The first public molecular recognition database, BindingDB supports research, education and practice in drug discovery, pharmacology and related fields.

BindingDB contains 2.8M data for 1.2M Compounds and 9.2K Targets. Of those, 1,346K data for 622K Compounds and 4.5K Targets were curated by BindingDB curators. BindingDB is a FAIRsharing resource.

If BindingDB was of value to your research, please take a moment to donate to this nonprofit project. Your donation will let us provide you with more data and improved service.

Advanced Search

397 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.EBI
High Magnetic Field Laboratory
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.EBI
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.EBI
East China Normal University
Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3.EBI
Eberhard Karls Universit£T T£Bingen
p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.EBI
Merck
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
Potent inhibitors of the MAP kinase p38.EBI
R. W. Johnson Pharmaceutical Research Institute
Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.EBI
Smithkline Beecham Pharmaceuticals
Non-kinase targets of protein kinase inhibitors.EBI
The University Of Sydney
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Phenylindenone isomers as divergent modulators of p38a MAP kinase.EBI
Universit£
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
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI
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.EBI
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.EBI
Takeda Pharmaceutical
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI
Novartis Institutes For Biomedical Research
Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma.EBI
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.EBI
High Magnetic Field Laboratory
Fragment-based drug discovery of potent and selective MKK3/6 inhibitors.EBI
Takeda California
Structure-based de novo design and synthesis of aminothiazole-based p38 MAP kinase inhibitors.EBI
Sejong University
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
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
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
Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.EBI
Translational Research Institute
Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38aMAPK and ERK1/2 inhibitory activity.EBI
Cairo University
Inhibitors of c-Jun N-terminal kinases: an update.EBI
Eberhard Karls Universit£T T£Bingen
SAR156497, an exquisitely selective inhibitor of aurora kinases.EBI
Sanofi
Discovery and characterization of MAPK-activated protein kinase-2 prevention of activation inhibitors.EBI
Astrazeneca
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI
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.EBI
Aska Pharmaceutical
Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.EBI
Syncom
Elements and modulation of functional dynamics.EBI
Janssen Research And Development
Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors.EBI
Hanyang University
Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.EBI
Translational Research Institute
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI
Galapagos
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI
Nerviano Medical Sciences
Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents.EBI
Zhejiang Academy Of Medical Sciences
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI
Takeda Pharmaceutical
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
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.EBI
Emory University
Amino acid derived quinazolines as Rock/PKA inhibitors.EBI
Translational Research Institute
Structure-based discovery of cellular-active allosteric inhibitors of FAK.EBI
Takeda Pharmaceutical
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
Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform.EBI
Cyclofluidic
Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity.EBI
University Of T£Bingen
p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.EBI
Glaxosmithkline
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI
Glaxosmithkline
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI
Glaxosmithkline
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
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.EBI
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.EBI
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.EBI
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.EBI
Sichuan University
A frozen analogue approach to aminopyridinylimidazoles leading to novel and promising p38 MAP kinase inhibitors.EBI
University Of Tuebingen
Targeting the hinge glycine flip and the activation loop: novel approach to potent p38a inhibitors.EBI
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.EBI
Teijin Pharma
From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.EBI
TBA
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.EBI
TBA
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
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
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
Modulation of cofilin phosphorylation by inhibition of the Lim family kinases.EBI
Bristol-Myers Squibb Research And Development
Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.EBI
Korea University
Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.EBI
University Of Washington
Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.EBI
Astrazeneca
Design and synthesis of novel p38a MAP kinase inhibitors: discovery of pyrazole-benzyl ureas bearing 2-molpholinopyrimidine moiety.EBI
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.EBI
Takeda Pharmaceutical
Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors.EBI
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.EBI
Astrazeneca
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI
Amgen
The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.EBI
