194 articles for thisTarget

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PMID	Data	Article Title	Organization
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27769623	21	Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core.	Ocean University Of China
27131066	36	An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.	Chinese Academy Of Sciences
27144831	149	Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.	Ariad Pharmaceuticals
27078757	121	Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).	Astrazeneca
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
27106711	87	Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).	Green Valley Research Institute
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
26698536	56	Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.	Chinese Academy Of Sciences
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
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
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
26005534	158	(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.	Genomics Institute Of The Novartis Research Foundation
25738750	84	Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.	Astrazeneca
25827399	52	Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.	Chinese Academy Of Sciences
25559205	31	Cyclopentyl-pyrimidine based analogues as novel and potent IGF-1R inhibitor.	Piramal Enterprises
25648298	18	Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro.	Shandong University Of Technology
25369539	116	SAR156497, an exquisitely selective inhibitor of aurora kinases.	Sanofi
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
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
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
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
24900886	66	Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.	Chinese Academy Of Sciences
24773549	20	Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.	Development Center For Biotechnology
24685542	67	Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.	Bristol-Myers Squibb Research And Development
24565969	69	Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.	Chinese Academy Of Sciences
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
24183742	40	Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.	Chinese Academy Of Sciences
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
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
24900721	24	Discovery of novel insulin-like growth factor-1 receptor inhibitors with unique time-dependent binding kinetics.	Osi Pharmaceuticals
23742252	81	Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase	Genomics Institute Of The Novartis Research Foundation
23602398	43	Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.	Merck Research Laboratories
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
23490150	48	Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.	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
23362959	72	Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.	Sichuan University
23249297	75	Trimeric hemibastadin congener from the marine sponge Ianthella basta.	Heinrich-Heine University
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
22621397	39	Irreversible protein kinase inhibitors: balancing the benefits and risks.	Covalution Pharma
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
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
23041456	10	The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: a proof-of-concept study.	Novartis Institutes For Biomedical Research
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
22727637	85	Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.	Abbott Laboratories
22452518	22	Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.	Sichuan University
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
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
22263917	77	Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.	Amgen
24900264	106	The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.	TBA
22465635	95	Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.	Abbott Laboratories
24900358	69	Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.	TBA
21441024	74	Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.	Sanofi-Aventis
21353571	26	Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.	Hanyang University
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
20420387	118	Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.	Glaxosmithkline
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
19778024	31	Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.	Bristol-Myers Squibb
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
19394223	50	Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.	Glaxosmithkline
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
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
18343125	9	Formation of fluorine-18 labeled diaryl ureas--labeled VEGFR-2/PDGFR dual inhibitors as molecular imaging agents for angiogenesis.	Hadassah Hebrew University Hospital
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
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
17502145	18	Inhibition of IGF-1R and lipoxygenase by nordihydroguaiaretic acid (NDGA) analogs.	San Francisco State University
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
16451062	46	Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.	Astrazeneca
12477352	85	Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.	Novartis Pharma
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
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
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
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
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
21982797	128	9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.	Peking 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
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
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
21741249	32	Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.	Heinrich Heine Universit£T
21665484	37	Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.	Chinese Academy Of Sciences
21775140	69	Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.	Astrazeneca
21764307	108	Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline.	Astrazeneca
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
21524503	73	Dual IGF-1R/SRC inhibitors based on a N'-aroyl-2-(1H-indol-3-yl)-2-oxoacetohydrazide structure.	Technische Universit£T Braunschweig
21517068	45	Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.	East China University Of Science And Technology
21561771	39	Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.	Chugai Pharmaceutical
21405128	47	Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.	Chinese Academy Of 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
21251824	24	Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy.	Osi Pharmaceuticals
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
21035336	42	5-amino-pyrazoles as potent and selective p38a inhibitors.	Bristol-Myers Squibb Research And Development
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
20817523	61	Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.	Abbott Laboratories
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
20643554	32	Synthesis of aryl-heteroaryl ureas (AHUs) based on 4-aminoquinoline and their evaluation against the insulin-like growth factor receptor (IGF-1R).	San Francisco State University
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
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
20675137	17	Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase.	Bristol-Myers Squibb Research And Development
20472330	16	Novel 8-arylated purines as inhibitors of glycogen synthase kinase.	Institut Curie
20483608	139	New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.	Novartis Institute Of Biomedical Research
20399649	41	Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.	Bristol-Myers Squibb
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
20456957	96	Serotonin derivatives as a new class of non-ATP-competitive receptor tyrosine kinase inhibitors.	Universit£T Leipzig
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
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
20153189	51	SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.	Bristol-Myers Squibb
20031417	40	Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.	Hadassah Hebrew University Hospital
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
20093027	92	Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.	Chugai Pharmaceutical
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
19362847	51	Design and synthesis of a novel tyrosine kinase inhibitor template.	St. Jude Children'S Research Hospital
19362830	47	Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.	Wyeth Research
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
19097792	24	Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.	Astrazeneca R&D Boston
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
18986805	39	Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.	Astrazeneca Pharmaceuticals
18572407	75	Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.	Bristol-Myers Squibb
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
18313174	26	Synthesis and biological evaluation of diversely substituted indolin-2-ones.	Université
18289854	44	Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.	Bristol-Myers Squibb Research And Development
18258427	60	2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.	Bristol-Myers Squibb Pharmaceutical Research Institute
18248988	16	Entry into a new class of protein kinase inhibitors by pseudo ring design.	Novartis Institutes For Biomedical Research
18055203	51	Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.	Bristol-Myers Squibb Research And Development
17826092	37	Optimization of triarylimidazoles for Tie2: influence of conformation on potency.	Glaxosmithkline
17689078	61	Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).	Abbott Laboratories
17398093	72	Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.	Bristol-Myers Squibb Pharmaceutical Research Institute
17350837	59	Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.	Amgen
17317169	37	Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).	Bristol-Myers Squibb Pharmaceutical Research Institute
17187980	42	Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.	Bristol-Myers Squibb Pharmaceutical Research Institute
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
17127062	97	1,3-Disubstituted-imidazo[1,5-a]pyrazines as insulin-like growth-factor-I receptor (IGF-IR) inhibitors.	Osi Pharmaceuticals
16789733	41	Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.	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
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
16111887	104	New dual inhibitors of EGFR and HER2 protein tyrosine kinases.	Bristol-Myers Squibb Pharmaceutical Research Institute
15943473	136	Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
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
15177482	90	Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.	Novartis Institutes For Biomedical Research
15012985	31	Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.	Kirin Brewery
12941331	96	Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
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