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258 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).EBI
Astrazeneca
Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS).EBI
Monash University (Parkville Campus)
RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.EBI
Beni-Suef University
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.EBI
Palack£
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.EBI
University Of Tours
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
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.EBI
Universit£
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI
Hanyang University
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.EBI
Eli Lilly
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI
Astrazeneca
Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action.EBI
Universit£
Biased and unbiased strategies to identify biologically active small molecules.EBI
Institut De Chimie Des Substances Naturelles
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.EBI
Lexicon Pharmaceuticals
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.EBI
Institut De Chimie Des Substances Naturelles
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.EBI
Amgen
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.EBI
Development Center For Biotechnology
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.EBI
Amgen
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.EBI
Takeda Pharmaceutical
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).EBI
Icahn School Of Medicine At Mount Sinai
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.EBI
Amgen
Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.EBI
University Of Nottingham
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.EBI
Chugai Pharmaceutical
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI
Califia Bio
Novel 1H-pyrrolo[2,3-b]pyridine derivative nortopsentin analogues: synthesis and antitumor activity in peritoneal mesothelioma experimental models.EBI
Universit£
6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity.EBI
Universit£
Synthesis, biological evaluation and molecular docking studies of pyrazole derivatives coupling with a thiourea moiety as novel CDKs inhibitors.EBI
Nanjing University
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.EBI
Roche Palo Alto
A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.EBI
Palack£
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.EBI
H. Lee Moffitt Cancer Center And Research Institute
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.EBI
University Of Nottingham
Synthesis and biological evaluation of guanidino analogues of roscovitine.EBI
Palack£
Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.EBI
Universitat De Barcelona
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.EBI
University Of Oxford
Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling.EBI
University Of Paris
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors.EBI
University Of St. Andrews
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.EBI
TBA
Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine.EBI
TBA
Cell cycle arrest and cytochrome c-mediated apoptotic induction by MCS-5A is associated with up-regulation of p16(INK4a) in HL-60 cells.EBI
Kyunggi-Do
Synthesis and cytotoxic activity of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidine derivatives.EBI
Universidad Nacional Aut£Noma De M£Xico
Pyrrolo[2,3-a]carbazoles as potential cyclin dependent kinase 1 (CDK1) Inhibitors. Synthesis, biological evaluation, and binding mode through docking simulations.EBI
University Of Patras
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.EBI
The Institute Of Cancer Research
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.EBI
Takeda Pharmaceutical
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.EBI
Cellzome
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.EBI
Universite£
Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist.EBI
TBA
Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.EBI
Universit£
Recent results in protein kinase inhibition for tropical diseases.EBI
Montclair State University
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.EBI
Martin-Luther-University Halle-Wittenberg
Identification of pyrimidine derivatives as hSMG-1 inhibitors.EBI
Pfizer
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI
Exelixis
Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents.EBI
University Of Nottingham
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
Targeted kinase selectivity from kinase profiling data.EBI
TBA
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
Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors.EBI
Biogen Idec
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI
TBA
Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1.EBI
Biogen Idec
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.EBI
TBA
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.EBI
Hanyang University
Selectivity and potency of cyclin-dependent kinase inhibitors.EBI
Georgetown University
Pharmacological inhibitors of glycogen synthase kinase 3.EBI
The Rockefeller University
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI
Nerviano Medical Sciences Oncology
Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases.EBI
Walter Reed Army Institute Of Research
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.EBI
Nerviano Medical Sciences
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.EBI
Schering-Plough Research Institute
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.EBI
Wyeth Research
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).EBI
Technische Universit£T Braunschweig
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI
National Cancer Institute-Bethesda
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).EBI
Boehringer Ingelheim Pharma
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.EBI
University Of California
Soluble 3',6-substituted indirubins with enhanced selectivity toward glycogen synthase kinase -3 alter circadian period.EBI
University Of Athens
Nitrogen-containing flavonoid analogues as CDK1/cyclin B inhibitors: synthesis, SAR analysis, and biological activity.EBI
Dalian University Of Technology
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI
Harvard Medical School
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.EBI
Millennium Pharmaceuticals
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.EBI
University Of Zurich
Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases.EBI
University Of Auckland
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
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.EBI
Astrazeneca
Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.EBI
Vanderbilt University School Of Medicine
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.EBI
