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119 articles for thisTarget


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

PMID
Data
Article Title
Organization
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
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
Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.EBI
Novartis Institutes For Biomedical Research
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
Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications.EBI
Merck Research Laboratories
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.EBI
Merck Research Laboratories
Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4.EBI
Merck Research Laboratories
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI
Astrazeneca
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI
Astellas Pharma
Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.EBI
Merck
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.EBI
Merck Research Laboratories
Discovery and hit-to-lead optimization of 2,6-diaminopyrimidine inhibitors of interleukin-1 receptor-associated kinase 4.EBI
Merck Research Laboratories
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.EBI
Vertex Pharmaceuticals
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.EBI
Merck Research Laboratories
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.EBI
Lexicon Pharmaceuticals
Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders.EBI
Nimbus Discovery
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI
Merck Research Laboratories
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI
Bristol-Myers Squibb Research And Development
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.EBI
Glaxosmithkline
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.EBI
Merck Research Laboratories
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.EBI
Merck Research Laboratories
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.EBI
Merck Research Laboratories
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
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
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
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI
Abbott Laboratories
Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.EBI
Amri
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.EBI
TBA
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI
TBA
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.EBI
Merck Research Laboratories
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI
Vertex Pharmaceuticals
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI
National Cancer Institute-Bethesda
IRAK-4 inhibitors. Part III: a series of imidazo[1,2-a]pyridines.EBI
Ucb Pharma
IRAK-4 inhibitors. Part 1: a series of amides.EBI
Ucb Pharma
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
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
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
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.EBI
Vertex Pharmaceuticals
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
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI
Merck Research Laboratories
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 orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI
Merck Research Laboratories
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.EBI
Center For Molecular Medicine Of The Austrian Academy Of Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI
Vertex Pharmaceuticals
IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding.EBI
Ucb Pharma
Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.EBI
Amgen
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI
Abbott Bioresearch Center
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors.EBI
Merck Research Laboratories
Discovery of 4EBI
TBA
Targeting IRAK4 for Degradation with PROTACs.EBI
Glaxosmithkline Medicines Research Centre
Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.EBI
Genentech
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.EBI
Genentech
Targeting the immunity protein kinases for immuno-oncology.EBI
China Pharmaceutical University
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
Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88EBI
Astrazeneca
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
PROTAC Degradation of IRAK4 for the Treatment of Neurodegenerative and Cardiovascular Diseases.EBI
Usona Institute
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.EBI
Dana-Farber Cancer Institute
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
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
Discovery of potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-associate kinase-4.EBI
Amgen
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.EBI
Astrazeneca
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
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.EBI
Merck
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute Of Science And Technology (Kist)
Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.EBI
Bristol-Myers Squibb
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88EBI
Astrazeneca
Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.EBI
Astrazeneca
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.EBI
Pfizer
Elucidation of the vasoactive intestinal peptide pharmacophore for VPAC(2) receptors in human and rat and comparison to the pharmacophore for VPAC(1) receptors.BDB
Nih
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.BDB
Schering-Plough Research Institute
Effects of pyridine ring substitutions on affinity, efficacy, and subtype selectivity of neuronal nicotinic receptor agonist epibatidine.BDB
University Of Miami
Synthesis, kinetic evaluation and cell-based analysis of C-alkylated isofagomines as chaperones of β-glucocerebrosidase.BDB
University Of British Columbia
A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines.BDB
Eli Lilly
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.BDB
University Of Pennsylvania
Further validation of in vivo and in vitro pharmacological procedures for assessing the alpha 2/alpha 1-selectivity of test compounds: (1). Alpha-adrenoceptor antagonists.BDB
Janssen Pharmaceutica
Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain.BDB
The Scripps Research Institute
Characterization of muscarinic receptors in human, guinea pig and rat lung.BDB
UniversitÉ
Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents.BDB
Cyclacel
Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.BDB
Intervet Innovation
Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.BDB
Deltagen Research Laboratories
Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.BDB
Vertex Pharmaceuticals
Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacids.BDB
University Of Tennessee Health Science Center
Structural basis of enantioselective inhibition of cyclooxygenase-1 by S-alpha-substituted indomethacin ethanolamides.BDB
Michigan State University
Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.BDB
Gsk
Protein engineering of the colony-stimulating factor-1 receptor kinase domain for structural studies.BDB
Johnson & Johnson Pharmaceutical
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors.BDB
Purdue Pharma
Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.BDB
Incyte
Inhibitors of the Diadenosine Tetraphosphate Phosphorylase Rv2613c of Mycobacterium tuberculosis.BDB
University Of Konstanz
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.BDB
Palacky University
A structure-based design approach to the development of novel, reversible AChE inhibitors.BDB
Syngenta
Discovery and Characterization of a Eukaryotic Initiation Factor 4A-3-Selective Inhibitor That Suppresses Nonsense-Mediated mRNA Decay.BDB
Bc Cancer Agency