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114 articles for thisTarget


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

PMID
Data
Article Title
Organization
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£
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
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
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
Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization.BDB
Institut De Recherches Servier
Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.BDB
Banyu Pharmaceutical
Pharmacological characterization of KUR-1246, a selective uterine relaxant.BDB
Kissei Pharmaceutical
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
Different binding affinities of NMDA receptor channel blockers in various brain regions--indication of NMDA receptor heterogeneity.BDB
Merz
Pharmacological characterization of a new class of nonpeptide neurokinin A antagonists that demonstrate species selectivity.BDB
Zeneca Pharmaceuticals
Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.BDB
Bristol-Myers Squibb