399 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
28249207	78	Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.	East China Normal University
28692292	73	Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.	Sichuan University and Collaborative Innovation Center For Biotherapy
28279847	40	Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.	Carna Biosciences
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
28039836	41	Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.	East China Normal University
27940419	31	Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.	Comenius University In Bratislava
15080993	23	Novel GSK-3 inhibitors with improved cellular activity.	Glaxosmithkline
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27474927	76	Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors.	Paris-Sud University
27815120	16	Identification of lead small molecule inhibitors of glycogen synthase kinase-3 beta using a fragment-linking strategy.	Institute For Basic Science (Ibs)
27391135	28	3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents.	Egyptian Russian University
27423119	9	Design, synthesis and biological evaluation of 5-benzylidene-2-iminothiazolidin-4-ones as selective GSK-3ß inhibitors.	National Institute of Pharmaceutical Education and Research
27660690	4	Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3ß.	Institute of Harvard and Mit
27406796	26	Synthesis of benzimidazole based thiadiazole and carbohydrazide conjugates as glycogen synthase kinase-3ß inhibitors with anti-depressant activity.	Jamia Hamdard (Hamdard University)
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
27089211	38	Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.	Zhejiang University
27003761	120	Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.	Nerviano Medical Sciences
27131621	5	New applications for known drugs: Human glycogen synthase kinase 3 inhibitors as modulators of Aspergillus fumigatus growth.	Centro De Investigaciones Biologicas (Cib, Csic)
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
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
26696252	32	Versatility of the Curcumin Scaffold: Discovery of Potent and Balanced Dual BACE-1 and GSK-3ß Inhibitors.	Alma Mater Studiorum-University of Bologna
26562543	14	Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.	Central University
26486317	9	Hit Optimization of 5-Substituted-N-(piperidin-4-ylmethyl)-1H-indazole-3-carboxamides: Potent Glycogen Synthase Kinase-3 (GSK-3) Inhibitors with in Vivo Activity in Model of Mood Disorders.	Angelini
26496242	4	Evaluation of Improved Glycogen Synthase Kinase-3a Inhibitors in Models of Acute Myeloid Leukemia.	Technische Universit£T Darmstadt
26431428	36	Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).	Wuxi Apptec
26342867	52	Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.	Sichuan University
26318067	34	Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.	Hanyang University
26222319	192	Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.	Nerviano Medical Sciences
26115571	38	Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.	Eli Lilly
25662701	23	Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.	Zhejiang University
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
26121481	37	Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.	Vertex Pharmaceuticals
25905468	3	9-Hydroxycanthin-6-one, aß-Carboline Alkaloid from Eurycoma longifolia, Is the First Wnt Signal Inhibitor through Activation of Glycogen Synthase Kinase 3ß without Depending on Casein Kinase 1a.	Chiba University
23305709	2	Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure.	Eli Lilly
25835317	63	Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.	Sichuan University
25845281	26	Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.	Bristol-Myers Squibb Research and Development
25680029	12	Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.	The Institute of Cancer Research
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
25655721	51	Discovery of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally-active GSK-3ß inhibitors for Alzheimer's disease.	Mitsubishi Tanabe Pharma
25019388	31	Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.	Vertex Pharmaceuticals
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
24951331	5	Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3ß of substituted quinolines.	Kansas State University
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
24881566	140	Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).	Glaxosmithkline
25589930	62	Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.	Lexicon Pharmaceuticals
25467150	5	Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3ß (GSK-3ß) with cellular activity of promoting glucose uptake.	Fudan University
25462247	20	In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.	Fudan University
25369270	93	Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.	Galapagos
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
25219901	19	Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.	Technische Universit£T Darmstadt
25198388	47	The design and synthesis of potent and selective inhibitors of Trypanosoma brucei glycogen synthase kinase 3 for the treatment of human african trypanosomiasis.	University of Dundee
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24858546	46	Guanidinium-based derivatives: searching for new kinase inhibitors.	Trinity College
24685542	67	Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.	Bristol-Myers Squibb Research and Development
24650640	43	Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.	Martin-Luther-University Halle-Wittenberg
23490150	48	Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.	Takeda Pharmaceutical
23434140	35	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
