264 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
28541695	192	Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRa) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).	East China University Of Science And Technology
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
28258797	32	Synthesis and evaluation of 5-(arylthio)-9H-pyrimido[4,5-b]indole-2,4-diamines as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.	Duquesne University
27750146	58	Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.	Chinese Academy Of Sciences
28004573	82	Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.	The Institute Of Cancer Research
27997164	18	Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting thea	Universit£
27914362	54	An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.	The First Affiliated Hospital Of Zhengzhou University
27894589	25	Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.	Duquesne University
28190652	26	Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors.	Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
27966954	19	Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.	High Magnetic Field Laboratory
27490023	25	Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors.	Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
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
27299736	37	The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.	St. John'S University
27348537	60	Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.	East China University Of Science & Technology
27131066	36	An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.	Chinese Academy Of Sciences
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
27077705	4	Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).	Chinese Academy Of Sciences
27011159	97	Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.	Experimental Therapeutics Centre
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
26923692	34	Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors.	Jiangxi Science And Technology Normal University
26944614	14	Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 2-oxo-4-chloro-1,2-dihydroquinoline-3-carboxamide moiety.	Jiangxi Science And Technology Normal University
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
26396681	58	Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.	Novartis Institutes For Biomedical Research
26526740	111	Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.	Univ. Lille
26318056	25	Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.	Universit£
26342867	52	Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.	Sichuan 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
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
25822739	37	Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.	Ku Leuven
25827399	52	Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.	Chinese Academy Of Sciences
25474320	10	Nintedanib: from discovery to the clinic.	Boehringer Ingelheim Pharma
25882519	45	The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.	Duquesne University
25086238	13	Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.	Shenyang Pharmaceutical University
25036791	56	Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor.	National Taiwan University
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
24785465	80	Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.	Chinese Academy Of Sciences
25440879	13	Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.	Shenyang Pharmaceutical University
25438768	44	Discovery andw biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors.	Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
25409491	83	A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.	Zhejiang University
25305330	75	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.	Southeast University
25221654	39	Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.	Novartis Institutes For Biomedical Research
24890652	44	The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.	Duquesne University
24996144	20	Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents.	Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
24904961	27	Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.	Qilu Pharmaceutical
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
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
24100158	148	Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).	Nerviano Medical Sciences
23993328	41	Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.	Chinese Academy Of Sciences
24012712	10	Design, synthesis, and structure-activity relationships of novel 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.	Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
23999040	27	Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors.	Nanjing University Of Technology
23352510	37	Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.	Roche Palo Alto
23900004	5	Quinazoline-based multi-tyrosine kinase inhibitors: synthesis, modeling, antitumor and antiangiogenic properties.	University Of Padova
23770449	16	Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs).	East China University Of Science And Technology
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
23566514	2	Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.	Pfizer
23498918	41	Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.	Takeda Pharmaceutical
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
23434139	47	Synthesis and biological activity of 5-chloro-N4-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.	Duquesne University
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
23375090	54	N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatic and antitumor agents.	Duquesne University
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
23414235	12	Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp.	Institute Of Microbial Chemistry (Bikaken)
23273517	53	Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.	National Center For Advancing Translational Sciences
22765894	223	The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.	Exelixis
23127890	96	SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.	Exelixis
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
24900421	87	Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.	TBA
23098265	46	Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.	University Of Genoa
22694093	16	Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.	National Institute Of Biological Sciences
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
22739090	86	Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.	Duquesne University
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
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
22497760	144	Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.	Astrazeneca
22465635	95	Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.	Abbott Laboratories
24900346	90	Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.	TBA
20558072	45	Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.	Duquesne University
20570525	56	Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.	Chinese Academy Of Sciences
20570526	84	Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.	National Taiwan University
20092323	23	Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.	Duquesne University
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
19320489	125	Discovery and development of aurora kinase inhibitors as anticancer agents.	Vertex Pharmaceuticals
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
18395443	37	Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.	Bristol-Myers Squibb
18324761	65	Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.	Amgen
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
18342505	43	Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.	Johnson & Johnson Pharmaceutical Research & Development
18289848	35	Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors.	Johnson & Johnson Pharmaceutical Research & Development
17113292	73	Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.	Targegen
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
16460940	13	Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.	Hoffmann-La Roche
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
16220969	219	Designed multiple ligands. An emerging drug discovery paradigm.	Organon Laboratories
12477352	85	Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.	Novartis Pharma
12238930	94	Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.	Kyowa Hakko Kogyo
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
22370340	91	N¿?¿-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.	Duquesne University
22221201	32	VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.	University Of Kentucky
16249345	25	Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.	Glaxosmithkline
10048786	2	Effects of the indolocarbazole 3744W on the tyrosine kinase activity of the cytoplasmic domain of the platelet-derived growth factor beta-receptor.	Wellcome Research Laboratories
