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

182 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.EBI
Carna Biosciences
First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-¿B Activity As Novel Anticancer Agents.EBI
Saarland University
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Design and Synthesis of Potent and Selective PIM Kinase Inhibitors by Targeting Unique Structure of ATP-Binding Pocket.EBI
The University Of Tokyo
Recent Advances in Scaffold Hopping.EBI
Rheinische Friedrich-Wilhelms-Universit£T
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors.EBI
Amgen
Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c.EBI
Universit£
Identification of quinones as novel PIM1 kinase inhibitors.EBI
Xavier University Of Louisiana
Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.EBI
Amgen
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
Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold.EBI
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of quinoline derivatives as potential anti-prostate cancer agents and Pim-1 kinase inhibitors.EBI
Shenyang Pharmaceutical University
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.EBI
Saarland University
Discovery of antitumor anthra[2,3-b]furan-3-carboxamides: Optimization of synthesis and evaluation of antitumor properties.EBI
Mendeleyev University Of Chemical Technology
Design and synthesis of substituted pyrido[3,2-d]-1,2,3-triazines as potential Pim-1 inhibitors.EBI
Shenyang Pharmaceutical 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 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.EBI
Genentech
Synthesis and activities of new indolopyrrolobenzodiazepine derivatives toward acute myeloid leukemia cells.EBI
Universit£
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI
Sichuan 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
Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene Kinase Pim-1.EBI
Taiwan Academia Sinica
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.EBI
Sichuan University
Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.EBI
Amgen
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.EBI
Amgen
Synthesis of pyrazolo[4,3-a]phenanthridines, a new scaffold for Pim kinase inhibition.EBI
Clermont Universit£
Pim kinase inhibitors for the treatment of cancer and possibly more.EBI
Therachem Research Medilab (India)
Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.EBI
Universit£
Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors.EBI
Astex Pharmaceuticals
Structure-based design of low-nanomolar PIM kinase inhibitors.EBI
Biogen Idec
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI
Nerviano Medical Sciences
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.EBI
Amgen
Pim kinase inhibitory and antiproliferative activity of a novel series of meridianin C derivatives.EBI
Keimyung University
Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase.EBI
Oxford University
Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.EBI
Heinrich Heine Universit£T
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.EBI
Heinrich-Heine-Universit£T D£Sseldorf
Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.EBI
Novartis Institutes For Biomedical Research
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI
Nerviano Medical Sciences
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.EBI
Merck Research Laboratories
Synthesis, resolution, and biological evaluation of atropisomeric (aR)- and (aS)-16-methyllamellarins N: unique effects of the axial chirality on the selectivity of protein kinases inhibition.EBI
Nagasaki University
Selectivity data: assessment, predictions, concordance, and implications.EBI
Eli Lilly
Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors.EBI
Clermont Universit£
Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.EBI
Genentech
Identification of pyrrolo[2,3-g]indazoles as new Pim kinase inhibitors.EBI
Clermont Universit£
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
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.EBI
Sichuan University
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
Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.EBI
The University Of Arizona
Synthesis and biological activities of 4-substituted pyrrolo[2,3-a]carbazole Pim kinase inhibitors.EBI
TBA
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.EBI
Cnrs
Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.EBI
Cylene Pharmaceuticals
A one-pot synthesis and biological activity of ageladine A and analogues.EBI
Macquarie University
Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound.EBI
The University Of Tokyo
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.EBI
Astrazeneca
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.EBI
Sichuan University
Kinase inhibitory potencies and in vitro antiproliferative activities of N-10 substituted pyrrolo[2,3-a]carbazole derivatives.EBI
Clermont Universit£
The design, synthesis, and biological evaluation of PIM kinase inhibitors.EBI
Exelixis
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.EBI
Hanmi Research Center
Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.EBI
TBA
Discovery of XL413, a potent and selective CDC7 inhibitor.EBI
Exelixis
Implications of promiscuous Pim-1 kinase fragment inhibitor hydrophobic interactions for fragment-based drug design.EBI
Genzyme
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
Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells.EBI
Cylene Pharmaceuticals
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
The selectivity of protein kinase inhibitors: a further update.EBI
University Of Dundee
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI
National Cancer Institute-Bethesda
Indolyl-pyrrolone as a new scaffold for Pim1 inhibitors.EBI
Universit£
Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors.EBI
Chemical Diversity Research Institute
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
Use of copper(I) catalyzed azide alkyne cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors.EBI
Clermont Universit£
Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.EBI
Spanish National Cancer Research Centre (Cnio)
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
9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.EBI
Peking University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI
RhôNe-Poulenc Rorer
7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.EBI
Cylene Pharmaceuticals
Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.EBI
Novartis Institutes Of Biomedical Research
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells.EBI
University Of Siena
Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.EBI
Heinrich Heine Universit£T
Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.EBI
Universite£? De Rennes 1
The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.EBI
Genzyme
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
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
Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.EBI
Abbott Laboratories
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.EBI
Abbott Laboratories
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.EBI
Cylene Pharmaceuticals
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI
Nerviano Medical Sciences
Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles.EBI
Clermont Université
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.EBI
Université
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.EBI
Universit£
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
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI
Nerviano Medical Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).EBI
National Human Genome Research Institute
Discovery of colon tumor cell growth inhibitory agents through a combinatorial approach.EBI
German University In Cairo
Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.EBI
Clermont Universit£
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI
Vertex Pharmaceuticals
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI
Glaxosmithkline
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI
Glaxosmithkline
Identification of novel protein kinase CK1 delta (CK1delta) inhibitors through structure-based virtual screening.EBI
Università
Comparative molecular field analysis of flavonoid inhibitors of the PIM-1 kinase.EBI
Loma Linda University School Of Medicine
A small molecule-kinase interaction map for clinical kinase inhibitors.EBI
Ambit Biosciences
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
Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.EBI
The University Of Tokyo
Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.EBI
Yunnan University
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI
Vertex Pharmaceuticals
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.EBI
University College Cork
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI
Vertex Pharmaceuticals
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.EBI
Astrazeneca
Indole in the target-based design of anticancer agents: A versatile scaffold with diverse mechanisms.EBI
Mazandaran University Of Medical Sciences
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.EBI
University Of Tours
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute Of Science And Technology (Kist)
From PIM1 to PI3K? via GSK3?: Target Hopping through the Kinome.EBI
Glaxosmithkline
Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors.EBI
Keimyung University
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.EBI
Universit£
Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.EBI
Genentech
Discovery of N-substituted 7-azaindoles as PIM1 kinase inhibitors - Part I.EBI
Sanofi Genzyme
Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors - Lead series identification - Part II.EBI
Sanofi Genzyme
Structure based drug design of Pim-1 kinase followed by pharmacophore guided synthesis of quinolone-based inhibitors.EBI
Zarqa University
Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.EBI
Dana-Farber Cancer Institute
Eco-friendly synthesis of novel cyanopyridine derivatives and their anticancer and PIM-1 kinase inhibitory activities.EBI
Ain Shams University
Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.EBI
University Of Oxford
Synthesis, activity evaluation, and docking analysis of barbituric acid aryl hydrazone derivatives as RSK2 inhibitors.BDB
East China University Of Science And Technology
Definition of peptide inhibitors from a synthetic peptide library by targeting gelatinase B/matrix metalloproteinase-9 (MMP-9) and TNF-a converting enzyme (TACE/ADAM-17).BDB
China Pharmaceutical University
Design, synthesis, and urease inhibition studies of some 1,3,4-oxadiazoles and 1,2,4-triazoles derived from mandelic acid.BDB
Quaid-I-Azam University
The different inhibition mechanisms of OXA-1 and OXA-24 ß-lactamases are determined by the stability of active site carboxylated lysine.BDB
Case Western Reserve University
Specialization among iron-sulfur cluster helicases to resolve G-quadruplex DNA structures that threaten genomic stability.BDB
National Institutes Of Health, National Institutes Of Health Biomedical Research Center
Identification of the first in silico-designed TREK1 antagonists that block channel currents dose dependently.BDB
Korea Institute Of Science And Technology
A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis.BDB
Nagoya University School Of Medicine
Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R.BDB
Merck Research Laboratories
BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.BDB
Upr 9023
Pharmacological characterization of KUR-1246, a selective uterine relaxant.BDB
Kissei Pharmaceutical
Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine alpha 4 beta 2 receptor.BDB
Abbott Laboratories
Characterization of cloned somatostatin receptors SSTR4 and SSTR5.BDB
University Of Pennsylvania
The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosine receptor antagonist.BDB
Zeneca Pharmaceuticals
RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist.BDB
Syntex Discovery Research
The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors.BDB
Syntex Discovery Research
Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor.BDB
Massachusetts General Hospital
Pharmacological characterization of a new class of nonpeptide neurokinin A antagonists that demonstrate species selectivity.BDB
Zeneca Pharmaceuticals
Pharmacological characterization of a novel muscarinic partial agonist, YM796, in transfected cells expressing the m1 or m2 muscarinic receptor gene.BDB
University Of Arizona
Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.BDB
Bristol-Myers Squibb
Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase.BDB
Cornell University
Structure-activity relationship of HIV-1 protease inhibitors containing AHPBA. Part III: Modification of P2 site.BDB
Sankyo
Strong solute-solute dispersive interactions in a protein-ligand complex.BDB
University Of Leeds