195 articles for thisTarget
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Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl)-sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III.
Shandong University
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).
Icahn School Of Medicine At Mount Sinai
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.
Chinese Academy Of Sciences
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.
Chugai Pharmaceutical
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.
Chinese Academy Of Sciences
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
Califia Bio
Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II.
Shandong University
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.
The Institute Of Cancer Research
Quinazoline-based multi-tyrosine kinase inhibitors: synthesis, modeling, antitumor and antiangiogenic properties.
University Of Padova
Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL.
Korea Advanced Institute Of Science And Technology
Pyrazolo[3,4-d]pyrimidine Prodrugs: Strategic Optimization of the Aqueous Solubility of Dual Src/Abl Inhibitors.
Universit£
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.
Technical University Of Dortmund
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase
Genomics Institute Of The Novartis Research Foundation
Design, synthesis, and biological evaluation of pyrazolo[3,4-d]pyrimidines active in vivo on the Bcr-Abl T315I mutant.
Universit£
Cyclic peptides containing tryptophan and arginine as Src kinase inhibitors.
University Of Rhode Island
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.
Chinese Academy Of Sciences
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.
East China University Of Science And Technology
Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.
Institut Curie
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.
University Of Zurich
Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform.
Cyclofluidic
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Pfizer
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.
Chinese Academy Of Sciences
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
National Center For Advancing Translational Sciences
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
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.
Cellzome
Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics.
TBA
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
TBA
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.
Chinese Academy Of Sciences
A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation.
University Of Siena
Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.
University Of Washington
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1.
University Of Washington
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.
The Institute Of Cancer Research
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
Hanmi Research Center
Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.
University Of Washington
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Amgen
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.
Ambit Biosciences
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Abbott Laboratories
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
TBA
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Merck Research Laboratories
Discovery of Potent and Selective Inhibitors of Calcium-Dependent Protein Kinase 1 (CDPK1) from C. parvum and T. gondii.
University Of Washington
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.
Nerviano Medical Sciences Oncology
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.
Chinese Academy Of Sciences
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.
The Institute Of Cancer Research
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
Nerviano Medical Sciences
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.
University Of Milano-Bicocca
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.
Wyeth Research
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
National Cancer Institute-Bethesda
Discovery and development of aurora kinase inhibitors as anticancer agents.
Vertex Pharmaceuticals
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr
Targegen
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.
Center For Molecular Medicine Of The Austrian Academy Of Sciences
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
Amgen
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University Of Oxford
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.
Osi Pharmaceuticals
Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines.
Universit£
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
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.
Pfizer
Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.
Nippon Shinyaku
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.
Targegen
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells.
Universit£
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.
Novartis Pharma
Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
Kyowa Hakko Kogyo
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.
Millennium Pharmaceuticals
[(Alkylamino)methyl]acrylophenones: potent and selective inhibitors of the epidermal growth factor receptor protein tyrosine kinase.
Ciba
Sulfonylbenzoyl-nitrostyrenes: potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase.
Ciba-Geigy
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.
University Of Kentucky
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.
Chugai Pharmaceutical
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
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.
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).
Ansaris
Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors.
Beijing National Laboratory For Molecular Sciences
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.
Pfizer
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.
Novartis Institute For Biomedical Research
Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells.
University Of Siena
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
Pfizer
Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.
Chinese Academy Of Sciences
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.
The Institute Of Cancer Research
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.
East China University Of Science And Technology
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.
Nerviano Medical Sciences
Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study.
University Of Siena
Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.
Chinese Academy Of Sciences
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.
University Of Strasburg
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.
Osi Pharmaceuticals
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Millennium Pharmaceuticals
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
TBA
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
University Of Regensburg
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.
Martin-Luther-University Halle-Wittenberg
Identification of potent ITK inhibitors through focused compound library design including structural information.
Nycomed
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
Pfizer
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
Nerviano Medical Sciences Oncology
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.
Novartis Institutes For Biomedical Research
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Amgen
Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.
Temple University School Of Medicine
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.
Center For Molecular Medicine Of The Austrian Academy Of Sciences
Rational design of inhibitors that bind to inactive kinase conformations.
Novartis Research Foundation
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.
Université
A type-II kinase inhibitor capable of inhibiting the T315I"gatekeeper" mutant of Bcr-Abl.
Harvard Medical School
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.
Technische Universit£T Braunschweig
Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms.
Institute Of Molecular Genetics Igm-Cnr
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Novartis Institute Of Biomedical Research
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.
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.
Nerviano Medical Sciences
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.
Wyeth Research
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.
Wyeth Research
Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.
Novartis Institutes For Biomedical 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).
Wyeth Research
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
Wyeth Research
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.
Cgi Pharmaceuticals
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
Curis
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.
Chugai Pharmaceutical
Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR.
Taisho Pharmaceutical
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.
Memorial Sloan-Kettering Cancer Center
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.
Hanmi Research Center
Determination of permeability and lipophilicity of pyrazolo-pyrimidine tyrosine kinase inhibitors and correlation with biological data.
Universit£
9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.
Ariad Pharmaceuticals
The Role of 4-phosphonodifluoromethyl- and 4-phosphono-phenylalanine in the selectivity and cellular uptake of SH2 domain ligands
TBA
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.
Boehringer Ingelheim Pharmaceuticals
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
University Of Regensburg
Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases.
Santen Pharmaceutical
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?
Pfizer
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.
Ariad Pharmaceuticals
N-(thiazol-2-yl)-2-thiophene carboxamide derivatives as Abl inhibitors identified by a pharmacophore-based database screening of commercially available compounds.
Università
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.
Amgen
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.
Amgen
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.
Università
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Genomics Institute Of The Novartis Research Foundation
Entry into a new class of protein kinase inhibitors by pseudo ring design.
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.
Memorial Sloan-Kettering Cancer Center
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.
Targegen
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
Tanabe Research Laboratories Usa
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.
Glaxosmithkline
Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties.
Mcgill University/Royal Victoria Hospital
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.
Boehringer Ingelheim Pharmaceuticals
Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.
Eberhard-Karls University
Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.
University Of Milano-Bicocca
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
Targegen
A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors.
Università
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
University Of Regensburg
Design and synthesis of 5-aryl-pyridone-carboxamides as inhibitors of anaplastic lymphoma kinase.
Chembridge Research Laboratories And Chembridge
(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.
Johnson & Johnson Pharmaceutical Research And Development
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.
Novartis Institutes For Biomedical Research
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
Novartis Institutes For Biomedical Research
Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase.
Mcgill University/Royal Victoria Hospital
7-Pyrrolidinyl- and 7-piperidinyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
Novartis Pharma Research
7-Alkyl- and 7-cycloalkyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
Novartis Pharma Research
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.
Bayer Research Center
Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.
Novartis Pharma
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.
Novartis
Design of peptidomimetics that inhibit the association of phosphatidylinositol 3-kinase with platelet-derived growth factor-beta receptor and possess cellular activity.
Warner-Lambert
4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase.
Ciba Pharmaceuticals
Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.
Ciba-Geigy
Synthesis of novel bisindolylmethanes: New carbonic anhydrase II inhibitors, docking, and 3D pharmacophore studies.
Universiti Teknologi Mara (Uitm)
Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo.
Eli Lilly
N1-(3-cyclohexylbutanoyl)-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-AK57), a potent partial agonist for the human histamine H1- and H2-receptors.
University Of Kansas
An efficient rapid system for profiling the cellular activities of molecular libraries.
Genomics Institute Of The Novartis Research Foundation
Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor.
Meiji Seika Kaisha