277 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
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
28280261	84	Non-kinase targets of protein kinase inhibitors.	The University of Sydney
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27474918	12	Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line.	Cairo 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
27187860	18	Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia.	Yonsei University
27155464	35	Part-1: Design, synthesis and biological evaluation of novel bromo-pyrimidine analogs as tyrosine kinase inhibitors.	Rallis India
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
27374241	2	A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant.	Universit£
27115835	85	Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.	University of Edinburgh
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
27189674	84	RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.	Beni-Suef University
27010810	24	Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.	Oribase Pharma
26555154	36	AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.	University of Edinburgh
27089211	38	Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.	Zhejiang University
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
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
26789553	10	Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.	High Magnetic Field Laboratory
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
26451772	42	Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine.	First Affiliated Hospital of Xi'An Jiaotong University
26526740	111	Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.	Univ. Lille
26342867	52	Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.	Sichuan University
26298495	20	Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib.	Xi'An Jiaotong University
26286460	25	Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration.	University of Michigan
26231079	26	Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents.	Xi'An Jiaotong 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
26195136	32	Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.	Guangzhou Institutes of Biomedicine and Health
26022079	15	Design, synthesis, and biological activity of phenyl-pyrazole derivatives as BCR-ABL kinase inhibitors.	Beijing University of Technology
25469771	37	Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma.	Universit£
25965804	80	Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.	Eli Lilly
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
25699576	42	Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.	University of South Florida
25757603	79	New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity.	Siedlce University of Natural Sciences and Humanities
25022204	78	Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.	Universit£
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
25589930	62	Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.	Lexicon Pharmaceuticals
25409491	83	A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.	Zhejiang University
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
24801610	52	Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.	Universit£
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
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
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
24681986	42	Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.	Siedlce University of Natural Sciences and Humanities
24440479	4	Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl)-sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III.	Shandong University
24417566	43	Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).	Icahn School of Medicine At Mount Sinai
24359159	60	Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.	Astrazeneca
24280068	4	Imatinib analogs as potential agents for PET imaging of Bcr-Abl and c-KIT expression at a kinase level.	The University of Texas M.D. Anderson Cancer Center
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
23993328	41	Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.	Chinese Academy of Sciences
24044867	86	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.	Califia Bio
24036042	2	Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II.	Shandong University
23937569	22	Selectivity data: assessment, predictions, concordance, and implications.	Eli Lilly
23920481	25	Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.	The Institute of Cancer Research
23900004	5	Quinazoline-based multi-tyrosine kinase inhibitors: synthesis, modeling, antitumor and antiangiogenic properties.	University of Padova
23790540	17	Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL.	Korea Advanced Institute of Science and Technology
24015327	42	Development of a chimeric c-Src kinase and HDAC inhibitor.	University of Michigan
24900720	2	Pyrazolo[3,4-d]pyrimidine Prodrugs: Strategic Optimization of the Aqueous Solubility of Dual Src/Abl Inhibitors.	Universit£
23773153	33	Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.	Technical University of Dortmund
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
23746084	25	Design, synthesis, and biological evaluation of pyrazolo[3,4-d]pyrimidines active in vivo on the Bcr-Abl T315I mutant.	Universit£
23611771	8	The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588.	Novartis Institutes For Biomedical Research
23602444	2	Cyclic peptides containing tryptophan and arginine as Src kinase inhibitors.	University of Rhode Island
23538233	16	Design, synthesis and biological activities of Nilotinib derivates as antitumor agents.	Xi'An Jiaotong University
23474386	26	Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.	Chinese Academy of Sciences
23473682	69	BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives.	The First People'S Hospital of Hangzhou
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
23301767	154	Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.	University of Nottingham
22749189	24	Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.	Institut Curie
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
23253074	38	Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.	University of Zurich
23441572	55	Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform.	Cyclofluidic
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
23301703	20	Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.	Chinese Academy of Sciences
23273517	53	Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.	National Center For Advancing Translational Sciences
23103095	125	Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.	Abbott Laboratories
22726925	216	Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.	Cellzome
23088644	39	Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)¿isoleucine(315) mutant.	Chinese Academy of Sciences
