287 articles for thisTarget

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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
28109791	44	Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.	Chugai Pharmaceutical
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
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27316541	2	Synthetic sulfoglycolipids targeting the serine-threonine protein kinase Akt.	University of Milano-Bicocca
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
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
26945110	3	Synthesis and evaluation of the cytotoxic activity of novel ethyl 4-[4-(4-substitutedpiperidin-1-yl)]benzyl-phenylpyrrolo[1,2-a]quinoxaline-carboxylate derivatives in myeloid and lymphoid leukemia cell lines.	University of Bordeaux
26652247	60	3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1.	Baylor College of Medicine
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£
26318067	34	Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.	Hanyang University
26233434	115	Design, synthesis and biological characterization of selective LIMK inhibitors.	Amakem Therapeutics
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
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
25007344	73	Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.	Christian-Albrechts-University of Kiel
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
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
25689347	29	Exploitation of the ability of¿-tocopherol to facilitate membrane co-localization of Akt and PHLPP1 to develop PHLPP1-targeted Akt inhibitors.	The Ohio State University
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
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
24811300	20	Biased and unbiased strategies to identify biologically active small molecules.	Institut De Chimie Des Substances Naturelles
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
25409491	83	A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.	Zhejiang University
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
25180768	11	2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.	Vanderbilt University Medical Center
24900862	14	Phenylalanine-Based Inactivator of AKT Kinase: Design, Synthesis, and Biological Evaluation.	Virginia Commonwealth University
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24650640	43	Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.	Martin-Luther-University Halle-Wittenberg
24508830	13	Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors.	Zhejiang University
24440479	4	Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl)-sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III.	Shandong University
24389511	25	Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.	Zhejiang University
24479418	39	Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.	Heinrich Heine Universit£T
24328302	94	Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.	Heinrich-Heine-Universit£T D£Sseldorf
24321345	11	Preparation and evaluation of deconstruction analogues of 7-deoxykalafungin as AKT kinase inhibitors.	Virginia Commonwealth University
24100158	148	Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).	Nerviano Medical Sciences
24036042	2	Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II.	Shandong University
23920481	25	Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.	The Institute of Cancer Research
23602398	43	Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.	Merck Research Laboratories
23587425	37	Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase 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
23506825	71	Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.	Pfizer
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
23415083	13	Synthesis, characterization and Akt phosphorylation inhibitory activity of cyclopentanecarboxylate-substituted alkylphosphocholines.	Kyung Hee University
23301767	154	Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.	University of Nottingham
23550937	72	Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.	Emory University
23414845	44	Structure-based discovery of cellular-active allosteric inhibitors of FAK.	Takeda Pharmaceutical
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
23249297	75	Trimeric hemibastadin congener from the marine sponge Ianthella basta.	Heinrich-Heine University
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
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
22621397	39	Irreversible protein kinase inhibitors: balancing the benefits and risks.	Covalution Pharma
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
22934575	124	Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.	Array Biopharma
22533986	181	Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.	Arqule
22548342	210	Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.	Exelixis
22889562	3	Synthesis, cytotoxicity of new 4-arylidene curcumin analogues and their multi-functions in inhibition of both NF-¿B and Akt signalling.	Sun Yat-Sen University
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
22560627	70	2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.	Technische Universit£T Braunschweig
22248236	24	Diverse heterocyclic scaffolds as allosteric inhibitors of AKT.	Astrazeneca
22320327	250	Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.	Amgen
22450127	64	Pyrazolopyrimidines as dual Akt/p70S6K inhibitors.	Exelixis
24900358	69	Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.	TBA
24900346	90	Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.	TBA
22342124	9	Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors.	Exelixis
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
20591679	1	Development of chemical probes: toward the mode of action of a methylene-linked di(aryl acetate) E1.	University College London
15975507	13	Features of selective kinase inhibitors.	University of California San Francisco
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20000735	12	Through the"gatekeeper door": exploiting the active kinase conformation.	Nerviano Medical Sciences
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
20097066	53	Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.	Schering-Plough Research Institute
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
19081716	57	Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.	Glaxosmithkline
14593182	34	Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.	Pfizer
18434148	43	Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.	Wyeth Research
18362070	79	Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.	Abbott Laboratories
18359226	50	Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.	Bristol-Myers Squibb Research and Development
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
18054229	35	Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.	Merck
