PMID

Data

Article Title

Organization

Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.

Abbvie Bioresearch Center

"Addition" and"Subtraction": Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors.

Novartis Institutes For Biomedical Research

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck

Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.

Merck

Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.

Harvard Medical School

Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.

Takeda Pharmaceutical

A review on ROCK-II inhibitors: From molecular modelling to synthesis.

Nirma University

Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.

Aerie Pharmaceuticals

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research

Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.

Georgia Institute Of Technology

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).

Icahn School Of Medicine At Mount Sinai

Discovery of bis-aryl urea derivatives as potent and selective Limk inhibitors: Exploring Limk1 activity and Limk1/ROCK2 selectivity through a combined computational study.

Shanghai Institute Of Technology

Design, synthesis and biological characterization of selective LIMK inhibitors.

Amakem Therapeutics

Rho kinase inhibitors: potentially versatile therapy for the treatment of cardiovascular diseases and more.

Therachem Research Medilab (India)

Design, synthesis, and biological evaluation of novel, highly active soft ROCK inhibitors.

Agoralaan Abis

Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.

Translational Research Institute

Discovery of potent and selective urea-based ROCK inhibitors: Exploring the inhibitor's potency and ROCK2/PKA selectivity by 3D-QSAR, molecular docking and molecular dynamics simulations.

Shanghai Institute Of Technology

Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.

Vertex Pharmaceuticals

Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.

Merck Research Laboratories

Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.

Lexicon Pharmaceuticals

Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.

Lexicon Pharmaceuticals

Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.

Merck Research Laboratories

Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.

Novartis Horsham Research Centre

In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.

Alcon Laboratories

Advances in the studies of roles of Rho/Rho-kinase in diseases and the development of its inhibitors.

Sun Yat-Sen University

3-[2-(Aminomethyl)-5-[(pyridin-4-yl)carbamoyl]phenyl] benzoates as soft ROCK inhibitors.

Amakem

Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.

Califia Bio

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

Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.

Merck Research Laboratories

Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.

Merck Research Laboratories

Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.

The Scripps Research Institute

Amino acid derived quinazolines as Rock/PKA inhibitors.

Translational Research Institute

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.

Astrazeneca

Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.

Msd

Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.

Msd

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Abbott Laboratories

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.

Sichuan University

Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.

Teijin Pharma

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

Abbott Laboratories

Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.

H. Lee Moffitt Cancer Center And Research Institute

Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK).

University Of Tartu

Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.

TBA

Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.

Merck Research Laboratories

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.

Boehringer Ingelheim Pharmaceuticals

Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.

Boehringer Ingelheim Pharmaceuticals

Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.

Pfizer

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

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

Design and synthesis of Rho kinase inhibitors (II).

Kirin Brewery

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

Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.

Serono Pharmaceutical Research Institute

Kinase inhibitors: not just for kinases anymore.

Northwestern University

Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.

Glaxosmithkline

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

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-II).

The Scripps Research Institute

Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I).

The Scripps Research Institute

1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.

RhôNe-Poulenc Rorer

Comprehensive analysis of kinase inhibitor selectivity.

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.

Novartis Institute For Biomedical Research

Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Merck Research Laboratories

Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.

Pfizer

Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.

Vertex Pharmaceuticals

Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors.

Translational Research Institute

Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.

Abbott Laboratories

Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.

Abbott Laboratories

Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277

TBA

Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Merck Research Laboratories

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

Ambit Biosciences

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 2, optimization for blood pressure reduction in spontaneously hypertensive rats.

Boehringer Ingelheim Pharmaceuticals

Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.

The Scripps Research Institute

Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.

Boehringer Ingelheim Pharmaceuticals

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.

Abbott Laboratories

Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.

Translational Research Institute And Department Of Molecular Therapeutics

Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases.

University Of Tartu

2,3-Diaminopyrazines as rho kinase inhibitors.

Amri

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.

Lexicon Pharmaceuticals

Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).

National Human Genome Research Institute

Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.

The Scripps Research Institute-Florida

Chroman-3-amides as potent Rho kinase inhibitors.

The Scripps Research Institute

Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.

The Scripps Research Institute

Design and synthesis of rho kinase inhibitors (III).

Kirin Brewery

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.

Astrazeneca

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Evaluation of a dithiocarbamate derivative as an inhibitor of human glutaredoxin-1.

South Dakota State University

Nantenine as an acetylcholinesterase inhibitor: SAR, enzyme kinetics and molecular modeling investigations.

City University Of New York Hunter College

One-pot synthesis of 4,6-diaryl-2-oxo(imino)-1,2-dihydropyridine-3-carbonitrile; a New Scaffold for p38alpha MAP kinase inhibition.

German University In Cairo

[125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors.

U. 109

Synthesis and evaluation of imidazole-dioxolane compounds as selective heme oxygenase inhibitors: effect of substituents at the 4-position of the dioxolane ring.

Queen'S University

4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.

Merck Research Laboratories

Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.

Gsk

Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.

Karo Bio

Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.

Gsk

Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.

University Of Tennessee At Knoxville

Ketopiperazine-based renin inhibitors: optimization of the "C" ring.

Pfizer

Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.

Bristol-Myers Squibb