TBA
Indolin-2-one p38a inhibitors I: design, profiling and crystallographic binding mode.EBI
RhôNe-Poulenc Rorer
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.EBI
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.EBI
H. Lundbeck
Features of selective kinase inhibitors.EBI
University Of California San Francisco
Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site.EBI
K£Mia
Through the"gatekeeper door": exploiting the active kinase conformation.EBI
Nerviano Medical Sciences
Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.EBI
Pfizer
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.EBI
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.EBI
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.EBI
Wyeth Research
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
The selectivity of protein kinase inhibitors: a further update.EBI
University Of Dundee
Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection.EBI
Tulane University School Of Medicine
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI
Pfizer
Kinase array design, back to front: biaryl amides.EBI
Glaxosmithkline
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
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI
Harvard Medical School
Isoxazolone based inhibitors of p38 MAP kinases.EBI
Eberhard Karls University Of Tuebingen
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.EBI
Bristol-Myers Squibb
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI
Bristol-Myers Squibb Research And Development
Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors.EBI
Merck Research Laboratories
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.EBI
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.EBI
Amgen
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.EBI
University Of Zurich
Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties.EBI
Eli Lilly
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).EBI
Takeda Pharmaceutical
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.EBI
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.EBI
Eberhard-Karls-Universit£T
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
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.EBI
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.EBI
Serono Pharmaceutical Research Institute
Kinase inhibitors: not just for kinases anymore.EBI
Northwestern University
Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.EBI
Leo Pharma
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI
Millennium Pharmaceuticals
Pyridazine based inhibitors of p38 MAPK.EBI
Merck Research Laboratories
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
Structure-based virtual screening approach to the discovery of p38 MAP kinase inhibitors.EBI
Sejong University
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.EBI
Celgene
Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.EBI
Amgen
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.EBI
Celgene
Identification of triazolopyridazinones as potent p38a inhibitors.EBI
Amgen
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
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
Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.EBI
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.EBI
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).EBI
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.EBI
Takeda Pharmaceutical
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI
RhôNe-Poulenc Rorer
Indolin-2-one p38a inhibitors III: bioisosteric amide replacement.EBI
RhôNe-Poulenc Rorer
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
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
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.EBI
Elan Pharmaceuticals
Indolin-2-one p38a inhibitors II: Lead optimisation.EBI
RhôNe-Poulenc Rorer
Selectivity of kinase inhibitor fragments.EBI
Glaxosmithkline
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.EBI
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.EBI
Bristol-Myers Squibb
Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.EBI
Pfizer
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI
Pfizer
Molecular modeling studies of phenoxypyrimidinyl imidazoles as p38 kinase inhibitors using QSAR and docking.EBI
University College Of Pharmaceutical Sciences
3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead.EBI
Roche Palo Alto
Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.EBI
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.EBI
Nerviano Medical Sciences
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
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
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
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.EBI
Millennium Pharmaceuticals
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.EBI
Elan Pharmaceuticals
Catechin derivatives from Parapiptadenia rigida with in vitro wound-healing properties.EBI
Albert-Ludwigs-University Of Freiburg
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI
TBA
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.EBI
Elan Pharmaceuticals
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.EBI
Elan Pharmaceuticals
5-amino-pyrazoles as potent and selective p38a inhibitors.EBI
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.EBI
Martin-Luther-University Halle-Wittenberg
Identification of potent ITK inhibitors through focused compound library design including structural information.EBI
Nycomed
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.EBI
Pfizer
Tri- and tetrasubstituted imidazoles as p38a mitogen-activated protein kinase inhibitors.EBI
Eberhard-Karls University Of TüBingen
5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidines as novel class of potent and highly selective CaMKII inhibitors.EBI
Dainippon Sumitomo Pharma
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI
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.EBI
Deciphera Pharmaceuticals
