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158 articles for thisTarget

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

Article Title
3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents.EBI
Egyptian Russian University
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.EBI
University of Nebraska Medical Center
A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.EBI
India Academy of Scientific & Innovative Research (Acsir)
Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy.EBI
University of South Carolina
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.EBI
The Institute of Cancer Research
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI
Zhejiang University
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
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 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 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
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptor▀ (PDGF-R▀) guided by water thermodynamics.EBI
Christian-Albrechts-University of Kiel
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.EBI
Institut De Chimie Des Substances Naturelles
Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents.EBI
Jamia Hamdard (Hamdard University)
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
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).EBI
The Institute of Cancer Research
Fragment based discovery of arginine isosteres through REPLACE: towards non-ATP competitive CDK inhibitors.EBI
University of South Carolina
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.EBI
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 selectivity of protein kinase inhibitors: a further update.EBI
University of Dundee
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.EBI
University of Oxford
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinaseEBI
S Bio
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 study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors.EBI
National Organization For Drug Control & Research
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.EBI
Nerviano Medical Sciences
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.EBI
Trinity College
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.EBI
Zunyi Medical University
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.EBI
Hefei University of Technology
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.EBI
Csir-Indian Institute of Integrative Medicine
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.EBI
The People'S Hospital of Xinjiang Uyghur Autonomous Region
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.EBI
Indian Institute of Technology (B.H.U.)
Current progress and novel strategies that target CDK12 for drug discovery.EBI
West China Hospital
Discovery, Optimization, and Evaluation of Selective CDK4/6 Inhibitors for the Treatment of Breast Cancer.EBI
China Pharmaceutical University
Medulloblastoma drugs in development: Current leads, trials and drawbacks.EBI
University of Connecticut
Discovery and Optimization of Highly Selective Inhibitors of CDK5.EBI
Goldfinc Bio
Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma.EBI
China Pharmaceutical University
Discovery of Dual CDK6/PIM1 Inhibitors with a Novel Structure, High Potency, and Favorable Druggability for the Treatment of Acute Myeloid Leukemia.EBI
China Pharmaceutical University
Indirubin Derivatives as Dual Inhibitors Targeting Cyclin-Dependent Kinase and Histone Deacetylase for Treating Cancer.EBI
Guizhou Medical University
Purdue University
Discovery of EBI
China Pharmaceutical University
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.EBI
Harvard Medical School
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.EBI
Chinese Academy of Sciences
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.EBI
Sichuan University
Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.EBI
University of Nottingham
Inávitro identification of imidazo[1,2-a]pyrazine-based antileishmanial agents and evaluation of L.ámajor casein kinase 1 inhibition.EBI
Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors.EBI
Cairo University
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1.EBI
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.EBI
China Pharmaceutical University
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.EBI
University Paris-Saclay
Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer.EBI
Beijing University of Chemical Technology
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.EBI
Shanghai Pharmaceuticals Holding
Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure.EBI
Institute For Organic Syntheses (Vuos)
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.EBI
Shanghaitech University
Tetrahydroindazole inhibitors of CDK2/cyclin complexes.EBI
University of Minnesota
The Resurrection of Phenotypic Drug Discovery.EBI
Temple University
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Beijing Normal University
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.EBI
China Pharmaceutical University
Anticancer potential of some imidazole and fused imidazole derivatives: exploring the mechanism EBI
Central University of Punjab
Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1).EBI
Shanghai Institute of Materia Medica
Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent inávitro and inávivo anticancer activity.EBI
Key Laboratory of Biomedical Materials of Natural Macromolecules (Beijing University of Chemical Technology)
Fragment Linking Strategies for Structure-Based Drug Design.EBI
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and EBI
Angelini Pharma
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.EBI
The First Affiliated Hospital of Zhengzhou University
Discovery and SARs of 5-Chloro-EBI
Anhui Medical University
Development of selective mono or dual PROTAC degrader probe of CDK isoforms.EBI
Sichuan University and Collaborative Innovation Center of Biotherapy
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Cink4T, a quinazolinone-based dual inhibitor of Cdk4 and tubulin polymerization, identified via ligand-based virtual screening, for efficient anticancer therapy.EBI
De Montfort University
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
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis.EBI
Nankai University
Discovery of CDK5 Inhibitors through Structure-Guided Approach.EBI
University of South Australia
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.EBI
Chongqing Medical University
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.EBI
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.EBI
China Pharmaceutical University
Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent inávitro and inávivo antitumor activity.EBI
China Pharmaceutical University
Discovery of novel pyrimidine-based benzothiazole derivatives as potent cyclin-dependent kinase 2 inhibitors with anticancer activity.EBI
Southern Medical University
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.EBI
Eberhard Karls University T£Bingen
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.EBI
University of Padova
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.EBI
University of South Australia Cancer Research Institute
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
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?EBI
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation.EBI
University of South Australia
Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity.EBI
De Montfort University
8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode.EBI
University of Oxford
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.EBI
Shanghai Pharmaceuticals Holding
Drug discovery for neglected diseases: molecular target-based and phenotypic approaches.EBI
University of Dundee
Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors.EBI
Jiangnan University
A ?-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.EBI
1,3,5-Triazines: A promising scaffold for anticancer drugs development.EBI
Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors.EBI
Jiangnan University
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.EBI
Seoul National University
Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.EBI
Chinese Academy of Sciences
Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate NEBI
The Institute of Cancer Research
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
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.EBI
Chinese Academy of Medical Sciences and Peking Union Medical College
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.EBI
University of Kwazulu-Natal
Discovery of the selective and efficacious inhibitors of FLT3 mutations.EBI
China Pharmaceutical University
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.EBI
University of Tours
Development of Second-Generation CDK2 Inhibitors for the Prevention of Cisplatin-Induced Hearing Loss.EBI
Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.EBI
Takeda Pharmaceutical
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute of Science & Technology (Kist)
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.EBI
Vertex Pharmaceuticals
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.EBI
Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.EBI
Csir-Indian Institute of Integrative Medicine
Synthesis and biological evaluation of N9-cis-cyclobutylpurine derivatives for use as cyclin-dependent kinase (CDK) inhibitors.EBI
Korea Research Institute of Chemical Technology
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.EBI
University of Paris
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.EBI
Csir-Indian Institute of Integrative Medicine
N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1?/? inhibitors: Synthesis, biological evaluation and molecular modeling studies.EBI
Rajiv Gandhi Proudyogiki Vishwavidyalaya
Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.EBI
University of Kaiserslautern
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.BDB
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.BDB
Vertex Pharmaceuticals
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
Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.BDB
Universite De Lyon
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.BDB
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
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.BDB
Vernalis (R&D)
Structural basis for Chk1 inhibition by UCN-01.BDB
Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.BDB
Vernalis (R&D)
A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor.BDB
Nerviano Medical Sciences
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
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.BDB
Vernalis (R&D)
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.BDB
Vernalis (R&D)
4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors.BDB
Tsukuba Research Laboratories
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.BDB
6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).BDB
5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).BDB
N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.BDB
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.BDB
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.BDB
Novartis Pharmaceuticals
Benzodipyrazoles: a new class of potent CDK2 inhibitors.BDB
Nerviano Medical Sciences
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.BDB
Pharmacia Italia
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.BDB
Nerviano Medical Sciences
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
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
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.BDB
2-Aminoquinazoline inhibitors of cyclin-dependent kinases.BDB
Naeja Pharmaceutical
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.BDB
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.BDB
Parke-Davis Pharmaceutical Research