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
23047001	30	Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3ß (GSK-3ß).	Fudan University
24900653	14	Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.	Abbott Laboratories
23354070	18	Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.	Universitat De Barcelona
23312943	166	Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.	Pfizer
23312472	129	Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.	Pfizer
23214499	24	3,6-Diamino-4-(2-halophenyl)-2-benzoylthieno[2,3-b]pyridine-5-carbonitriles are selective inhibitors of Plasmodium falciparum glycogen synthase kinase-3.	Technische Universit£T Braunschweig
22995819	4	Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine.	TBA
21764580	51	Identification of 2-(4-pyridyl)thienopyridinones as GSK-3ß inhibitors.	Glaxosmithkline
19303774	87	1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.	Glaxosmithkline
19349179	47	4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.	Glaxosmithkline
17194588	92	N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.	Glaxosmithkline
23147077	23	Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.	Takeda Pharmaceutical
23123015	22	Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.	Takeda Pharmaceutical
23103095	125	Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.	Abbott Laboratories
23099099	14	Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3ß inhibitors through virtual screening.	Fudan University
22883026	34	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
22726925	216	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
24900428	67	Structure-Based Design of Potent and Selective CK1¿ Inhibitors.	TBA
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
23088521	12	Novel 3-Azaindolyl-4-arylmaleimides exhibiting potent antiangiogenic efficacy, protein kinase inhibition, and antiproliferative activity.	Johannes Gutenberg University of Mainz
22998443	69	Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.	Cnrs
22489897	41	Discovery of novel potent and highly selective glycogen synthase kinase-3ß (GSK3ß) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.	Astrazeneca
23039927	44	Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.	Martin-Luther-University Halle-Wittenberg
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
23021994	108	Identification of pyrimidine derivatives as hSMG-1 inhibitors.	Pfizer
22980219	55	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
22877629	42	2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1¿) inhibitors.	Amgen
22695126	98	Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.	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
22642587	2	Langkolide, a 32-membered macrolactone antibiotic produced by Streptomyces sp. Acta 3062.	Technische Universit£T Berlin
22554206	33	Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.	Pfizer
22533818	84	Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a.	Technische Universit£T Darmstadt
24900464	66	Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.	TBA
22672803	57	Design, synthesis and biological evaluation of novel imidazopyridines as potential antidiabetic GSK3ß inhibitors.	Crystalgenomics
22439974	79	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
22404346	52	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
22050263	3	Exploring the binding sites of glycogen synthase kinase 3. Identification and characterization of allosteric modulation cavities.	Instituto De Quimica Medica-Csic
22368763	82	Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.	TBA
22257026	31	5-imino-1,2,4-thiadiazoles: first small molecules as substrate competitive inhibitors of glycogen synthase kinase 3.	Instituto De Qu£Mica M£Dica-Csic
24900346	90	Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.	TBA
22321216	2	Towards the preparation of radiolabeled 1-aryl-3-benzyl ureas: Radiosynthesis of [(11)C-carbonyl] AR-A014418 by [(11)C]CO(2) fixation.	University of Toronto
21353571	26	Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.	Hanyang University
21126094	5	Eutypoids B-E produced by a Penicillium sp. strain from the North Sea.	Institute of Marine Sciences (Ifm-Geomar)
21155605	39	Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.	Novartis Institutes For Biomedical Research
15559249	55	Pharmacological inhibitors of glycogen synthase kinase 3.	The Rockefeller University
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20561787	46	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
20138514	93	3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.	Vertex Pharmaceuticals
20138512	82	Discovery of potent and bioavailable GSK-3beta inhibitors.	Roche Palo Alto
20153204	109	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
20030405	7	Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode.	Peking University
19906467	109	Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).	Technische Universit£T Braunschweig
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
17850214	99	The selectivity of protein kinase inhibitors: a further update.	University of Dundee
19616957	9	The marine natural-derived inhibitors of glycogen synthase kinase-3beta phenylmethylene hydantoins: In vitro and in vivo activities and pharmacophore modeling.	University of Louisiana At Monroe
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
19320489	125	Discovery and development of aurora kinase inhibitors as anticancer agents.	Vertex Pharmaceuticals
9677190	49	Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.	University of California
14593182	34	Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.	Pfizer
18598080	2	Kinetic studies and bioactivity of potential manzamine prodrugs.	The University of Mississippi
18595720	1	2-N-Methyl modifications and SAR studies of manzamine A.	The University of Mississippi