Martin-Luther-University Halle-Wittenberg
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.EBI
Johnson And Johnson Pharmaceutical Research And Development
Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinases.EBI
Institute Of Research
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.EBI
Novartis Pharma
3D-QSAR CoMFA on cyclin-dependent kinase inhibitors.EBI
Institut Curie
2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors.EBI
Academy Of Sciences Of The Czech Republic
Synthesis and biological activity of olomoucine II.EBI
Palack£
Structure-activity relationship studies of flavopiridol analogues.EBI
Mitotix
2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.EBI
Novartis Pharmaceuticals
Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.EBI
University Of Queensland
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.EBI
Chugai Pharmaceutical
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.EBI
Hoffmann-La Roche
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.EBI
Shenyang Pharmaceutical University
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.EBI
Nerviano Medical Sciences
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
Synthesis of 6-(het) ary Xylocydine analogues and evaluating their inhibitory activities of CDK1 and CDK2 in vitro.EBI
Jilin University
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.EBI
The Institute Of Cancer Research
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI
Hanyang University
A modular approach to trim cellular targets in anticancer drug discovery.EBI
Instituto Universitario De Bio-Org£Nica Antonio Gonz£Lez (Iubo-Ag)
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
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.EBI
University Of South Florida
Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).EBI
Biogen Idec
Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities--development of highly efficacious cytotoxic agents.EBI
Guru Nanak Dev University
Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors.EBI
Keimyung University
Irreversible Nek2 kinase inhibitors with cellular activity.EBI
University Of California
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.EBI
Imperial College
Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.EBI
Millennium Pharmaceuticals
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.EBI
Trinity College
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
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
Identification of potent ITK inhibitors through focused compound library design including structural information.EBI
Nycomed
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.EBI
Novartis Institutes For Biomedical Research
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI
Nerviano Medical Sciences
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI
Amgen
Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay.EBI
University Of Jordan
Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.EBI
Temple University School Of Medicine
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.EBI
Boehringer Ingelheim Austria
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI
Cyclacel
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.EBI
Nerviano Medical Sciences
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.EBI
Universit£
5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.EBI
Institute Of Science And Technology
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.EBI
Wyeth Research
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-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.EBI
Wyeth Research
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI
Wyeth Research
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI
Wyeth Research
Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.EBI
Sanofi-Aventis
Selectively nonselective kinase inhibition: striking the right balance.EBI
Schering-Plough
Azole-based inhibitors of AKT/PKB for the treatment of cancer.EBI
Amgen
Synthesis and antiproliferative activity of 7-azaindirubin-3'-oxime, a 7-aza isostere of the natural indirubin pharmacophore.EBI
University Of Athens
Discovery of highly potent and selective type I B-Raf kinase inhibitors.EBI
Wyeth Research
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.EBI
Wyeth Research
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI
Nerviano Medical Sciences
New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme.EBI
Schering-Plough Research Institute
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.EBI
Chugai Pharmaceutical
Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR.EBI
Taisho Pharmaceutical
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.EBI
Taisho Pharmaceutical
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors.EBI
Institute Of Radiopharmacy
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.EBI
Takeda Pharmaceutical
Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency.EBI
Pfizer
Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency.EBI
Pfizer
Synthesis and biological evaluation of 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as a novel class of potential anti-tumor agents.EBI
National Organization For Drug Control And Research
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.EBI
Sunesis Pharmaceuticals
 
Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK IIEBI
TBA
 
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylationEBI
TBA
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.EBI
University Of Illinois At Chicago
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.EBI
Wyeth Research
Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.EBI
Johnson & Johnson Pharmaceutical Research & Development
The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing.EBI
Astrazeneca Pharmaceuticals
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.EBI
Sunesis Pharmaceuticals
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.EBI
Johnson & Johnson Pharmaceutical Research And Development
A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.EBI
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.EBI
Piramal Life Sciences
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI
Wyeth Research
Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors.EBI
Université
4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4).EBI
Wyeth Research
Natural products as leads to potential drugs: an old process or the new hope for drug discovery?EBI
National Cancer Institute-Frederick
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.EBI
Université
Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.EBI
University Of Auckland
Cellular characterization of a novel focal adhesion kinase inhibitor.EBI
University Of Virginia
Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species.EBI
Harbor Branch Oceanographic Institution
Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors.EBI
Keimyung University
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
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.EBI
Johnson & Johnson Pharmaceutical Research & Development
4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.EBI
Johnson & Johnson Pharmaceutical Research And Development
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.EBI
Abbott Laboratories
Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).EBI
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.EBI
Roche Research Center
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.EBI
Abbott Laboratories
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.EBI
Keimyung University
Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.EBI
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.EBI
Johnson & Johnson Pharmaceutical Research & Development
Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9.EBI
Banyu Tsukuba Research Institute
Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3.EBI
Université
Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis.EBI
Cephalon
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.EBI
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.EBI
Johnson & Johnson Pharmaceutical Research And Development
Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors.EBI
Bayer Research Center
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.EBI
Novartis Institutes For Biomedical Research
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinEBI
Cephalon
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.EBI
Eli Lilly
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors.EBI
Academy Of Sciences Of The Czech Republic
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.EBI
Novartis Pharma
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI
Abbott Bioresearch Center
Synthesis and antitumor activity of 1,5,6-substituted E-3-(2-chloro-3-indolylmethylene)-1,3-dihydroindol-2-ones.EBI
Università
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.EBI
Aventis Pharma Deutschland
Beta-carbolines as specific inhibitors of cyclin-dependent kinases.EBI
Institute Of Molecular And Cell Biology
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI
Glaxosmithkline
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.EBI
Research Biomet. Glaxo Wellcome Medicines Research Centre
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.EBI
Basf Bioresearch
Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.EBI
Novartis Pharma
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.EBI
UniversitäT Hamburg
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.EBI
UniversitäT Hamburg
Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure.EBI
Kyushu University
Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds.EBI
Charles University
Alkyl and alkoxyethyl antineoplastic phospholipids.EBI
National Hellenic Research Foundation
Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.BDB
Ankara University
The molecular chaperone Hsp70 activates protein phosphatase 5 (PP5) by binding the tetratricopeptide repeat (TPR) domain.BDB
University Of Michigan
Identification of Novel Selective Lysine-Specific Demethylase 1 (LSD1) Inhibitors Using a Pharmacophore-Based Virtual Screening Combined with Docking.BDB
China Pharmaceutical University
Structure-guided design of a selective BCL-X(L) inhibitor.BDB
Walter And Eliza Hall Institute Of Medical Research
New active HIV-1 protease inhibitors derived from 3-hexanol: conformation study of the free inhibitors in crystalline state and in complex with the enzyme.BDB
Technical University Of LÓDz
A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.BDB
Gpc Biotech
Identification of inhibitors of checkpoint kinase 1 through template screening.BDB
The Institute Of Cancer Research
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.BDB
Takeda Pharmaceutical
Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor.BDB
Nerviano Medical Sciences
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.BDB
Astex
Discovery of selective aminothiazole aurora kinase inhibitors.BDB
Novartis
Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).BDB
Paradigm Pharmaceuticals
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.BDB
Astex
Structural basis for Chk1 inhibition by UCN-01.BDB
Glaxosmithkline
Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.BDB
Vernalis (R&D)
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.BDB
Vernalis (R&D)
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.BDB
Hoffmann-La Roche
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.BDB
Nerviano Medical Sciences
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.BDB
Palacky University
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.BDB
Lawrence Berkeley National Laboratory
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.BDB
Vernalis (R&D)
Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.BDB
Cnrs
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.BDB
Glaxosmithkline
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.BDB
Cyclacel
First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease.BDB
Instituto De Quimica Medica (Csic)
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.BDB
Glaxosmithkline
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.BDB
Pharmacia Italia
3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.BDB
Johnson & Johnson Pharmaceutical
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.BDB
Johnson & Johnson Pharmaceutical
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.BDB
Eli Lilly
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.BDB
Avenida De La Industria
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.BDB
Eli Lilly
A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues.BDB
Banyu Tsukuba Research Institute
Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.BDB
Johnson & Johnson Pharmaceutical
Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.BDB
Johnson & Johnson Pharmaceutical
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.BDB
Pfizer
2-Aminoquinazoline inhibitors of cyclin-dependent kinases.BDB
Naeja Pharmaceutical
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.BDB
Parke-Davis Pharmaceutical Research
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.BDB
Bristol-Myers Squibb
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.BDB
Bristol-Myers Squibb
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.BDB
Bristol-Myers Squibb
Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.BDB
Bristol-Myers Squibb
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.BDB
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.BDB
Bristol-Myers Squibb Pharmaceutical Research Institute
Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines.BDB
Novartis Pharmaceuticals