 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.EBI Eberhard-Karls-University Tuebingen
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
18373337 20 Isoxazolone based inhibitors of p38 MAP kinases.EBI Eberhard Karls University of Tuebingen
18364256 33 Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.EBI Bristol-Myers Squibb
18359226 50 Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI Bristol-Myers Squibb Research and Development
18316187 29 Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors.EBI Merck Research Laboratories
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18325768 12 The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.EBI K£mia, Inc.
18278858 93 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.EBI Amgen Inc.
18271520 423 Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.EBI University of Zurich
18039577 62 Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties.EBI Eli Lilly and Co.
18313304 50 Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).EBI Takeda Pharmaceutical Company, Ltd
18083554 54 N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.EBI Amgen Inc.
17181176 17 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.EBI Eberhard-Karls-Universit£t
16876403 85 Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
16570917 32 Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.EBI GlaxoSmithKline
16451062 46 Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.EBI Centre de Recherches
15999997 85 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.EBI Serono Pharmaceutical Research Institute
12672248 50 Kinase inhibitors: not just for kinases anymore.EBI Northwestern University
14667219 24 Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.EBI LEO Pharma
12166950 208 Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI Millennium Pharmaceuticals, Inc.
11844702 14 Pyridazine based inhibitors of p38 MAPK.EBI Merck Research Laboratories
11591521 39 Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach.EBI Bayer Research Center
22342625 6 Structure-based virtual screening approach to the discovery of p38 MAP kinase inhibitors.EBI Sejong University
22244937 44 Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.EBI Celgene Corporation
22168824 4 Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.EBI Amgen Inc.
22226655 88 Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.EBI Celgene Corporation
22196117 48 Identification of triazolopyridazinones as potent p38a inhibitors.EBI Amgen Inc.
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
22154891 19 Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38a.EBI Chemical Genomics Centre of the Max Planck Society
21888439 7 Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.EBI Pfizer Inc.
22154349 123 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.EBI Nerviano Medical Sciences srl
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
22003817 71 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.EBI Takeda Pharmaceutical Company Limited
22014755 36 Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI Hanyang University
21999461 90 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI Rhône-Poulenc Rorer
21958544 31 Indolin-2-one p38a inhibitors III: bioisosteric amide replacement.EBI Rhône-Poulenc Rorer
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
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
21813278 95 Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.EBI Elan Pharmaceuticals
21813275 40 Indolin-2-one p38a inhibitors II: Lead optimisation.EBI Rhône-Poulenc Rorer
21696866 36 Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-ß type 1 receptor kinase inhibitors.EBI Ewha Womans University
21699136 16 Selectivity of kinase inhibitor fragments.EBI GlaxoSmithKline R&D
21536449 16 Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.EBI Institute of Cancer Research
21705217 60 Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.EBI Bristol-Myers Squibb
21640588 31 Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.EBI Pfizer Inc.
21620699 51 Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI Pfizer Inc.
17706839 44 Molecular modeling studies of phenoxypyrimidinyl imidazoles as p38 kinase inhibitors using QSAR and docking.EBI University College of Pharmaceutical Sciences
21515047 24 3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.EBI Roche Palo Alto
21489792 26 Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.EBI Korea Institute of Science and Technology
21470862 110 NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.EBI Nerviano Medical Sciences srl
21449619 86 Chiral sulfoxides as metabolites of 2-thioimidazole-based p38a mitogen-activated protein kinase inhibitors: enantioselective synthesis and biological evaluation.EBI Eberhard-Karls-University Tu£bingen
21435890 38 Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.EBI Ewha Womans University
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 (Europe) Ltd.
21375264 77 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 inhibitorsEBI Roche Palo Alto LLC
21341678 49 Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.EBI Millennium Pharmaceuticals, Inc.
21316234 133 Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.EBI Elan Pharmaceuticals, Inc.
21080642 4 Catechin derivatives from Parapiptadenia rigida with in vitro wound-healing properties.EBI Albert-Ludwigs-Universita£t
24900250 81 Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI TBA
21112785 151 Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.EBI Elan Pharmaceuticals
21071223 190 Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.EBI Elan Pharmaceuticals
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
21035334 55 Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.EBI Martin Luther University Halle-Wittenberg
20965724 57 Identification of potent ITK inhibitors through focused compound library design including structural information.EBI Nycomed GmbH
20961062 42 Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.EBI Pfizer Inc.