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
18502127	77	2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3).	Kemia
18502121	31	Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors.	Chemical Diversity Research Institute
18345609	57	Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.	The Institute of Cancer Research
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
18221871	24	Pyrazinoindolone inhibitors of MAPKAP-K2.	Boehringer Ingelheim Pharmaceuticals
18324764	151	Pharmacophore modeling, quantitative structure-activity relationship analysis, and in silico screening reveal potent glycogen synthase kinase-3beta inhibitory activities for cimetidine, hydroxychloroquine, and gemifloxacin.	University of Jordan
18280153	9	Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors.	Glaxosmithkline
18006321	14	Novel GSK-3beta inhibitors from sequential virtual screening.	Korea Institute of Science and Technology
17708655	10	Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease.	University of Mississippi
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
17350261	16	Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
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
15267232	65	Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.	Eli Lilly
12954055	47	Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.	Johnson and Johnson Pharmaceutical Research and Development
12852764	20	Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors.	Novo Nordisk
22325951	41	Structure-activity relationship of the 7-hydroxy benzimidazole analogs as glycogen synthase kinase 3ß inhibitor.	Crystalgenomics
22310227	89	5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.	Glaxosmithkline
16249345	25	Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.	Glaxosmithkline
22269278	50	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
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
22261023	14	Quinolone derivatives containing strained spirocycle as orally active glycogen synthase kinase 3ß (GSK-3ß) inhibitors for type 2 diabetics.	Kyorin Pharmaceutical
22202172	17	6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3ß: discovery of nitrile derivatives with picomolar potency.	Activx Biosciences
22104147	29	Design and combinatorial synthesis of a novel kinase-focused library using click chemistry-based fragment assembly.	Carna Biosciences
22040023	63	Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).	Pfizer
22154349	123	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
22119469	107	Novel and selective spiroindoline-based inhibitors of Sky kinase.	Pfizer
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
22003817	71	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
22014755	36	Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.	Hanyang University
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
21873061	34	Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3ß.	Activx Biosciences
21907583	48	CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.	University of South Florida
21807510	31	Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.	Technische Universit£T Darmstadt
21699136	16	Selectivity of kinase inhibitor fragments.	Glaxosmithkline
21500862	38	Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds.	Instituto De Qui£?Mica Medica-Csic
21470862	110	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
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
21341675	266	Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.	Glaxosmithkline
21353545	39	Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors.	Harvard Medical School
24900231	22	Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.	TBA
21295469	37	6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3ß inhibitors.	Pfizer
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
21273066	83	Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.	National University of Ireland
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
21082766	49	Discovery of novel GSK-3ß inhibitors with potent in vitro and in vivo activities and excellent brain permeability using combined ligand- and structure-based virtual screening.	University of Louisiana At Monroe
21038853	133	4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.	Novartis Institutes For Biomedical Research
20873740	111	Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.	Nerviano Medical Sciences
20817473	57	Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.	Nerviano Medical Sciences Oncology
20833055	44	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
20708937	2	Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells.	University of Rostock
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
20675134	88	Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.	Daiichi Sankyo
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19338355	104	From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.	University of Illinois At Chicago
19327989	40	Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.	Pfizer
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19217301	6	Synthesis and cytotoxic activity of new azepino[3',4':4,5]pyrrolo[2,1-a]isoquinolin-12-ones.	Universidad Nacional AutóNoma De MéXico
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17395594	10	Cellular characterization of a novel focal adhesion kinase inhibitor.	University of Virginia
18054489	9	Novel heterocycle-substituted pyrimidines as inhibitors of NF-kappaB transcription regulation related to TNF-alpha cytokine release.	Seoul National University
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30996781	14	Discovery of the First-in-Class GSK-3?/HDAC Dual Inhibitor as Disease-Modifying Agent To Combat Alzheimer's Disease.	Alma Mater Studiorum-University of Bologna
27676184	29	Application of Fragment-Based de Novo Design to the Discovery of Selective Picomolar Inhibitors of Glycogen Synthase Kinase-3 Beta.	Sejong University