18479914	52	Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.	Merck Research Laboratories
18296048	50	Rapid assembly of diverse and potent allosteric Akt inhibitors.	Merck Research Laboratories
18248814	24	Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.	Novartis Institute For Biomedical Research
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
17887663	34	Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.	Pfizer
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
16789737	1	Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells.	University of Pune
16460940	13	Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.	Hoffmann-La Roche
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
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
22377675	44	Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.	Westf£Lische Wilhelms-Universit£T M£Nster
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
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
22204902	9	Synthesis and biological activity of novel organoselenium derivatives targeting multiple kinases and capable of inhibiting cancer progression to metastases.	Institute of The Sir Mortimer Jewish General Hospital
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
22001093	4	Synthesis of GSK3ß mimetic inhibitors of Akt featuring a novel extended dipeptide surrogate.	H. Lee Moffitt Cancer Center and Research Institute
21982797	128	9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.	Peking University
22027102	7	Pharmacophore identification, virtual screening and biological evaluation of prenylated flavonoids derivatives as PKB/Akt1 inhibitors.	Zhejiang University
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
21824779	67	Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.	Amgen
21823617	58	9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.	Chugai Pharmaceutical
21714526	54	Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.	Amgen
21699136	16	Selectivity of kinase inhibitor fragments.	Glaxosmithkline
21741249	32	Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.	Heinrich Heine Universit£T
21705217	60	Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.	Bristol-Myers Squibb
20674350	63	Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
21650457	25	Backbone cyclic peptide inhibitors of protein kinase B (PKB/Akt).	The Hebrew University of Jerusalem
21561771	39	Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.	Chugai Pharmaceutical
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
21332118	157	Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.	Amgen
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
21420856	37	Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.	Array Biopharma
21392984	50	Discovery and SAR of spirochromane Akt inhibitors.	Array Biopharma
24900231	22	Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.	TBA
24900229	41	Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.	TBA
20971641	53	Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.	Array Biopharma
21038853	133	4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.	Novartis Institutes For Biomedical Research
20875738	9	5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidines as novel class of potent and highly selective CaMKII inhibitors.	Dainippon Sumitomo Pharma
20873740	111	Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.	Nerviano Medical Sciences
20855207	26	Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
20817473	57	Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.	Nerviano Medical Sciences Oncology
20817449	19	4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.	Pfizer
20810279	86	Discovery of pyrrolopyrimidine inhibitors of Akt.	Array Biopharma
19465931	12	Inhibitor hijacking of Akt activation.	University of California
20684549	76	Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.	Amgen
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
20481595	48	Design of selective, ATP-competitive inhibitors of Akt.	Pfizer
20483608	139	New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.	Novartis Institute of Biomedical Research
20462263	127	Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.	Cyclacel
20397705	208	Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.	Nerviano Medical Sciences
20363128	42	Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.	Wyeth Research
20074837	58	The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).	Wyeth Research
19179070	89	Aminofurazans as potent inhibitors of AKT kinase.	Glaxosmithkline
20347317	6	Synthesis and structure-activity relationship studies of peptidomimetic PKB/Akt inhibitors: the significance of backbone interactions.	The Hebrew University of Jerusalem
20307980	22	B-Raf kinase inhibitors: hit enrichment through scaffold hopping.	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
20137943	60	Azole-based inhibitors of AKT/PKB for the treatment of cancer.	Amgen
20137932	47	2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.	Amgen
19969400	4	5-Substituted [1]pyrindine derivatives with antiproliferative activity.	University of Paris
19879134	94	Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.	Cgi Pharmaceuticals
20045647	35	Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.	Institute For Medical Research
20151677	67	Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).	The Institute of Cancer Research
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
20093027	92	Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.	Chugai Pharmaceutical
20006500	60	Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.	Glaxosmithkline
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
19945869	7	Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR.	Taisho Pharmaceutical
19945867	39	Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.	Taisho Pharmaceutical
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19734051	17	Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.	The University of Texas
19888761	52	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.	Hanmi Research Center
19497644	147	QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine.	Zhejiang University
19604696	6	Discovery of a novel protein kinase B inhibitor by structure-based virtual screening.	Torrey Pines Institute For Molecular Studies
19362830	47	Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.	Wyeth Research
19356929	17	Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.	Boehringer Ingelheim Pharmaceuticals
19317452	155	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
19285393	90	Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.	Glaxosmithkline
19097777	55	Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.	Merck Research Laboratories
19053831	39	Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles.	Institute of General Genetics