20934337 59 Tri- and tetrasubstituted imidazoles as p38a mitogen-activated protein kinase inhibitors.EBI Eberhard Karls University of Tübingen
20875738 9 5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidines as novel class of potent and highly selective CaMKII inhibitors.EBI Dainippon Sumitomo Pharma Co., Ltd
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences Srl
20800479 33 Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region.EBI Deciphera Pharmaceuticals LLC
20817473 57 Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI Nerviano Medical Sciences-Oncology
20732813 33 Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38a MAP kinase inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
20471255 34 Biochemical and biophysical characterization of unique switch pocket inhibitors of p38a.EBI Abbott Laboratories
20804198 29 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.EBI Bristol-Myers Squibb Research and Development
20712346 23 Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors.EBI Amgen Inc.
20684549 76 Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI Amgen Inc.
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
16783341 34 Rational design of inhibitors that bind to inactive kinase conformations.EBI Novartis Research Foundation
10998351 24 Specificity and mechanism of action of some commonly used protein kinase inhibitors.EBI University of Dundee
20675134 88 Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.EBI Daiichi Sankyo Co., Ltd
20655210 3 X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.EBI Roche Palo Alto
20621496 31 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.EBI The University of Arizona
20637613 4 Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.EBI Daiichi Sankyo Co., Ltd
20620059 54 Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.EBI Pfizer Inc.
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20472445 23 Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.EBI Ewha Womans University
20462263 127 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI Cyclacel Ltd.
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19950901 23 Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.EBI Roche Palo Alto
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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
20060294 21 Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.EBI Novartis Institutes for BioMedical Research
20045647 35 Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.EBI Institute for Medical Research
20031411 8 Piperidine-based heterocyclic oxalyl amides as potent p38alpha MAP kinase inhibitors.EBI Scios, Inc
19962319 14 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.EBI The University of Arizona
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19822424 4 Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles.EBI The University of Texas at Austin
19591487 38 3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta.EBI Eberhard-Karls-University
19775160 79 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.EBI Takeda Pharmaceutical Company, Ltd.
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19414255 58 Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI Vertex Pharmaceuticals Inc
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19356929 17 Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.EBI Boehringer Ingelheim Pharmaceutical
19327989 40 Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI Pfizer Global R&D
19301816 6 Role of the hydrogen bonding heteroatom-Lys53 interaction between the p38alpha mitogen-activated protein (MAP) kinase and pyridinyl-substituted 5-membered heterocyclic ring inhibitors.EBI Islamic University of Gaza
19285393 90 Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI GlaxoSmithKline
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19253982 19 Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors: design, synthesis, and biological data of inhibitors with improved physicochemical properties.EBI Eberhard-Karls-Universität
19135364 38 2-Aminoimidazoles inhibitors of TGF-beta receptor 1.EBI Abbot Laboratories
19101143 70 Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).EBI GlaxoSmithKline
19097792 24 Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.EBI AstraZeneca R&D Boston
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18682324 33 Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.EBI Amgen, Inc.
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18602262 56 Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.EBI GlaxoSmithKline R&D
18571921 72 Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase.EBI Ewha Womans University
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18539026 5 Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.EBI Cardiff University
17855341 4 Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.EBI Merck Research Laboratories
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18296051 27 Benzothiazole based inhibitors of p38alpha MAP kinase.EBI Bristol-Myers Squibb Research and Development
18207396 10 Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors.EBI Eberhard-Karls-University
17664068 27 Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17570666 64 Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI Pfizer Global Research and Development
17552507 21 Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.EBI Ewha Womans University
17524641 69 3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI GlaxoSmithKline
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16516473 444 Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.EBI Centre de Recherches
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16111887 104 New dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15990304 4 The molecular basis for coxib inhibition of p38alpha MAP kinase.EBI Universidade Federal do Rio de Janeiro (UFRJ)
15943486 8 Rapid computational identification of the targets of protein kinase inhibitors.EBI University of Iowa
15837333 5 The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.EBI Procter and Gamble Pharmaceuticals
15801819 23 Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.EBI Eli Lilly and Co.