24900387	11	Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics.	TBA
24900538	27	Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.	TBA
22863529	31	Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.	Chinese Academy of Sciences
22853993	18	A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation.	University of Siena
22320388	116	Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.	University of Washington
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
24900482	32	Targeted kinase selectivity from kinase profiling data.	TBA
22795629	59	Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1.	University of Washington
22404346	52	Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.	The Institute of Cancer Research
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
22369268	29	Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.	University of Washington
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
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
21608528	166	Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.	Merck Research Laboratories
21116453	51	Discovery of Potent and Selective Inhibitors of Calcium-Dependent Protein Kinase 1 (CDPK1) from C. parvum and T. gondii.	University of Washington
15975507	13	Features of selective kinase inhibitors.	University of California San Francisco
20674368	12	New effective inhibitors of the Abelson kinase.	Iowa State University
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20570525	56	Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.	Chinese Academy of Sciences
20561787	46	Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.	The Institute of Cancer Research
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
20117004	68	Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.	University of Milano-Bicocca
20038108	19	Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.	Wyeth Research
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
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
17371799	12	Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr	Targegen
17684099	4	The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.	Center For Molecular Medicine of The Austrian Academy of Sciences
18324759	133	Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.	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
18257513	13	Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines.	Universit£
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
17376680	18	Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.	Nippon Shinyaku
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
16678414	25	3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors.	Chiron
16686543	44	Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells.	Universit£
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
7608909	66	[(Alkylamino)methyl]acrylophenones: potent and selective inhibitors of the epidermal growth factor receptor protein tyrosine kinase.	Ciba
1652014	44	Sulfonylbenzoyl-nitrostyrenes: potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase.	Ciba-Geigy
22221201	32	VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.	University of Kentucky
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
22119469	107	Novel and selective spiroindoline-based inhibitors of Sky kinase.	Pfizer
22014550	337	Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).	Ansaris
22033461	4	Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors.	Beijing National Laboratory For Molecular Sciences
22014755	36	Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.	Hanyang University
21999461	90	1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.	RhôNe-Poulenc Rorer
21958547	108	Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.	Pfizer
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
21856155	45	Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells.	University of Siena
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
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
21536449	16	Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.	The Institute of Cancer Research
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
21561771	39	Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.	Chugai Pharmaceutical
21470862	110	NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.	Nerviano Medical Sciences
21443205	33	Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study.	University of Siena
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
21322567	18	Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.	University of Strasburg
21376587	15	Hybrid compounds as new Bcr/Abl inhibitors.	Chinese Academy of Sciences
21353551	23	Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.	Osi Pharmaceuticals
21341678	49	Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.	Millennium Pharmaceuticals
24900231	22	Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.	TBA
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
20961062	42	Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.	Pfizer
20873740	111	Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.	Nerviano Medical Sciences
20828158	92	Expanding the diversity of allosteric bcr-abl inhibitors.	Harvard Medical School
20817473	57	Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.	Nerviano Medical Sciences Oncology
20817538	16	Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.	Novartis Institutes For Biomedical Research
20684549	76	Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.	Amgen
20188579	42	Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.	Temple University
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
19039322	50	Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.	Center For Molecular Medicine of The Austrian Academy of Sciences
16783341	34	Rational design of inhibitors that bind to inactive kinase conformations.	Novartis Research Foundation
16415863	2	Allosteric inhibitors of Bcr-abl-dependent cell proliferation.	Genomics Institute of The Novartis Research Foundation
16408016	6	Assignment of protein function in the postgenomic era.	The Scripps Research Institute
20655209	18	Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.	Université
20604564	2	A type-II kinase inhibitor capable of inhibiting the T315I"gatekeeper" mutant of Bcr-Abl.	Harvard Medical School
20513156	44	Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.	Ariad Pharmaceuticals
20409618	31	Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.	Technische Universit£T Braunschweig
20451394	10	Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms.	Institute of Molecular Genetics Igm-Cnr
20483608	139	New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.	Novartis Institute of Biomedical Research
20462263	127	Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.	Cyclacel
