97 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
28291695	36	Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy.	Takeda California
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27050625	76	Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.	Temple University
27089211	38	Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.	Zhejiang University
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
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
26318056	25	Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.	Universit£
26039570	100	Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.	Vertex Pharmaceuticals
26071372	89	Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.	Astellas Pharma
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
25827523	275	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
25589936	36	Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.	Lexicon Pharmaceuticals
25369270	93	Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.	Galapagos
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
24044867	86	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.	Califia Bio
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
19303774	87	1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.	Glaxosmithkline
19349179	47	4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.	Glaxosmithkline
23103095	125	Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.	Abbott Laboratories
22795331	51	Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.	Janssen Pharmaceutical Companies of Johnson & Johnson
22738630	76	Structure-based optimization of aminopyridines as PKC¿ inhibitors.	Vertex Pharmaceuticals
22272748	46	Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.	H. Lee Moffitt Cancer Center and Research Institute
24900264	106	The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.	TBA
22521647	56	Conjugates of 5-isoquinolinesulfonylamides and oligo-D-arginine possess high affinity and selectivity towards Rho kinase (ROCK).	University of Tartu
22465635	95	Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.	Abbott Laboratories
24900346	90	Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.	TBA
20420387	118	Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.	Glaxosmithkline
20138514	93	3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.	Vertex Pharmaceuticals
20000469	179	Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.	Boehringer Ingelheim Pharmaceuticals
19703774	56	C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.	Wyeth Research
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
17046269	86	Design and synthesis of Rho kinase inhibitors (II).	Kirin Brewery
22310227	89	5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.	Glaxosmithkline
17018693	30	Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.	Glaxosmithkline
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
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	Ambit Biosciences
21341675	266	Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.	Glaxosmithkline
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
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
20434334	60	Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.	Kalypsys
19894727	164	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
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
20223663	100	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.	Wyeth Research
20188552	75	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
19884006	47	Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.	Wyeth Research
20166671	85	Selectively nonselective kinase inhibition: striking the right balance.	Schering-Plough
19854649	49	Discovery of highly potent and selective type I B-Raf kinase inhibitors.	Wyeth Research
19854645	87	Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.	Wyeth Research
19837589	52	Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.	Translational Research Institute and Department of Molecular Therapeutics
19632115	105	4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.	Vertex Pharmaceuticals
20022494	60	2,3-Diaminopyrazines as rho kinase inhibitors.	Amri
20006497	49	2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.	Glaxosmithkline
20005102	34	2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.	Glaxosmithkline
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19762237	58	First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.	Wyeth Research
19682896	49	C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.	Wyeth Research
19831390	54	Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.	Lexicon Pharmaceuticals
19800787	27	Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model.	Ligand Pharmaceuticals
19361991	80	Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.	Vertex Pharmaceuticals
19447612	59	Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.	Wyeth Research
19364658	113	Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).	Wyeth Research
19285393	90	Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.	Glaxosmithkline
18606543	68	2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.	Wyeth Research
17084087	36	Design and synthesis of rho kinase inhibitors (III).	Kirin Brewery
15955699	33	(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.	Glaxosmithkline
22299579	1	Evaluation of a dithiocarbamate derivative as an inhibitor of human glutaredoxin-1.	South Dakota State University
1975644	47	Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics.	U. 109
17581239	25	Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.	Pfizer
10662686	6	Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.	University of California San Francisco
10467133	4	Structural basis for selective inhibition of Src family kinases by PP1.	Princeton University
16275079	29	4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.	Merck Research Laboratories
18457381	36	Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.	Gsk
16303304	18	Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.	Karo Bio
17696333	2	Crystal Structure of the Anthrax Drug Target, Bacillus anthracis Dihydrofolate Reductase.	University of Tennessee At Knoxville
17055272	30	(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.	Merck Research Laboratories