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84 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
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
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
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
Structure-based de novo design and synthesis of aminothiazole-based p38 MAP kinase inhibitors.EBI
Sejong University
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
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
Novel triazolopyridylbenzamides as potent and selective p38a inhibitors.EBI
RhôNe-Poulenc Rorer
Discovery of a novel series of 4-quinolone JNK inhibitors.EBI
Roche Palo Alto
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor.EBI
Astellas Pharma
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.EBI
Janssen Pharmaceutical Companies Of Johnson & Johnson
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI
TBA
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI
Pfizer
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI
Bristol-Myers Squibb Research And Development
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
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
Kinase inhibitors: not just for kinases anymore.EBI
Northwestern University
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
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
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI
RhôNe-Poulenc Rorer
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.EBI
Bristol-Myers Squibb
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.EBI
Daiichi Sankyo
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.EBI
Abbott Laboratories
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
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
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
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI
Pfizer
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
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
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI
Abbott Bioresearch Center
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
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
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
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
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI
Boehringer Ingelheim Pharmaceuticals
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
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI
Merck Research Laboratories
Substituted imidazoles as glucagon receptor antagonists.EBI
Merck Research Laboratories
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Merck
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
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.EBI
Novartis Pharma
Chemical Space of DNA-Encoded Libraries.EBI
University Of Utah
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
Discovery of 4EBI
TBA
Pyrroles and other heterocycles as inhibitors of p38 kinase.EBI
Merck Research Laboratory
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
Why Some Targets Benefit from beyond Rule of Five Drugs.EBI
Boston University
Synthesis and molecular docking studies of new furochromone derivatives as p38? MAPK inhibitors targeting human breast cancer MCF-7 cells.EBI
Cairo University
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI
Abbvie Bioresearch Center
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
The identification of novel p38? isoform selective kinase inhibitors having an unprecedented p38? binding mode.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
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
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.EBI
Sichuan University/Collaborative Innovation Center Of Biotherapy
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
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.EBI
Novartis Institutes For Biomedical Research
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