22070629	61	Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).	Millennium Pharmaceuticals
22153662	137	Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.	Astrazeneca
22169262	26	Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.	Shenyang Pharmaceutical University
22101132	41	Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.	Shionogi
22204741	46	N¿?¿-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.	Duquesne University
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
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
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
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
21561767	48	Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.	Ariad Pharmaceuticals
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
24900231	22	Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.	TBA
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
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
20965724	57	Identification of potent ITK inhibitors through focused compound library design including structural information.	Nycomed
21028894	47	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.	Shanghai Hengrui Pharmaceuticals
20925433	21	Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.	Aristotle University Of Thessaloniki
20850301	68	Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors.	Astrazeneca
20833039	37	Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.	Industrial Technology Research Institute
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
20817538	16	Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.	Novartis Institutes For Biomedical Research
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
16783341	34	Rational design of inhibitors that bind to inactive kinase conformations.	Novartis Research Foundation
16565716	4	Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish.	Dana-Farber Cancer Institute
20681538	61	Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile.	Development Center For Biotechnology
20403700	76	Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.	Duquesne University
20403693	60	The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines.	Duquesne University
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
19646870	34	Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.	Ambit Biosciences
20031417	40	Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.	Hadassah Hebrew University Hospital
20148563	42	BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.	The Institute Of Cancer Research
19692247	295	Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.	4Sc
19754199	29	Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.	Ambit Biosciences
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
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
	46	The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-	TBA
	42	A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation	TBA
	230	Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives	TBA
	90	Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors	TBA
19301902	104	Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.	University Of Regensburg
19211246	320	N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.	4Sc
19113866	129	Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.	Novartis Institutes For Biomedical Research
19110422	12	5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.	Mahidol University
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
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18467105	71	Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.	Duquesne University
17197699	3	Structure and regulation of the human Nek2 centrosomal kinase.	University Of Oxford
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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
16931012	61	Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.	Targegen
16884302	209	4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution.	University Of Auckland
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
16750628	47	Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.	Abbott Laboratories
16722630	100	Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.	University Of Regensburg
16570908	39	Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.	Pharmaceutical Research Institute
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
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16078851	47	High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors.	Hadassah Hebrew University
15999992	25	Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.	Johnson & Johnson Pharmaceutical Research And Development
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
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
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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
15341941	140	Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor.	In Vivo Sciences Millennium Pharmaceuticals
15012985	31	Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.	Kirin Brewery
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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
14584942	91	Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.	Pharmaceutical Research Institute
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
12941341	23	Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.	Aventis Pharmaceuticals
12941331	96	Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
12941321	40	Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.	Kyowa Hakko Kogyo
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12039590	51	Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.	Abbott Bioresearch Center
11934592	24	Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.	Merck Research Laboratories
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9873628	1	Design and synthesis of a pyridone-based phosphotyrosine mimetic.	Cadus Pharmaceutical
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28411455	45	Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization.	Shanghai Pharmaceuticals Holding
28714692	232	Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.	University Of Chinese Academy Of Sciences
23488743	30	Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.	King Fahd University Of Petroleum & Minerals
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23935099	16	Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.	Glaxosmithkline
27231830	27	Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.	Aimst University
15256540	15	Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor.	Neurocrine Biosciences
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18416543	89	Aza-peptidyl Michael Acceptors. A New Class of Potent and Selective Inhibitors of Asparaginyl Endopeptidases (Legumains) from Evolutionarily Diverse Pathogens.	Georgia Institute Of Technology
16204883	5	The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition.	University Of California San Francisco
11567092	4	Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors.	Gsk
16632353	14	Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.	Abbott Laboratories
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17168540	20	Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.	Genentech
16495061	8	Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent.	Johnson & Johnson Pharmaceutical
17570665	19	Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.	Vernalis (R&D)
15685167	42	A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design.	Plexxikon
16517596	2	A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity.	Duke University Medical Center
14561089	6	Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.	Pharmacia
16699172	59	Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.	German Cancer Research Center
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16913714	4	Structure-Based Design of Novel HIV-1 Protease Inhibitors To Combat Drug Resistance.	Purdue University
16916797	8	Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.	Incyte
17110106	78	Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.	Abbott Laboratories
17181177	4	Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.	University Of Michigan
17034148	51	Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.	Abbott Laboratories
15771423	98	Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.	University Of Antwerp
16978863	42	3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.	Merck Research Laboratories
16870442	18	Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease.	Hawaii Biotech
24059701	21	Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors.	Qingdao University
16722663	12	Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.	Universita Di Siena
10639288	55	Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]indoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase.	Parke-Davis Pharmaceutical Research
11543677	20	Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.	Linkoping University