PMID

Data

Article Title

Organization

Guanidinium-based derivatives: searching for new kinase inhibitors.

Trinity College

Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.

Development Center For Biotechnology

Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.

Peking Union Medical College & Chinese Academy Of Medical Sciences

Recent progress in the identification of BRAF inhibitors as anti-cancer agents.

Cairo University

Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.

Takeda Pharmaceutical

Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.

Zhejiang University

Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.

Takeda Pharmaceutical

Synthetic approaches to the 2011 new drugs.

Shenogen Pharma Group

Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.

Takeda Pharmaceutical

Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.

Takeda Pharmaceutical

Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.

Astrazeneca

The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors.

Glaxosmithkline

Identification of a novel family of BRAF(V600E) inhibitors.

University Of Pennsylvania

1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.

Glaxosmithkline

Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.

Takeda Pharmaceutical

Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.

Takeda Pharmaceutical

Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.

Takeda Pharmaceutical

Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.

Cellzome

Conformation-specific effects of Raf kinase inhibitors.

Takeda California

Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.

Takeda Pharmaceutical

Design, synthesis and biological evaluation ofß-carboline derivatives as novel inhibitors targeting B-Raf kinase.

China Pharmaceutical University

Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.

Takeda Pharmaceutical

Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.

Genentech

Synthesis, biological evaluation and 3D-QSAR studies of novel 4,5-dihydro-1H-pyrazole niacinamide derivatives as BRAF inhibitors.

Nanjing University

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

Tri- and tetrasubstituted pyrazole derivates: regioisomerism switches activity from p38MAP kinase to important cancer kinases.

Islamic University Of Gaza

Features of selective kinase inhibitors.

University Of California San Francisco

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

The selectivity of protein kinase inhibitors: a further update.

University Of Dundee

Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors.

Glaxosmithkline

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.

Harvard Medical School

Dual binding site inhibitors of B-RAF kinase.

Johnson & Johnson Pharmaceutical Research & Development

Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.

Amgen

The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.

Glaxosmithkline

Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.

Westf£Lische Wilhelms-Universit£T M£Nster

Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.

Glaxosmithkline

Small molecule inhibitors of BRAF in clinical trials.

The Institute Of Cancer Research

Structure-based de novo design and biochemical evaluation of novel BRAF kinase inhibitors.

Sejong University

Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors.

Celgene

Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.

Pfizer

Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.

Takeda Pharmaceutical

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Identification of novel BRAF kinase inhibitors with structure-based virtual screening.

Sejong University

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Ariad Pharmaceuticals

Non-oxime pyrazole based inhibitors of B-Raf kinase.

Array Biopharma

Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.

Millennium 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

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

Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region.

Deciphera Pharmaceuticals

Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.

Takeda Pharmaceutical

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

Rational design of inhibitors that bind to inactive kinase conformations.

Novartis Research Foundation

The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.

The University Of Arizona

B-Raf kinase inhibitors: hit enrichment through scaffold hopping.

Wyeth Research

Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.

Wyeth Research

5-Substituted [1]pyrindine derivatives with antiproliferative activity.

University Of Paris

Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.

Wyeth Research

Discovery of highly potent and selective type I B-Raf kinase inhibitors.

Wyeth Research

BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.

The Institute Of Cancer Research

Novel pyrazolopyrimidines as highly potent B-Raf inhibitors.

Wyeth Research

Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.

Wyeth Research

Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.

Boehringer Ingelheim Pharmaceuticals

Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.

Wyeth Research

4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.

Wyeth Research

SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.

Bayer Research Center

Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.

Institute Of Cancer Research

Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.

Glaxosmithkline

Chromone containing sulfonamides as potent carbonic anhydrase inhibitors.

Ondokuz Mayis University

Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.

Taisho Pharmaceutical

Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.

Kyowa Hakko Kogyo

Comparison of A1 adenosine receptors in brain from different species by radioligand binding and photoaffinity labelling.

UniversitÄT Heidelberg

Regulation of dopamine D2 receptors by sodium and pH.

Medical Research Service

Carbonic anhydrase inhibitors: inhibition of cytosolic carbonic anhydrase isozymes II and VII with simple aromatic sulfonamides and some azo dyes.

Universita Degli Studi Di Firenze