236 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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University and Collaborative Innovation Center For Biotherapy
Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Carna Biosciences
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Green Valley Research Institute
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Identification of allosteric ERK2 inhibitors through in silico biased screening and competitive binding assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Icahn School of Medicine At Mount Sinai
Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Ligand efficient tetrahydro-pyrazolopyridines as inhibitors of ERK2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Technische Universit£T Braunschweig
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38aMAPK and ERK1/2 inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Entremed
Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Array Biopharma
Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universit£
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Lexicon Pharmaceuticals
5Z-7-Oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Fudan University
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Array Biopharma
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Martin-Luther-University Halle-Wittenberg
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Novel acetamidothiazole derivatives: synthesis and in vitro anticancer evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Mansoura
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Califia Bio
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Roche Palo Alto
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The Institute of Cancer Research
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Exelixis
Incorporation of rapid thermodynamic data in fragment-based drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The University of Tokyo
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Irreversible protein kinase inhibitors: balancing the benefits and risks.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Covalution Pharma
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cellzome
Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanyang University
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences Oncology
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Cancer Institute-Bethesda
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Oxford
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hoffmann-La Roche
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Millennium Pharmaceuticals
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hoffmann-La Roche
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ansaris
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RhôNe-Poulenc Rorer
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institute For Biomedical Research
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Elan Pharmaceuticals
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Imperial College
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Elan Pharmaceuticals
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National University of Ireland
Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Elan Pharmaceuticals
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Elan Pharmaceuticals
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences Oncology
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Taisho Pharmaceutical
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanmi Research Center
Identification of death-associated protein kinases inhibitors using structure-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharmadesign
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Identification of novel inhibitors of extracellular signal-regulated kinase 2 based on the structure-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sejong University
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Targeting Extracellular Signal-Regulated Protein Kinase 1/2 (ERK1/2) in Cancer: An Update on Pharmacological Small-Molecule Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Southwest Jiaotong University
(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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research and Development
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Fujisawa Pharmaceutical
X-ray Screening of an Electrophilic Fragment Library and Application toward the Development of a Novel ERK 1/2 Covalent Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astex Pharmaceuticals
Identification of novel extracellular signal-regulated kinase docking domain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Maryland
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research and Development
Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Discovery of SHR2415, a Novel Pyrrole-Fused Urea Scaffold ERK1/2 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shanghai Hengrui Pharmaceutical
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Michigan State University
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astex Pharmaceuticals
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Beijing Normal University
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharmaceutical Research Institute
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Aventis Pharma Deutschland
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Newcastle University
Discovery of a novel kinase hinge binder fragment by dynamic undocking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universitat De Barcelona
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck And
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Array Biopharma
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Japan Tobacco
Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase I? and ?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Progress in the development of more effective and safer analgesics for pain management.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Catania
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbvie Bioresearch Center
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astex Pharmaceuticals
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Institute of Science & Technology (Kist)
Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Ankara University
Synthesis and biological evaluation of novel N, N'-disubstituted urea and thiourea derivatives as potential anti-melanoma agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nanjing University
Synthesis and biological evaluation of fused oxepinocoumarins as free radicals scavengers.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Aristotle University of Thessaloniki
Hyperbolic mixed-type inhibition of acetylcholinesterase by tetracyclic thienopyrimidines.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Bonn
Efficient synthesis of novel dialkyl-3-cyanopropylphosphate derivatives and evaluation of their anticholinesterase activity![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Carthage
Targeting Bacterial Nitric Oxide Synthase with Aminoquinoline-Based Inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of California Irvine
Design of a carbonic anhydrase IX active-site mimic to screen inhibitors for possible anticancer properties.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Florida
Agonist, antagonist, and inverse agonist characteristics of TIPP (H-Tyr-Tic-Phe-Phe-OH), a selective delta-opioid receptor ligand.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Arkansas
Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Emory University
A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
The Scripps Research Institute
Cloning and expression of an A1 adenosine receptor from rat brain.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
National Institute of Mental Health
Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
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](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
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](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
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](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Namur
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Merck Research Laboratories
DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORS![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Parke-Davis Pharmaceutical Research
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biocryst Pharmaceuticals
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](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Auckland