105 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
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
28109791	44	Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.	Chugai Pharmaceutical
28011205	3	Macrocyclic MEK1/2 inhibitor with efficacy in a mouse model of cardiomyopathy caused by lamin A/C gene mutation.	Columbia University
28011204	65	Structure-guided development of covalent TAK1 inhibitors.	Harvard Medical School
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
26943489	8	Discovery of Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3-Kinase (PI3K).	The University Of Michigan Medical School
26555154	36	AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.	University Of Edinburgh
27117263	51	Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.	Takeda Pharmaceutical
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
26611920	50	Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties.	Bayer Healthcare
26652860	68	A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.	Korea Institute Of Science And Technology (Kist)
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
26318067	34	Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.	Hanyang University
22315332	1	Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.	Genentech
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
25977981	76	Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.	TBA
25835317	63	Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.	Sichuan University
25766633	9	Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor.	The University Of Michigan Medical School
25529738	4	5Z-7-Oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner.	Osaka Prefecture University
25350923	7	Hybrids of phenylsulfonylfuroxan and coumarin as potent antitumor agents.	Fudan University
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
25193232	32	Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.	Genentech
24755426	38	Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors.	Shanghai Hengrui Pharmaceutical
23490150	48	Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.	Takeda Pharmaceutical
23550937	72	Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.	Emory University
23414845	44	Structure-based discovery of cellular-active allosteric inhibitors of FAK.	Takeda Pharmaceutical
23394126	170	Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).	Exelixis
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
23145854	9	Principles and applications of halogen bonding in medicinal chemistry and chemical biology.	Eberhard-Karls University
22612866	123	Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.	Astrazeneca
22506516	29	Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions.	Argenta Discovery
22621397	39	Irreversible protein kinase inhibitors: balancing the benefits and risks.	Covalution Pharma
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
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
22746295	91	Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.	Teijin Pharma
24900486	18	Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973).	TBA
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
22771009	9	Discovery of MEK/PI3K dual inhibitor via structure-based virtual screening.	Sejong 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
22406151	21	Design and synthesis of orally available MEK inhibitors with potent in vivo antitumor efficacy.	Takeda California
21353571	26	Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.	Hanyang University
20621728	19	Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.	Takeda California
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
18789685	172	Kinase array design, back to front: biaryl amides.	Glaxosmithkline
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
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
15999997	85	Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.	Serono Pharmaceutical Research Institute
12672248	50	Kinase inhibitors: not just for kinases anymore.	Northwestern University
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
11784156	20	Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1).	University Of Utah
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
9873633	50	MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.	Dupont Pharmaceuticals
20053779	5	Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models.	Hoffmann-La Roche
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
21741249	32	Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.	Heinrich Heine Universit£T
21620699	51	Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.	Pfizer
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
21316218	5	Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent.	Chugai Pharmaceutical
21310613	18	Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer.	Takeda California
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
20965724	57	Identification of potent ITK inhibitors through focused compound library design including structural information.	Nycomed
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
19945869	7	Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR.	Taisho Pharmaceutical
19945867	39	Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.	Taisho Pharmaceutical
19481464	41	Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.	Zhejiang University
	42	A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation	TBA
19327989	40	Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.	Pfizer
18815050	34	4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.	Wyeth Research
18755587	46	Discovery of thieno[2,3-c]pyridines as potent COT inhibitors.	Abbott Bioresearch Center
16934458	124	Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors.	Valeant Pharmaceuticals Research & Development
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
16725322	63	Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors.	Valeant Pharmaceutical Research And Development
16420026	19	Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones.	Array Biopharma
16275076	45	Pyrrolopyridazine MEK inhibitors.	Pharmaceutical Research Institute
16199156	1	Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors.	Genomics Institute Of The Novartis Research Foundation
16165349	40	Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.	Wyeth Research
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
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
15566294	5	Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.	Università
15006386	53	Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.	Bristol-Myers Squibb Pharmaceuticals Research Institute
12941327	24	Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade.	Wyeth Research
12086491	116	Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.	Pharmaceutical Research Institute
11934592	24	Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.	Merck Research Laboratories
11814812	12	4-Anilino-3-cyanobenzo[g]quinolines as kinase inhibitors.	Wyeth-Ayerst Research
11378365	52	MEK (MAPKK) inhibitors. Part 2: structure-activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines.	Wyeth-Ayerst Research
11378364	34	Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.	Research Biomet. Glaxo Wellcome Medicines Research Centre
11133101	29	Synthesis and structure-activity relationships of 3-cyano-4-(phenoxyanilino)quinolines as MEK (MAPKK) inhibitors.	Wyeth-Ayerst Research
28478927	46	Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors.	Martin-Luther-University Halle-Wittenberg
21985377	42	Synthesis and biological evaluation of novel N, N'-disubstituted urea and thiourea derivatives as potential anti-melanoma agents.	Nanjing University
27589335	78	Synthesis and biological evaluation of novel dasatinib analogues as potent DDR1 and DDR2 kinase inhibitors.	Guangzhou Institutes Of Biomedicine And Health, Chinese Academy Of Sciences
22170047	24	Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed.	University Of Copenhagen
17251021	24	Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.	Valeant Pharmaceuticals Research And Development
	80	Increasing the cellular PKC inhibitory activity of balanol: a study of ester analogs.	Sphinx Pharmaceuticals