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
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31103902	41	Multi-target design strategies for the improved treatment of Alzheimer's disease.	China Pharmaceutical University
31074988	95	Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.	Vertex Pharmaceuticals (Europe)
30502116	8	An insight into medicinal chemistry of anticancer quinoxalines.	India
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30925338	60	Discovery of novel glycogen synthase kinase-3? inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.	Peking University
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30715878	68	Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.	Genentech
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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
26547690	17	Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.	The University of Tokyo
26498573	7	Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme.	University of Pisa
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24094818	26	6-(4-Pyridyl)pyrimidin-4(3H)-ones as CNS penetrant glycogen synthase kinase-3? inhibitors.	Mitsubishi Tanabe Pharma
23683591	23	Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors.	Jeil Pharmaceutical
23725591	31	Characterization of maleimide-based glycogen synthase kinase-3 (GSK-3) inhibitors as stimulators of steroidogenesis.	University of Illinois At Chicago
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15715498	7	CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor.	Vertex Pharmaceuticals
15686883	59	The development of potent and selective bisarylmaleimide GSK3 inhibitors.	Lilly Research Laboratories
15603961	35	3D QSAR studies on GSK-3 inhibition by aloisines.	Zhejiang University
30293796	34	Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3? (GSK-3?).	Fudan University
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29578342	35	Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.	Yunnan University
29541355	35	Dual GSK-3?/AChE Inhibitors as a New Strategy for Multitargeting Anti-Alzheimer's Disease Drug Discovery.	China Pharmaceutical University
29461846	1	Ca	Iwate University
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28689095	45	First dual AK/GSK-3? inhibitors endowed with antioxidant properties as multifunctional, potential neuroprotective agents.	Universit£
29208522	34	Discovery of new GSK-3? inhibitors through structure-based virtual screening.	Peking University
30078314	39	Tau-Centric Multitarget Approach for Alzheimer's Disease: Development of First-in-Class Dual Glycogen Synthase Kinase 3? and Tau-Aggregation Inhibitors.	Alma Mater Studiorum-University of Bologna
29306837	16	Glycogen synthase kinase-3 and its inhibitors: Potential target for various therapeutic conditions.	National Institute of Pharmaceutical Education and Research (NIPER)
29107425	90	Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.	Korea Institute of Science & Technology (Kist)
29259738	74	Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.	Vertex Pharmaceuticals
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28810189	11	Hydroxy-substituted trans-cinnamoyl derivatives as multifunctional tools in the context of Alzheimer's disease.	Alma Mater Studiorum-University of Bologna
29653895	210	An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.	Glaxosmithkline
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28460311	8	The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3? inhibitors for the treatment of ovarian cancer.	Fudan University
27689729	17	Natural and synthetic bioactive inhibitors of glycogen synthase kinase.	Jamia Hamdard (Hamdard University)
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28749667	10	BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease.	University of Dundee
29016121	44	Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.	Novartis Institutes For Biomedical Research
28557430	45	Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.	University of Kaiserslautern
28548834	40	Subtly Modulating Glycogen Synthase Kinase 3?: Allosteric Inhibitor Development and Their Potential for the Treatment of Chronic Diseases.	Centro De Investigaciones Biol�Gicas-Csic
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21054237	11	Effects of some drugs on human erythrocyte glucose 6-phosphate dehydrogenase: an in vitro study.	Ataturk University
19558346	15	Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.	Shandong University
26874344	6	Dihydropyrano [2,3-c] pyrazole: Novel in vitro inhibitors of yeast a-glucosidase.	King Abdulaziz University
25346381	6	Identification of Novel Selective Lysine-Specific Demethylase 1 (LSD1) Inhibitors Using a Pharmacophore-Based Virtual Screening Combined with Docking.	China Pharmaceutical University
23603658	33	Structure-guided design of a selective BCL-X(L) inhibitor.	Walter and Eliza Hall Institute of Medical Research
18608755	4	New tryptophanase inhibitors: towards prevention of bacterial biofilm formation.	Ben-Gurion University of The Negev
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11961071	4	Agonist, antagonist, and inverse agonist characteristics of TIPP (H-Tyr-Tic-Phe-Phe-OH), a selective delta-opioid receptor ligand.	University of Arkansas
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17981461	29	Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.	Gsk
17425297	18	Structure-based design and synthesis of N(omega)-nitro-L-arginine-containing peptidomimetics as selective inhibitors of neuronal nitric oxide synthase. Displacement of the heme structural water.	Northwestern University
17920884	18	New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation.	Amgen
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