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217 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.EBI
Sichuan University and Collaborative Innovation Center for Biotherapy
Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.EBI
Carna Biosciences, Inc
Structure-guided development of covalent TAK1 inhibitors.EBI
Harvard Medical School
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck & Co.
Macrocyclic Inhibitors of ERK2 Kinase.EBI
Dart Neuroscience LLC
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
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI
Southeast 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 srl
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).EBI
Green Valley Research Institute
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI
Novartis Institutes for BioMedical Research
Identification of allosteric ERK2 inhibitors through in silico biased screening and competitive binding assay.EBI
Osaka Prefecture 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
Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.EBI
Genentech
Recent progress on MAP kinase pathway inhibitors.EBI
Ontario Institute for Cancer Research
Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase.EBI
Novartis Institutes for BioMedical Research
Ligand efficient tetrahydro-pyrazolopyridines as inhibitors of ERK2 kinase.EBI
Novartis Institutes for BioMedical Research
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 srl
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.EBI
Technische Universit£t Braunschweig
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.EBI
TBA
Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38aMAPK and ERK1/2 inhibitory activity.EBI
Cairo University
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
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.EBI
EntreMed Inc.
Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.EBI
Array BioPharma Inc
Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors.EBI
Merck Research Laboratories
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£ de Nantes
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI
Nerviano Medical Sciences
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.EBI
Merck Research Laboratories
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.EBI
Lexicon Pharmaceuticals, Inc.
5Z-7-Oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner.EBI
Osaka Prefecture University
In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.EBI
Fudan University
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI
Merck Research Laboratories
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.EBI
Array BioPharma Inc
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI
Nerviano Medical Sciences
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.EBI
Martin-Luther-University Halle-Wittenberg
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI
Nerviano Medical Sciences srl
Novel acetamidothiazole derivatives: synthesis and in vitro anticancer evaluation.EBI
University of Mansoura
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI
Califia Bio Inc.
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
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.EBI
The Institute of Cancer Research
ERK2 Inhibitors May Provide Treatment for Cancer.EBI
Therachem Research Medilab (India) Pvt. Ltd.
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.EBI
Merck Research Laboratories
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.EBI
Merck Research Laboratories
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.EBI
Merck Research Laboratories
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.EBI
Emory University
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis Inc
Incorporation of rapid thermodynamic data in fragment-based drug discovery.EBI
The University of Tokyo
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI
Pfizer Inc
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI
Pfizer Inc
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI
GlaxoSmithKline
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI
GlaxoSmithKline
Irreversible protein kinase inhibitors: balancing the benefits and risks.EBI
Covalution Pharma BV
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
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 Ltd
Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist.EBI
TBA
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.EBI
Sichuan University
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI
Abbott Laboratories
Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.EBI
Pfizer Inc
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.EBI
Ambit Biosciences
The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.EBI
TBA
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.EBI
Hanyang University
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.EBI
Merck Research Laboratories
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI
Nerviano Medical Sciences Oncology
Discovery of potent and bioavailable GSK-3beta inhibitors.EBI
Roche Palo Alto
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 srl
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
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI
National Cancer Institute-Bethesda
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University of Oxford
Pyrazinoindolone inhibitors of MAPKAP-K2.EBI
Boehringer Ingelheim Pharmaceuticals Inc
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
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 Inc
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1).EBI
University of Utah
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI
Millennium Pharmaceuticals Inc
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI
GlaxoSmithKline
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.EBI
Hoffmann-La Roche Inc
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
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 srl
Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI
Pfizer Inc
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
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
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI
Rhône-Poulenc Rorer
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
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
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.EBI
Elan Pharmaceuticals
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI
Merck Research Laboratories
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
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI
Pfizer Inc
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 srl
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 Inc
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.EBI
TBA
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.EBI
Elan Pharmaceuticals, Inc.