20218623	68	Emerging targets in osteoporosis disease modification.	Amgen
20397705	208	Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.	Nerviano Medical Sciences
20363128	42	Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.	Wyeth Research
19894727	164	Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.	Wyeth Research
20231096	81	Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.	Novartis Institutes For Biomedical Research
20223663	100	2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.	Wyeth Research
20188552	75	Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).	Wyeth Research
19884006	47	Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.	Wyeth Research
20166671	85	Selectively nonselective kinase inhibition: striking the right balance.	Schering-Plough
19879134	94	Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.	Cgi Pharmaceuticals
19854649	49	Discovery of highly potent and selective type I B-Raf kinase inhibitors.	Wyeth Research
20143778	70	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.	Curis
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
19945869	7	Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR.	Taisho Pharmaceutical
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19889540	76	Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.	Memorial Sloan-Kettering Cancer Center
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
19410338	44	Determination of permeability and lipophilicity of pyrazolo-pyrimidine tyrosine kinase inhibitors and correlation with biological data.	Universit£
19572547	51	9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.	Ariad Pharmaceuticals
	230	Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives	TBA
	47	The Role of 4-phosphonodifluoromethyl- and 4-phosphono-phenylalanine in the selectivity and cellular uptake of SH2 domain ligands	TBA
	31	Novel phosphotyrosine mimetics in the design of peptide ligands for pp60src SH2 domain	TBA
19356929	17	Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.	Boehringer Ingelheim Pharmaceuticals
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
19109024	5	Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases.	Santen Pharmaceutical
19019675	52	Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?	Pfizer
18691885	60	Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.	Ariad Pharmaceuticals
18621522	18	N-(thiazol-2-yl)-2-thiophene carboxamide derivatives as Abl inhibitors identified by a pharmacophore-based database screening of commercially available compounds.	Università
18554909	50	Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.	Amgen
18447379	96	Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.	Amgen
18342402	77	Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.	Università
18313174	26	Synthesis and biological evaluation of diversely substituted indolin-2-ones.	Université
17185414	30	Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.	Genomics Institute of The Novartis Research Foundation
18248988	16	Entry into a new class of protein kinase inhibitors by pseudo ring design.	Novartis Institutes For Biomedical Research
17956080	4	Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.	Memorial Sloan-Kettering Cancer Center
17827012	30	The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.	Targegen
17827009	116	Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.	Tanabe Research Laboratories Usa
17826092	37	Optimization of triarylimidazoles for Tie2: influence of conformation on potency.	Glaxosmithkline
17572088	11	Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties.	Mcgill University/Royal Victoria Hospital
17560108	5	New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.	Boehringer Ingelheim Pharmaceuticals
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
16970400	14	Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling.	University of Milano-Bicocca
16931012	61	Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.	Targegen
16722646	24	A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors.	Università
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
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
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
15501042	18	Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.	Novartis Institutes For Biomedical Research
15177482	90	Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.	Novartis Institutes For Biomedical Research
12951113	11	Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase.	Mcgill University/Royal Victoria Hospital
11277536	130	7-Pyrrolidinyl- and 7-piperidinyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.	Novartis Pharma Research
11277535	80	7-Alkyl- and 7-cycloalkyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.	Novartis Pharma Research
10999468	30	1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.	Bayer Research Center
10853665	104	Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.	Novartis Pharma
10090785	63	Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.	Novartis
9784108	22	Design of peptidomimetics that inhibit the association of phosphatidylinositol 3-kinase with platelet-derived growth factor-beta receptor and possess cellular activity.	Warner-Lambert
8691423	89	4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase.	Ciba Pharmaceuticals
8151612	88	Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.	Ciba-Geigy
21985426	27	Chromone containing sulfonamides as potent carbonic anhydrase inhibitors.	Ondokuz Mayis University
21143042	30	Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors.	Shandong University
28056160	3	Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA-Encoded Chemical Library.	X-Chem Pharmaceuticals
27474804	19	Synthesis of novel bisindolylmethanes: New carbonic anhydrase II inhibitors, docking, and 3D pharmacophore studies.	Universiti Teknologi Mara (Uitm)
27289559	38	Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.	Tehran University of Medical Sciences
27231830	27	Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.	Aimst University
16690725	29	Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo.	Eli Lilly
16554355	47	N1-(3-cyclohexylbutanoyl)-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-AK57), a potent partial agonist for the human histamine H1- and H2-receptors.	University of Kansas
16492761	51	An efficient rapid system for profiling the cellular activities of molecular libraries.	Genomics Institute of The Novartis Research Foundation
16436501	8	Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor.	Meiji Seika Kaisha
15764739	7	Desensitization of the human motilin receptor by motilides.	Katholieke Universiteit Leuven
18849971	56	Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.	University of California San Francisco
17163639	13	High affinity InhA inhibitors with activity against drug-resistant strains of Mycobacterium tuberculosis.	Suny Stony Brook