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI
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.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Biochemical and biophysical characterization of unique switch pocket inhibitors of p38a.EBI
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.EBI
Bristol-Myers Squibb Research And Development
Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors.EBI
Amgen
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI
Amgen
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Rational design of inhibitors that bind to inactive kinase conformations.EBI
Novartis Research Foundation
Specificity and mechanism of action of some commonly used protein kinase inhibitors.EBI
University Of Dundee
Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.EBI
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.EBI
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.EBI
The University Of Arizona
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.EBI
Daiichi Sankyo
Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.EBI
Pfizer
Unexpected reaction of 2-alkylsulfanylimidazoles to imidazol-2-ones: pyridinylimidazol-2-ones as novel potent p38alpha mitogen-activated protein kinase inhibitors.EBI
Eberhard Karls University Of Tubingen
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI
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.EBI
Nerviano Medical Sciences
Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.EBI
Pfizer
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.EBI
Wyeth Research
Amide-based inhibitors of p38alpha MAP kinase. Part 2: design, synthesis and SAR of potent N-pyrimidyl amides.EBI
Scios
Amide-based inhibitors of p38alpha MAP kinase. Part 1: discovery of novel N-pyridyl amide lead molecules.EBI
Scios
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase.EBI
Pfizer
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.EBI
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.EBI
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).EBI
Wyeth Research
Small molecule JNK (c-Jun N-terminal kinase) inhibitors.EBI
Merck Research Laboratories
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.EBI
Roche Palo Alto
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI
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.EBI
Amgen
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.EBI
Wyeth Research
Discovery of highly potent and selective type I B-Raf kinase inhibitors.EBI
Wyeth Research
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.EBI
Wyeth Research
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.EBI
Novartis Institutes For Biomedical Research
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.EBI
Institute For Medical Research
Piperidine-based heterocyclic oxalyl amides as potent p38alpha MAP kinase inhibitors.EBI
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.EBI
The University Of Arizona
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.EBI
The Institute Of Cancer Research
Design and synthesis of piperazine-indole p38alpha MAP kinase inhibitors with improved pharmacokinetic profiles.EBI
Scios
Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition.EBI
Pfizer
Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38 alpha mitogen-activated protein kinase inhibitors.EBI
Eberhard-Karls-University Of T£Bingen
Displacement assay for the detection of stabilizers of inactive kinase conformations.EBI
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.EBI
Memorial Sloan-Kettering Cancer Center
Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles.EBI
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.EBI
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.EBI
Takeda Pharmaceutical
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI
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.EBI
Amgen
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI
Vertex Pharmaceuticals
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI
Wyeth Research
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.EBI
Boehringer Ingelheim Pharmaceuticals
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI
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.EBI
Islamic University Of Gaza
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI
Glaxosmithkline
Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors.EBI
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.EBI
Eberhard-Karls-UniversitäT
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).EBI
Glaxosmithkline
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.EBI
Astrazeneca R&D Boston
'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.EBI
Kemia
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.EBI
Glaxosmithkline
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.EBI
Amgen
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.EBI
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.EBI
Eberhard-Karls University Of TüBingen
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.EBI
Amgen
Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.EBI
Piramal Life Sciences
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.EBI
Glaxosmithkline
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI
Wyeth Research
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.EBI
Glaxosmithkline
Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase.EBI
Ewha Womans University
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.EBI
Amgen
Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.EBI
Cardiff University
Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.EBI
Merck Research Laboratories
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.EBI
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.EBI
Bristol-Myers Squibb
Benzothiazole based inhibitors of p38alpha MAP kinase.EBI
Bristol-Myers Squibb Research And Development
Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors.EBI
Eberhard-Karls University