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.EBI
National University of Ireland
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI
TBA
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.EBI
Elan Pharmaceuticals
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.EBI
Elan Pharmaceuticals
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 srl
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI
Merck Research Laboratories
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI
Nerviano Medical Sciences Oncology
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI
Cyclacel Ltd
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 srl
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
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 srl
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.EBI
Taisho Pharmaceutical Co., Ltd
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.EBI
Hanmi Research Center
Identification of death-associated protein kinases inhibitors using structure-based virtual screening.EBI
PharmaDesign Inc
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI
Vertex Pharmaceuticals Inc
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI
Vertex Pharmaceuticals Inc
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI
Wyeth Research
Identification of novel inhibitors of extracellular signal-regulated kinase 2 based on the structure-based virtual screening.EBI
Sejong University
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI
Wyeth Research
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
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI
Pfizer Inc
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
Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.EBI
University of Maryland
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.EBI
AstraZeneca
(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 LLC
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative.EBI
Fujisawa Pharmaceutical Co., Ltd
Identification of novel extracellular signal-regulated kinase docking domain inhibitors.EBI
University of Maryland
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 LLC
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.EBI
Michigan State University
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.EBI
Astex Pharmaceuticals
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.EBI
Chinese Academy of Sciences
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.EBI
Sichuan University
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Beijing Normal University
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.EBI
Genomics Institute of the Novartis Research Foundation
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.EBI
Pharmaceutical Research Institute
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.EBI
Aventis Pharma Deutschland GmbH
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.EBI
Newcastle University
Discovery of a novel kinase hinge binder fragment by dynamic undocking.EBI
Universitat de Barcelona
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.EBI
China Pharmaceutical University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Merck & Co.
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck and Co.
Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.EBI
Merck & Co., Inc.
Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.EBI
Array BioPharma Inc
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 Inc.
Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase I? and ?.EBI
Korea Institute of Science and Technology
Discovery of potent, orally bioavailable ERK1/2 inhibitors with isoindolin-1-one structure by structure-based drug design.EBI
China Pharmaceutical University
Progress in the development of more effective and safer analgesics for pain management.EBI
University of Catania
Discovery of 4EBI
TBA
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.EBI
Chengdu University
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.EBI
Bristol-Myers Squibb
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.EBI
University of Naples Federico II
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
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).EBI
AstraZeneca
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
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI
Vertex Pharmaceuticals Inc
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI
Vertex Pharmaceuticals, Inc
Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.EBI
Merck & Co.
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.EBI
Merck & Co.
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.EBI
Merck & Co.
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.EBI
Astex Pharmaceuticals
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI
Korea Institute of Science and Technology (KIST)
A combination ofEBI
The University of Tokyo
Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.EBI
AstraZeneca
Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.EBI
Sanford Burnham Prebys Medical Discovery Institute
Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth.EBI
The University of Texas at Austin
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.EBI
Novartis Institutes for BioMedical Research
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.EBI
University of Chinese Academy of Sciences
Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.BDB
Ankara University
Synthesis and biological evaluation of fused oxepinocoumarins as free radicals scavengers.BDB
Aristotle University of Thessaloniki
Hyperbolic mixed-type inhibition of acetylcholinesterase by tetracyclic thienopyrimidines.BDB
University of Bonn
 
Efficient synthesis of novel dialkyl-3-cyanopropylphosphate derivatives and evaluation of their anticholinesterase activityBDB
University of Carthage
Targeting Bacterial Nitric Oxide Synthase with Aminoquinoline-Based Inhibitors.BDB
University of California Irvine
Design of a carbonic anhydrase IX active-site mimic to screen inhibitors for possible anticancer properties.BDB
University of Florida
Agonist, antagonist, and inverse agonist characteristics of TIPP (H-Tyr-Tic-Phe-Phe-OH), a selective delta-opioid receptor ligand.BDB
University of Arkansas
Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.BDB
Emory University
A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms.BDB
The Scripps Research Institute
Cloning and expression of an A1 adenosine receptor from rat brain.BDB
National Institute of Mental Health
Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist.BDB
University of California San Francisco
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.BDB
Universita di Siena
Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference.BDB
Universita degli Studi di Firenze
Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX.BDB
University of Namur
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.BDB
Merck Research Laboratories
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.BDB
BioCryst Pharmaceuticals Inc
Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor.BDB
University of Auckland