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
18815050	34	4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.	Wyeth Research
18550373	97	The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.	Merck Research Laboratories
18539456	106	Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors.	Merck Research Laboratories
18457385	41	Recent developments in fragment-based drug discovery.	Astex Therapeutics
15620258	2	A phthalide with in vitro growth inhibitory activity from an oidiodendron strain.	Cetek
18248988	16	Entry into a new class of protein kinase inhibitors by pseudo ring design.	Novartis Institutes For Biomedical Research
17826092	37	Optimization of triarylimidazoles for Tie2: influence of conformation on potency.	Glaxosmithkline
17658776	109	Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.	Abbott Laboratories
17574417	98	SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.	Bayer Research Center
17343372	143	Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.	Abbott Laboratories
17276059	32	Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics.	Yale University
17188862	27	Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927.	Wyeth Research
17149885	20	Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.	Eberhard-Karls University
16990001	12	Synthesis and biological evaluation of 5-arylamino-6-chloro-1H-indazole-4,7-diones as inhibitors of protein kinase B/Akt.	Ildong Pharmaceutical
16970394	147	Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.	Amgen
16765046	63	Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.	Chiron
16682193	62	Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
16216502	119	Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.	Abbott Laboratories
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
30660827	70	Quinolone hybrids and their anti-cancer activities: An overview.	Qilu University of Technology (Shandong Academy of Sciences)
31757666	314	Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.	Merck
27491711	422	Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.	Merck And
27305487	105	Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.	Arqule
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
31298542	108	Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.	Chinese Academy of Sciences
30469042	9	Pharmaceutical significance of azepane based motifs for drug discovery: A critical review.	Wuhan Institute of Technology
31404864	11	Coumarin-containing hybrids and their anticancer activities.	Tsinghua University
31207462	42	Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.	Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
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
31301565	20	Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors.	Hangzhou Institute of Innovative Medicine
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
24445311	1	Benzofuran derivatives as a novel class of inhibitors of mTOR signaling.	Cnrs/Universit£
31200237	95	Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.	Shanghai Pharmaceuticals Holding
19271717	96	Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium.	Heinrich-Heine-Universitat
18494522	244	Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense.	Heinrich-Heine-Universit£T
29578342	35	Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.	Yunnan 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
29549836	47	Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.	Universit£
29545102	159	Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.	Merck
28704757	16	Structural optimization elaborates novel potent Akt inhibitors with promising anticancer activity.	Shandong University
29466002	193	Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.	University of Edinburgh
29966916	11	Design, synthesis, in vitro and in silico evaluation of a new series of oxadiazole-based anticancer agents as potential Akt and FAK inhibitors.	Anadolu University
29927604	90	Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.	Chinese Academy of Medical Sciences and Peking Union Medical College
29107425	90	Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.	Korea Institute of Science & Technology (Kist)
28886509	15	Acridone-pyrimidine hybrids- design, synthesis, cytotoxicity studies in resistant and sensitive cancer cells and molecular docking studies.	Svkm'S Dr. Bhanuben Nanavati College of Pharmacy
29655979	25	Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.	Eli Lilly
28259529	31	Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.	The Ohio State University
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
28506751	4	Recent progress towards clinically relevant ATP-competitive Akt inhibitors.	Merck
29111705	4	One-Bead-Two-Compound Thioether Bridged Macrocyclic?-AApeptide Screening Library against EphA2.	University of South Florida
28287700	17	Price for Opening the Transient Specificity Pocket in Human Aldose Reductase upon Ligand Binding: Structural, Thermodynamic, Kinetic, and Computational Analysis.	Philipps-Universität Marburg
28221775	5	Electrostatic Interactions as Mediators in the Allosteric Activation of Protein Kinase A RIa.	University of California San Diego
27667561	16	Small-Molecule Chemical Probe Rescues Cells from Mono-ADP-Ribosyltransferase ARTD10/PARP10-Induced Apoptosis and Sensitizes Cancer Cells to DNA Damage.	University of Oulu
12739951	91	Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases.	University of Anterwerp
20804212	6	Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.	Pfizer
9776361	16	SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.	Smithkline Beecham Pharmaceuticals
9577836	119	Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.	University of Toronto
9023329	6	Affinity and selectivity of PD156707, a novel nonpeptide endothelin antagonist, for human ET(A) and ET(B) receptors.	University of Cambridge
1968985	56	Characteristics of 125I-iodocyanopindolol binding to beta-adrenergic and serotonin-1B receptors of rat brain: selectivity of beta-adrenergic agents.	Niigata College of Pharmacy
17581239	25	Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.	Pfizer
20444281	18	Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility.	University of Pittsburgh
11701096	24	Di-, tri- and tetra-5'-O-phosphorothioadenosyl substituted polyols as inhibitors of Fhit: Importance of the alpha-beta bridging oxygen and beta phosphorus replacement.	Kimmel Cancer Center
21867920	46	Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-Type Cannabinoid CB(2) Receptor Inverse Agonists.	University of Bern
16789731	3	Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.	University of Michigan
16759082	9	Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.	University of Michigan
18343106	12	Beta-lactam congeners of orlistat as inhibitors of fatty acid synthase.	Texas A&M University