177 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
28249207	78	Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.	East China Normal University
28140585	52	Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.	High Magnetic Field Laboratory
27789138	355	Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.	Abbvie Bioresearch Center
26169764	48	Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors.	China Pharmaceutical University
28254166	81	Discovery of novel BTK inhibitors with carboxylic acids.	Merck
27912175	14	Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.	Dalian Medical University
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
27956037	8	Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.	Dalian Medical University
27994757	41	Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kd.	TBA
27994736	28	Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a	Dalian Medical University
27583770	82	Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke	Bristol-Myers Squibb Research and Development
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
27210433	10	Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors.	China Pharmaceutical University
26976214	15	Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.	Kbp Biosciences
26951753	336	Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.	Novartis Institutes For Biomedical Research
26762835	342	Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).	Icahn School of Medicine At Mount Sinai
26630553	9	Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.	Chinese Academy of Sciences
26675441	46	Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.	Genentech
26396685	19	Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.	Amgen
26342867	52	Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.	Sichuan University
26320619	88	Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).	Bristol-Myers Squibb Pharmaceutical Research Institute
26344595	26	Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.	Xi'An Jiaotong University
26277759	31	Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.	China Pharmaceutical University
26258521	104	Development of Selective Covalent Janus Kinase 3 Inhibitors.	Harvard Medical School
26087137	30	Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.	Takeda California
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
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
25872980	21	TR-FRET binding assay targeting unactivated form of Bruton's tyrosine kinase.	Carna Biosciences
25701252	54	Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.	Genentech
25596757	64	Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.	China Pharmaceutical University
25630223	5	Target engagement in lead generation.	Eli Lilly
25589924	6	Novel Disubstituted Pyrimidines as Inhibitors of Bruton's Tyrosine Kinase.	Dart Neuroscience
25515957	33	Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.	China Pharmaceutical University
25466710	14	Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.	Hoffmann-La Roche
24915291	73	Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.	Peking University
24731277	2	Small chemicals with inhibitory effects on PtdIns(3,4,5)P3 binding of Btk PH domain.	Konkuk University
24685542	67	Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.	Bristol-Myers Squibb Research and Development
24900590	55	Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.	Glaxosmithkline
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
23442188	4	A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.	Graduate School of Peking Union Medical College and Chinese Academy of Medical Sciences
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
21429745	49	3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß.	Glaxosmithkline
22621397	39	Irreversible protein kinase inhibitors: balancing the benefits and risks.	Covalution Pharma
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
23098091	91	Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.	Pfizer
24900538	27	Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.	TBA
22394077	19	Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.	Hoffmann-La Roche
22320327	250	Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.	Amgen
22148921	48	Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c	Cephalon
19716697	110	The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.	Boehringer Ingelheim Pharmaceuticals
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
18321716	7	ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds.	Institute of Molecular Physiology
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
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
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
18278858	93	Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.	Amgen
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
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
21733693	7	Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.	Glaxosmithkline
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
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
21035336	42	5-amino-pyrazoles as potent and selective p38a inhibitors.	Bristol-Myers Squibb Research and Development
20684549	76	Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.	Amgen
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
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
20307980	22	B-Raf kinase inhibitors: hit enrichment through scaffold hopping.	Wyeth Research
19879134	94	Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.	Cgi Pharmaceuticals
19362830	47	Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.	Wyeth Research
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
18993068	75	Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.	Amgen
18667312	24	Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.	The Scripps Research Institute
17499505	78	Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.	Boehringer Ingelheim Pharmaceuticals
17350837	59	Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.	Amgen
16970394	147	Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.	Amgen
16686533	89	Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.	Boehringer Ingelheim Pharmaceuticals
16682193	62	Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
15711537	653	A small molecule-kinase interaction map for clinical kinase inhibitors.	Ambit Biosciences
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
28315597	85	Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.	University of Science and Technology of China
29457982	80	Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.	Genentech
28945083	33	In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.	National Institute of Biological Sciences, Beijing
28433531	69	Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.	Wuxi Apptec (Shanghai)
21612376	6	Carbonic anhydrase I and II inhibition with natural products: caffeine and piperine.	Gitam University
21438710	18	Oxamic acid analogues as LDH-C4-specific competitive inhibitors.	Instituto Politécnico Nacional
24047900	19	Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.	Vanderbilt University
20962348	17	Probing the active site of the deoxynucleotide N-hydrolase Rcl encoded by the rat gene c6orf108.	Institut Pasteur
14564311	4	Selective COX-2 inhibition and cardiovascular effects: a review of the rofecoxib development program.	University of Maryland Hospital
15293988	1	A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.	Virginia Commonwealth University
18722768	10	Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.	Anadys Pharmaceuticals
18242088	26	Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine.	Anadys Pharmaceuticals
19477642	87	Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.	Gsk
19167883	5	Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines.	Gilead Sciences
19071019	16	Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors.	Roche
18290603	5	Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase.	Vertex Pharmaceuticals
15857113	12	Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.	Gsk
17709247	33	Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.	Amgen
15755665	7	Discovery of novel non-peptidic ketopiperazine-based renin inhibitors.	Pfizer
17114291	10	Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.	Johns Hopkins University
17636946	94	Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.	Gsk
15466206	10	BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.	Bayer Pharmaceuticals
17523610	73	Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension.	Abbott Laboratories
15582402	9	Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).	University of Illinois At Chicago
17451235	19	Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design.	Astex
14592490	80	Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.	Merck Research Laboratories
16942016	27	Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.	University of Kansas
15887974	10	Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.	Universidad Central De Venezuela
15537349	18	Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.	University of Bologna
10866371	12	Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.	Glaxosmithkline
15743198	134	Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.	Saarland University
16392787	16	Anthrax lethal factor protease inhibitors: synthesis, SAR, and structure-based 3D QSAR studies.	Burnham Institute
11266159	63	3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).	Smithkline Beecham Pharmaceuticals
15771433	30	Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.	Johnson & Johnson Pharmaceutical
8568816	69	Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor Receptor	Parke-Davis Pharmaceutical Research
8642565	36	Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and oral bioavailability.	Sandoz Research Institute
	50	Potent, orally bioavailable HIV-1 protease inhibitors containing noncoded D-amino acids	Eli Lilly
8558507	7	A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.	Abbott Laboratories