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66 articles for thisTarget


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

PMID
Data
Article Title
Organization
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI
Zhejiang University
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
Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.EBI
Sanofi R & D
Novel azaindazole sulfonamides inhibitors of serum and glucocorticoid regulated kinase.EBI
Dart Neuroscience
2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.EBI
Vanderbilt University Medical Center
N-[4-(1H-Pyrazolo[3,4-B]pyrazin-6yl)-phenyl]-sulonamides and Their Use As Pharmaceuticals.EBI
Temple University
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI
Califia Bio
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI
Pfizer
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI
Glaxosmithkline
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
Identification of a novel serum and glucocorticoid regulated kinase-1 (SGK1) ligand from virtual screening.EBI
Northeast Ohio Medical University
Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK).EBI
University of Tartu
Through the"gatekeeper door": exploiting the active kinase conformation.EBI
Nerviano Medical Sciences
The selectivity of protein kinase inhibitors: a further update.EBI
University of Dundee
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI
Pfizer
Kinase array design, back to front: biaryl amides.EBI
Glaxosmithkline
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.EBI
Merck
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.EBI
Pfizer
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
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.EBI
Hoffmann-La Roche
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
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.EBI
Hoffmann-La Roche
Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI
Pfizer
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
Selectivity of kinase inhibitor fragments.EBI
Glaxosmithkline
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
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.EBI
TBA
Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.EBI
Spanish National Cancer Research Centre (Cnio)
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
2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.EBI
Amgen
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Identification of death-associated protein kinases inhibitors using structure-based virtual screening.EBI
Pharmadesign
Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors.EBI
Glaxosmithkline
Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.EBI
Merck Research Laboratories
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.EBI
Abbott Laboratories
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.EBI
Abbott Laboratories
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
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.EBI
Zunyi Medical University
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.EBI
Università
Selective Macrocyclic Inhibitors of DYRK1A/B.EBI
Dana-Farber Cancer Institute
Rational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis.EBI
Sanofi R&D
Discovery of EBI
Zhejiang University
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI
Boehringer Ingelheim Pharmaceuticals
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Beijing Normal University
Development of Pyrazolo[3,4-EBI
University of Genoa
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
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
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.EBI
Chinese Academy of Sciences
Discovery of 4EBI
TBA
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
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
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
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).EBI
Moffitt Cancer Center
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
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.BDB
Chemical Diversity