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89 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
27839918 28 Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).EBI Takeda California, Inc.
27994755 18 Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.EBI Merck& Co.
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.EBI Nerviano Medical Sciences Srl
26951753 336 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI 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).EBI Icahn School of Medicine at Mount Sinai
26384287 65 Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.EBI Kangwon National 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.EBI Nerviano Medical Sciences Srl
26071372 89 Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI Astellas Pharma Inc.
26005534 158 (R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.EBI Genomics Institute of the Novartis Research Foundation
25633741 67 Discovery and profiling of a selective and efficacious Syk inhibitor.EBI Novartis Institutes for Biomedical Research
25625541 58 Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.EBI Merck & Co., Inc.
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24726806 108 Syk inhibitors with high potency in presence of blood.EBI Novartis Institutes for Biomedical Research
24569110 11 Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk.EBI University of Zurich
23993776 17 Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics.EBI University of Zurich
24100158 148 Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI Nerviano Medical Sciences S.r.l.
24044867 86 Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI Califia Bio Inc.
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 EBI Genomics Institute of the Novartis Research Foundation
23490150 48 Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI Takeda Pharmaceutical Co., Ltd
23394126 170 Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI Exelixis
23398373 88 Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.EBI Vertex Pharmaceuticals (Europe) Ltd.
21903390 79 Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.EBI GlaxoSmithKline R&D
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.EBI Takeda Pharmaceutical Co. Ltd
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd
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.EBI Takeda Pharmaceutical Company Limited
22289061 14 Identification of binding specificity-determining features in protein families.EBI Sandia National Laboratories
24900264 106 The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.EBI TBA
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
18823784 38 Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors.EBI Kissei Pharmaceutical Company Ltd
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
17997320 29 Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.EBI Kissei Pharmaceutical Company Ltd
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.EBI Amgen Inc.
17095233 45 Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.EBI Kissei Pharmaceutical Company Ltd
16876403 85 Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
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.EBI Ludwig-Maximilians University of Munich
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).EBI Ansaris
21794960 194 Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.EBI Universit£ di Bologna
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI 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.EBI Novartis Institute for BioMedical Research
21620699 51 Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI Pfizer Inc.
21470862 110 NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.EBI Nerviano Medical Sciences srl
21391610 139 Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.EBI Vertex Pharmaceuticals (Europe) Ltd.
24900250 81 Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI TBA
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences Srl
20817473 57 Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI Nerviano Medical Sciences-Oncology
20684549 76 Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI Amgen Inc.
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
19879134 94 Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI CGI Pharmaceuticals, Inc.
20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences Srl
19945869 7 Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR.EBI Taisho Pharmaceutical Co., Ltd
19945867 39 Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.EBI Taisho Pharmaceutical Co., Ltd
19674816 31 Discovery of potential ZAP-70 kinase inhibitors: pharmacophore design, database screening and docking studies.EBI GVK Biosciences Pvt. Ltd.
19427203 28 Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.EBI Johnson& Johnson Pharmaceutical Research& Development L.L.C. 920 Route 202
 5 Non-peptide itam mimics as ZAP-70 antagonistsEBI TBA
18986805 39 Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.EBI AstraZeneca Pharmaceuticals
18938080 102 Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).EBI Vertex Pharmaceuticals, Inc.
18585046 32 A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.EBI Kissei Pharmaceutical Company Ltd
17185414 30 Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.EBI Genomics Institute of the Novartis Research Foundation
17350837 59 Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.EBI Amgen Inc.
17280833 52 Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.EBI Amgen Inc.
16970394 147 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen, Inc.
16682193 62 Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
15566298 34 The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.EBI Bristol-Myers Squibb
15317463 16 Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
12139450 29 Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals Inc.
12086485 10 Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.EBI Boehringer Ingelheim Pharmaceuticals
12039590 51 Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI Abbott Bioresearch Center
11527723 32 A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain.EBI ARIAD Pharmaceuticals, Inc.
11012021 69 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.EBI BASF Bioresearch Corporation
10612598 29 4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.EBI Celltech Therapeutics Limited
10571165 30 Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70.EBI ARIAD Pharmaceuticals, Inc.
9871587 8 Solid phase synthesis of a biased mini tetrapeptoid-library for the discovery of monodentate ITAM mimics as ZAP-70 inhibitors.EBI Preclinical Research Novartis
28043720 9 Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.BDB China Pharmaceutical University
27231830 27 Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.BDB AIMST University
19663506 21 Developing dual and specific inhibitors of dimethylarginine dimethylaminohydrolase-1 and nitric oxide synthase: toward a targeted polypharmacology to control nitric oxide.BDB The University of Texas
15590769 16 Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.BDB I.G.B.M.C.
21609408 6 Pyrone-based inhibitors of metalloproteinase types 2 and 3 may work as conformation-selective inhibitors.BDB University of California at San Diego
16632353 14 Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.BDB Abbott Laboratories
15808463 35 Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.BDB Abbott Laboratories