196 articles for thisTarget

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

PMID	Data	Article Title	Organization
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
28186750	11	"Addition" and"Subtraction": Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors.	Novartis Institutes For Biomedical Research
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27490956	59	Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.	Merck
27190596	53	Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.	Harvard Medical School
27117263	51	Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.	Takeda Pharmaceutical
27080184	3	A review on ROCK-II inhibitors: From molecular modelling to synthesis.	Nirma University
27072905	49	Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.	Aerie Pharmaceuticals
26951753	336	Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.	Novartis Institutes For Biomedical Research
26356532	39	Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.	Georgia Institute of Technology
26762835	342	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
26545798	10	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
26233434	115	Design, synthesis and biological characterization of selective LIMK inhibitors.	Amakem Therapeutics
25941551	4	Rho kinase inhibitors: potentially versatile therapy for the treatment of cardiovascular diseases and more.	Therachem Research Medilab (India)
25898023	67	Design, synthesis, and biological evaluation of novel, highly active soft ROCK inhibitors.	Agoralaan Abis
25621531	114	Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.	Translational Research Institute
25882521	121	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
24913714	53	Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.	Merck Research Laboratories
25589936	36	Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.	Lexicon Pharmaceuticals
25589930	62	Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.	Lexicon Pharmaceuticals
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
25248678	66	Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.	Novartis Horsham Research Centre
24684843	24	In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.	Alcon Laboratories
24211637	1	Advances in the studies of roles of Rho/Rho-kinase in diseases and the development of its inhibitors.	Sun Yat-Sen University
24119557	27	3-[2-(Aminomethyl)-5-[(pyridin-4-yl)carbamoyl]phenyl] benzoates as soft ROCK inhibitors.	Amakem
24044867	86	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.	Califia Bio
23742252	81	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
23602398	43	Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.	Merck Research Laboratories
23535330	83	Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.	Merck Research Laboratories
23570561	80	Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.	The Scripps Research Institute
23416002	126	Amino acid derived quinazolines as Rock/PKA inhibitors.	Translational Research Institute
23394126	170	Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).	Exelixis
23394218	159	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
21251828	44	Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.	Msd
21145740	41	Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.	Msd
23103095	125	Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.	Abbott Laboratories
23116168	42	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
22746295	91	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
22727637	85	Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.	Abbott Laboratories
22272748	46	Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.	H. Lee Moffitt Cancer Center and Research Institute
22521647	56	Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK).	University of Tartu
24900358	69	Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.	TBA
21128646	88	Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.	Merck Research Laboratories
20471253	32	Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.	Boehringer Ingelheim Pharmaceuticals
20000469	179	Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.	Boehringer Ingelheim Pharmaceuticals
14593182	34	Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.	Pfizer
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
17983756	55	Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.	Osi Pharmaceuticals
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
16876403	85	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
15999997	85	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
12672248	50	Kinase inhibitors: not just for kinases anymore.	Northwestern University
17018693	30	Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.	Glaxosmithkline
22136433	67	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
22014550	337	Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).	Ansaris
22018789	73	Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-II).	The Scripps Research Institute
22004718	58	Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I).	The Scripps Research Institute
21999461	90	1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.	RhôNe-Poulenc Rorer
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	Ambit Biosciences
21936542	143	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
20674350	63	Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
21620699	51	Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.	Pfizer
21391610	139	Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.	Vertex Pharmaceuticals
21349713	35	Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors.	Translational Research Institute
21288717	131	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
21282054	178	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
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
20855207	26	Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
10998351	24	Specificity and mechanism of action of some commonly used protein kinase inhibitors.	University of Dundee
20678931	23	Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 2, optimization for blood pressure reduction in spontaneously hypertensive rats.	Boehringer Ingelheim Pharmaceuticals
20684608	73	Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.	The Scripps Research Institute
20462760	70	Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.	Boehringer Ingelheim Pharmaceuticals
20346655	117	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
19837589	52	Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.	Translational Research Institute and Department of Molecular Therapeutics
19800227	31	Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases.	University of Tartu
20022494	60	2,3-Diaminopyrazines as rho kinase inhibitors.	Amri
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19831390	54	Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.	Lexicon Pharmaceuticals
19053756	27	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
18996009	36	Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.	The Scripps Research Institute-Florida
18990570	72	Chroman-3-amides as potent Rho kinase inhibitors.	The Scripps Research Institute
17368019	46	Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.	The Scripps Research Institute
16516473	444	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
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
32324396	17	p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.	China Pharmaceutical University
32944136	4	Identification of Novel Rho-Kinase-II Inhibitors with Vasodilatory Activity.	Banasthali Vidyapith
32001136	52	Discovery of thieno[2,3-d]pyrimidin-4(3H)-one derivatives as a new class of ROCK inhibitors.	Sichuan University
31757666	314	Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.	Merck
30819619	18	Discovery of (S)-6-methoxy-chroman-3-carboxylic acid (4-pyridin-4-yl-phenyl)-amide as potent and isoform selective ROCK2 inhibitors.	Shanghai Institute of Technology
27491711	422	Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.	Merck And
31223434	6	Potential of ROCK Inhibitors as Treatment for Cardiovascular Diseases, Cancer, and More.	Therachem Research Medilab
30755337	95	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.	Japan Tobacco
30594029	42	CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.	Shaoxing University
31693351	473	Discovery of 4	TBA
31330446	13	Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors.	Purdue University
31088713	2	Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats.	The First Affiliated Hospital of Nanjing Medical University
30384606	137	Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design.	Abbvie Bioresearch Center
30384048	365	ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.	University of Florida
31526603	379	Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.	Takeda Pharmaceutical
27002243	42	Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.	Novartis Institutes For Biomedical Research
26505898	123	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.	Novartis Institutes For Biomedical Research
26509640	234	Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.	Abbvie Bioresearch Center
23275831	121	Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).	Moffitt Cancer Center
29969256	21	Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.	Universitaire Vaudois
30457335	9	Polyheteroaryl Oxazole/Pyridine-Based Compounds Selected in Vitro as G-Quadruplex Ligands Inhibit Rock Kinase and Exhibit Antiproliferative Activity.	University Paris-Sud
29558119	30	Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61.	Zhejiang University
30082069	359	ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.	Vertex Pharmaceuticals
29945794	193	ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.	Vertex Pharmaceuticals
29545102	159	Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.	Merck
29266937	36	Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?	University of South Australia
30209946	5	Medermycin-Type Naphthoquinones from the Marine-Derived Streptomyces sp. XMA39.	Zhejiang University
29389122	10	Cyclizidine-Type Alkaloids from Streptomyces sp. HNA39.	Zhejiang University
29655979	25	Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.	Eli Lilly
28539220	198	Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.	Bristol-Myers Squibb Research and Development
28699740	294	Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.	Takeda Pharmaceutical
24070067	20	Fluorescence Linked Enzyme Chemoproteomic Strategy for Discovery of a Potent and Selective DAPK1 and ZIPK Inhibitor.	Duke University Medical Center
16243961	17	M2 and M3 muscarinic receptor activation of urinary bladder contractile signal transduction. I. Normal rat bladder.	Temple University
19143565	58	Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases.	University of Tartu
16699172	59	Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.	German Cancer Research Center