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI
Pfizer
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI
Glaxosmithkline
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.EBI
Amgen
From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors.EBI
Eberhard-Karls-University TüBingen
Inhibitors of unactivated p38 MAP kinase.EBI
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.EBI
Amgen
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
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
Astrazeneca
Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3.EBI
Astrazeneca R&D SöDertäLje
Fast small molecule similarity searching with multiple alignment profiles of molecules represented in one-dimension.EBI
Pharmacopeia
p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones.EBI
Merck
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.EBI
Abbott Laboratories
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI
Abbott Bioresearch Center
Two classes of p38alpha MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes.EBI
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.EBI
Takeda Pharmaceutical
The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold.EBI
University College London
Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3.EBI
Astrazeneca R&D SöDertäLje
New dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
The molecular basis for coxib inhibition of p38alpha MAP kinase.EBI
Universidade Federal Do Rio De Janeiro (Ufrj)
Rapid computational identification of the targets of protein kinase inhibitors.EBI
University Of Iowa
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.EBI
Procter And Gamble Pharmaceuticals
Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.EBI
Eli Lilly
A small molecule-kinase interaction map for clinical kinase inhibitors.EBI
Ambit Biosciences
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
Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position.EBI
Eberhard-Karls-University TüBingen
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.EBI
Bristol-Myers Squibb
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.EBI
Astrazeneca
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.EBI
Astrazeneca
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors.EBI
Procter And Gamble Pharmaceuticals
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
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
Eli Lilly
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
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
SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.EBI
Merck Research Laboratories
The kinetics of binding to p38MAP kinase by analogues of BIRB 796.EBI
Boehringer Ingelheim Pharmaceuticals
Indole-based heterocyclic inhibitors of p38alpha MAP kinase: designing a conformationally restricted analogue.EBI
Scios
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI
Boehringer Ingelheim Pharmaceuticals
N-Phenyl-N-purin-6-yl ureas: the design and synthesis of p38alpha MAP kinase inhibitors.EBI
Glaxosmithkline
Imidazopyrimidines, potent inhibitors of p38 MAP kinase.EBI
Johnson & Johnson Pharmaceutical Research And Development
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.EBI
Merck Research Laboratories
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.EBI
Merck Research Laboratories
Imidazole inhibitors of cytokine release: probing substituents in the 2 position.EBI
Eberhard-Karls-University TüBingen
Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.EBI
Bayer Research Center
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI
Merck Research Laboratories
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI
Glaxosmithkline
Substituted imidazoles as glucagon receptor antagonists.EBI
Merck Research Laboratories
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
p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas.EBI
Bayer Research Center
Design and molecular modeling of novel P38? MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds.EBI
National Research Centre
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease.EBI
Glaxosmithkline R&D
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.EBI
Bayer Research Center
Discovery of a new class of p38 kinase inhibitors.EBI
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.EBI
Yanbian University
Chemical Space of DNA-Encoded Libraries.EBI
University Of Utah
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.EBI
Japan Tobacco
Progress in the development of more effective and safer analgesics for pain management.EBI
University Of Catania
Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.EBI
Shanghai Jiao-Tong University School Of Medicine
Kinase Atlas: Druggability Analysis of Potential Allosteric Sites in Kinases.EBI
University Of California
Pyridinylimidazoles as dual glycogen synthase kinase 3?/p38? mitogen-activated protein kinase inhibitors.EBI
Eberhard Karls Universit£T T£Bingen
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase ? through a Deconstruction and Regrowth Approach.EBI
Glaxosmithkline R&D
Potent, orally absorbed glucagon receptor antagonists.EBI
Merck Research Laboratories
Discovery of 4EBI
TBA
Pyrroles and other heterocycles as inhibitors of p38 kinase.EBI
Merck Research Laboratory
Systematically Mitigating the p38? Activity of Triazole-based BET Inhibitors.EBI
University Of Minnesota Twin Cities
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38? and BRD4.EBI
Newcastle University
Discovery of novel Bcr-AblEBI
Xi'An Jiaotong 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.EBI
Yanbian University
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.EBI
University Of Naples Federico Ii
Discovery of potent p38? MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation.EBI
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.EBI
University Of Florida
Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.EBI
Eppley Institute For Research In Cancer And Allied Diseases
Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors.EBI
Johann Wolfgang Goethe-University
Why Some Targets Benefit from beyond Rule of Five Drugs.EBI
Boston University
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.EBI
Cresset
Discovery of a potent p38?/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies.EBI
University Of Sharjah
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.EBI
University Of Minnesota
Pyridinylimidazoles as GSK3? Inhibitors: The Impact of Tautomerism on Compound Activity via Water Networks.EBI
Eberhard Karls Universit£T T£Bingen
Synthesis and molecular docking studies of new furochromone derivatives as p38? MAPK inhibitors targeting human breast cancer MCF-7 cells.EBI
Cairo University
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.EBI
Novartis Institutes For Biomedical Research
Syntheses and structure-activity relationships for some triazolyl p38? MAPK inhibitors.EBI
Syncom
KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space.EBI
Vu University Amsterdam
Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.EBI
The Scripps Research Institute
Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood.EBI
Eberhard-Karls-University T£Bingen
The identification of novel p38? isoform selective kinase inhibitors having an unprecedented p38? binding mode.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Tri-substituted imidazole analogues of SB203580 as inducers for cardiomyogenesis of human embryonic stem cells.EBI
Institute Of Chemical And Engineering Sciences
High-content single-cell drug screening with phosphospecific flow cytometry.EBI
Stanford University
Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry.EBI
Paradigm Therapeutics
Synthesis, biological testing, and binding mode prediction of 6,9-diarylpurin-8-ones as p38 MAP kinase inhibitors.EBI
Eberhard-Karls-University T£Bingen
p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold.EBI
Merck Research Laboratories
The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production.EBI
Procter And Gamble Pharmaceuticals
Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-alpha production.EBI
Procter And Gamble Pharmaceuticals
Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes.EBI
Eberhard-Karls-University T£Bingen
From imidazoles to pyrimidines: new inhibitors of cytokine release.EBI
Eberhard-Karls-University T£Bingen
An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors.EBI
Aventis Pharma
Are free energy calculations useful in practice? A comparison with rapid scoring functions for the p38 MAP kinase protein system.EBI
Vertex Pharmaceuticals
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.EBI
Universitaire Vaudois
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAFEBI
Nanjing University
Discovery of 4-Azaindole Inhibitors of TGF?RI as Immuno-oncology Agents.EBI
Bristol-Myers Squibb Research And Development
Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis.EBI
Montclair State University
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI
Vertex Pharmaceuticals
Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.EBI
Takeda Pharmaceutical
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.EBI
Glaxosmithkline
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.EBI
Novartis Institutes For Biomedical Research
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute Of Science And Technology (Kist)
Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer.EBI
University Of Zagreb
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.EBI
Eberhard Karls Universit£T T£Bingen
Drug Discovery Targeting Bromodomain-Containing Protein 4.EBI
University Of Texas Medical Branch
Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38? MAPK/PDE-4 Inhibitor with Activity against TNF?-Related Diseases.EBI
C-A-I-R Biosciences
In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.EBI
National Institute Of Biological Sciences, Beijing
Design, Synthesis, and Biological Evaluation of Novel Type IEBI
Eberhard-Karls-Universitaet Tuebingen
Carbonic anhydrases inhibitory effects of new benzenesulfonamides synthesized by using superacid chemistry.BDB
Laboratoire Synthese Et Reactivite Des Substances Naturelles
A Novel Approach to the Discovery of Small-Molecule Ligands of CDK2.BDB
Moffitt Cancer Center
Synthesis and SAR exploration of dinapsoline analogues.BDB
Bristol-Myers Squibb Pharmaceutical Research Institute
Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.BDB
National Cancer Institute-Frederick
Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands.BDB
Universit&Aagrove
Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines.BDB
Harvard University
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
Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat human T lymphocyte cell line.BDB
Medical College Of Georgia
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors.BDB
Eli Lilly
Development of new and selective Trypanosoma cruzi trans-sialidase inhibitors from sulfonamide chalcones and their derivatives.BDB
University Of British Columbia
High throughput receptor-based virtual screening under ZINC database, synthesis, and biological evaluation of ketol-acid reductoisomerase inhibitors.BDB
Nankai University
Pharmacological evidence for alpha-2 adrenoceptor heterogeneity: differential binding properties of [3H]rauwolscine and [3H]idazoxan in rat brain.BDB
University Of California
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
Synthesis and molecular modelling of novel substituted-4,5-dihydro-(1H)-pyrazole derivatives as potent and highly selective monoamine oxidase-A inhibitors.BDB
UniversitÀ
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
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
 
Cyclodextrin Inclusion Complexes: Studies of the Variation in the Size of Alicyclic GuestsBDB
University Of Mississippi
Insights into antifolate resistance from malarial DHFR-TS structures.BDB
Mahidol University
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