15711537 653 A small molecule-kinase interaction map for clinical kinase inhibitors.EBI Ambit Biosciences
15615512 21 Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15566301 36 Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position.EBI Eberhard-Karls-University Tübingen
15566298 34 The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.EBI Bristol-Myers Squibb
15454232 51 Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.EBI AstraZeneca
15454231 32 A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.EBI AstraZeneca
15341957 9 The development of new bicyclic pyrazole-based cytokine synthesis inhibitors.EBI Procter and Gamble Pharmaceuticals
15317463 16 Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15177480 42 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.EBI Lilly Research Laboratory
14640546 46 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 clinEBI Cephalon, Inc
14592495 60 Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).EBI Bristol-Myers Squibb Pharmaceutical Research Institute
14592489 71 SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.EBI Merck Research Laboratories
12954047 80 Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.EBI The Lilly Research Laboratories
12941343 49 The kinetics of binding to p38MAP kinase by analogues of BIRB 796.EBI Boehringer Ingelheim Pharmaceuticals
12941340 10 Indole-based heterocyclic inhibitors of p38alpha MAP kinase: designing a conformationally restricted analogue.EBI Scios Inc.
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
12643941 20 N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors.EBI GlaxoSmithKline Pharmaceuticals
12565927 24 Imidazopyrimidines, potent inhibitors of p38 MAP kinase.EBI Johnson & Johnson Pharmaceutical Research and Development
12540232 53 Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.EBI Merck Research Laboratories
12482439 51 Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.EBI Merck Research Laboratories
12361396 15 Imidazole inhibitors of cytokine release: probing substituents in the 2 position.EBI Eberhard-Karls-University Tübingen
12039561 30 Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.EBI Bayer Research Center
11934592 24 Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI Merck Research Laboratories
11597418 47 Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI GlaxoSmithKline Pharmaceuticals
11549467 85 Substituted imidazoles as glucagon receptor antagonists.EBI Merck Research Laboratories
11354358 53 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.EBI GlaxoSmithKline Pharmaceuticals
11140741 43 p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas.EBI Bayer Research Center
10999468 30 1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.EBI Bayer Research Center
10999467 19 Discovery of a new class of p38 kinase inhibitors.EBI Bayer Research Center
10201821 166 Potent, orally absorbed glucagon receptor antagonists.EBI Merck Research Laboratories
9873604 72 Pyrroles and other heterocycles as inhibitors of p38 kinase.EBI Merck Research Laboratory
22168802 12 Carbonic anhydrases inhibitory effects of new benzenesulfonamides synthesized by using superacid chemistry.BDB Laboratoire SynthŔse et RÚactivitÚ des Substances Naturelles
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21765407 30 Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.BDB National Cancer Institute-Frederick
13679167 34 Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands.BDB Universit&aagrove; di Milano
12921854 130 Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines.BDB Harvard University
11714898 21 Functional calcitonin gene-related peptide subtype 2 receptors in porcine coronary arteries are identified as calcitonin gene-related peptide subtype 1 receptors by radioligand binding and reverse transcription-polymerase chain reaction.BDB Creighton University
10087012 8 Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat human T lymphocyte cell line.BDB Medical College of Georgia
20028400 4 High throughput receptor-based virtual screening under ZINC database, synthesis, and biological evaluation of ketol-acid reductoisomerase inhibitors.BDB Nankai University
2885406 68 Pharmacological evidence for alpha-2 adrenoceptor heterogeneity: differential binding properties of [3H]rauwolscine and [3H]idazoxan in rat brain.BDB University of California
2877462 17 1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs.BDB The Oregon Health Sciences University
1321043 17 Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist.BDB Université Libre de Bruxelles
9383449 21 Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.BDB SmithKline Beecham Pharmaceuticals
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12704428 9 Insights into antifolate resistance from malarial DHFR-TS structures.BDB Mahidol University
16392822 87 2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.BDB National Health Research Institutes
8667360 46 Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins.BDB Hebrew University of Jerusalem