172 articles for thisTarget

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PMID	Data	Article Title	Organization
27527804	109	Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).	Teva Branded Pharmaceutical Products R & D
27144831	149	Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.	Ariad Pharmaceuticals
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast 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
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
27106709	92	Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.	Korea Research Institute of Chemical Technology
26951750	59	Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.	Novartis Institutes For Biomedical Research
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
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
26235945	58	Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor.	Korea Research Institute of Chemical Technology
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
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
26005534	158	(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.	Genomics Institute of The Novartis Research Foundation
25559205	31	Cyclopentyl-pyrimidine based analogues as novel and potent IGF-1R inhibitor.	Piramal Enterprises
25180654	29	Design, synthesis, and evaluation of novel imidazo[1,2-a][1,3,5]triazines and their derivatives as focal adhesion kinase inhibitors with antitumor activity.	University of Paris
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
25271963	93	Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.	Astrazeneca
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24900877	107	Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.	Merck Research Laboratories
24685542	67	Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.	Bristol-Myers Squibb Research and Development
24900830	46	Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.	Vichem Chemie Research
23906342	14	Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.	Takeda Pharmaceutical
24157370	22	The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.	Chugai Pharmaceutical
24100158	148	Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).	Nerviano Medical Sciences
24900590	55	Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.	Glaxosmithkline
24044867	86	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.	Califia Bio
23755884	23	Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.	Takeda Pharmaceutical
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
23490150	48	Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.	Takeda Pharmaceutical
23249297	75	Trimeric hemibastadin congener from the marine sponge Ianthella basta.	Heinrich-Heine University
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
22765894	223	The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.	Exelixis
22612866	123	Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.	Astrazeneca
23123015	22	Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.	Takeda Pharmaceutical
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
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
22734674	81	The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.	Amgen
22141319	56	Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.	Cephalon
22548342	210	Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.	Exelixis
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
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
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
24900237	41	Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.	TBA
22372864	25	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.	Hanmi Research Center
22320327	250	Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.	Amgen
22168626	32	Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.	Ambit Biosciences
24900346	90	Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.	TBA
21441024	74	Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.	Sanofi-Aventis
21123062	48	Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.	Cephalon
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20153646	28	Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.	Institute of Science and Technology
20170163	157	Identification of 2-anilino-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-ones as dual PLK1/VEGF-R2 kinase inhibitor chemotypes by structure-based lead generation.	Technische Universitat Braunschweig
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
19716697	110	The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.	Boehringer Ingelheim Pharmaceuticals
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
19610618	41	Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.	University of South Florida
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
19522465	102	Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).	Boehringer Ingelheim Pharma
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
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
18321716	7	ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds.	Institute of Molecular Physiology
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
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
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
16480284	126	Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.	Pfizer
12166950	208	Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.	Millennium Pharmaceuticals
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
16476733	18	Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.	University of Queensland
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
22285571	49	QSAR studies for prediction of cross-ß sheet aggregate binding affinity and selectivity.	The Ohio State University College of Medicine
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
21967808	52	Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.	Cephalon
22169263	73	Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.	Cephalon
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
22101132	41	Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.	Shionogi
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
22061645	68	Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.	Cephalon
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
21859094	61	2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.	Cephalon
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
21812414	106	Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).	Pfizer
21775140	69	Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.	Astrazeneca
21708465	141	Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.	St. Jude Children'S Research Hospital
21632243	48	Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.	Cephalon
21561767	48	Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.	Ariad Pharmaceuticals
21493067	22	In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.	Astrazeneca R&D Boston
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
21353551	23	Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.	Osi Pharmaceuticals
21414779	64	Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.	Amgen
24900240	19	Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR.	TBA
24900229	41	Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.	TBA
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
21074994	46	Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.	Cephalon
21190849	53	2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines.	Cephalon
21080629	153	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.	University of Regensburg
21035334	55	Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.	Martin-Luther-University Halle-Wittenberg
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
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
18559524	21	BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.	Boehringer Ingelheim Austria
17376430	19	ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents.	The Hebrew University of Jerusalem
20472447	45	Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).	Nycomed Pharma
20483608	139	New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.	Novartis Institute of Biomedical Research
20430619	73	8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors.	Cephalon
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
20382527	26	Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.	Bristol-Myers Squibb Research and Development
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
20166671	85	Selectively nonselective kinase inhibition: striking the right balance.	Schering-Plough
19879134	94	Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.	Cgi Pharmaceuticals
19854052	420	Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.	Genomics Institute of The Novartis Research Foundation
20178321	74	Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening.	Chinese Academy of Sciences
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
20121196	12	Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening.	Yale University
20093027	92	Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.	Chugai Pharmaceutical
19775160	79	2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.	Takeda Pharmaceutical
19362847	51	Design and synthesis of a novel tyrosine kinase inhibitor template.	St. Jude Children'S Research Hospital
1479375	215	Protein-Tyrosine Kinase Inhibition: Mechanism-Based Discovery of Antitumor Agents	TBA
	42	A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation	TBA
19327989	40	Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.	Pfizer
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
19246196	104	5-Aminomethylbenzimidazoles as potent ITK antagonists.	Boehringer Ingelheim Pharmaceuticals
19211246	320	N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.	4Sc
19101143	70	Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).	Glaxosmithkline
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
19035792	85	Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.	Glaxosmithkline
18819799	72	Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).	Johnson & Johnson
18819794	53	Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.	Johnson & Johnson
18793846	33	Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.	Genomics Institute of The Novartis Research Foundation
18691885	60	Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.	Ariad Pharmaceuticals
18529047	156	Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.	Eberhard-Karls University
17185414	30	Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.	Genomics Institute of The Novartis Research Foundation
18308565	70	Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.	Cephalon
18289854	44	Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.	Bristol-Myers Squibb Research and Development
17826092	37	Optimization of triarylimidazoles for Tie2: influence of conformation on potency.	Glaxosmithkline
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
16682193	62	Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
16451066	58	Design and synthesis of 5-aryl-pyridone-carboxamides as inhibitors of anaplastic lymphoma kinase.	Chembridge Research Laboratories and Chembridge
16366598	51	(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.	Johnson & Johnson Pharmaceutical Research and Development
16198560	19	Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases.	Imclone Systems
16134929	22	Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.	Bristol-Myers Squibb
15771417	48	2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.	Johnson & Johnson Pharmaceutical Research and Development
15711537	653	A small molecule-kinase interaction map for clinical kinase inhibitors.	Ambit Biosciences
15615512	21	Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.	Bristol-Myers Squibb Pharmaceutical Research Institute
14640546	46	A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin	Cephalon
12941342	21	Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.	Aventis Pharmaceuticals
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
12039590	51	Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.	Abbott Bioresearch Center
11000003	8	Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor.	Merck Research Laboratories
9240345	33	Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.	Parke-Davis Pharmaceutical Research
2033582	2	Phosphonate-containing inhibitors of tyrosine-specific protein kinases.	National Cancer Institute-Bethesda
27231830	27	Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.	Aimst University
25346162	16	Synthesis, Biological Evaluation, and Molecular Simulation of Chalcones and Aurones as Selective MAO-B Inhibitors.	Pontificia Universidad Catolica De Chile
19743875	5	Characterization of the CHK1 allosteric inhibitor binding site.	Pfizer
21848665	9	Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands.	Yeditepe University
7681406	8	Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors.	Sanofi Recherche
11567092	4	Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors.	Gsk
16495061	8	Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent.	Johnson & Johnson Pharmaceutical