89 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
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27839918	28	Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).	Takeda California
27994755	18	Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.	Merck
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
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
26384287	65	Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.	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.	Nerviano Medical Sciences
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
25633741	67	Discovery and profiling of a selective and efficacious Syk inhibitor.	Novartis Institutes For Biomedical Research
25625541	58	Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.	Merck
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24726806	108	Syk inhibitors with high potency in presence of blood.	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.	University Of Zurich
23993776	17	Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics.	University Of Zurich
24100158	148	Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).	Nerviano Medical Sciences
24044867	86	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.	Califia Bio
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
23490150	48	Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.	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
23398373	88	Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.	Vertex Pharmaceuticals
21903390	79	Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.	Glaxosmithkline
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
22738630	76	Structure-based optimization of aminopyridines as PKC¿ inhibitors.	Vertex Pharmaceuticals
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
22289061	14	Identification of binding specificity-determining features in protein families.	Sandia National Laboratories
24900264	106	The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.	TBA
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
18183025	12060	A quantitative analysis of kinase inhibitor selectivity.	Ambit Biosciences
18823784	38	Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors.	Kissei Pharmaceutical
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University Of Oxford
17997320	29	Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.	Kissei Pharmaceutical
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
17095233	45	Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.	Kissei Pharmaceutical
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
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
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
21794960	194	Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.	Universit£
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
21620699	51	Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.	Pfizer
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
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
20873740	111	Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.	Nerviano Medical Sciences
20817473	57	Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.	Nerviano Medical Sciences Oncology
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
20483608	139	New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.	Novartis Institute Of Biomedical Research
19879134	94	Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.	Cgi Pharmaceuticals
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
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
19674816	31	Discovery of potential ZAP-70 kinase inhibitors: pharmacophore design, database screening and docking studies.	Gvk Biosciences
19427203	28	Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.	Johnson & Johnson Pharmaceutical Research & Development
	5	Non-peptide itam mimics as ZAP-70 antagonists	TBA
18986805	39	Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.	Astrazeneca Pharmaceuticals
18938080	102	Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).	Vertex Pharmaceuticals
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.	Kissei Pharmaceutical
17185414	30	Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.	Genomics Institute Of The Novartis Research Foundation
17350837	59	Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.	Amgen
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.	Amgen
16970394	147	Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.	Amgen
16682193	62	Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.	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.	Abbott Bioresearch Center
15566298	34	The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.	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.	Bristol-Myers Squibb Pharmaceutical Research Institute
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
12139450	29	Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
12086485	10	Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.	Boehringer Ingelheim Pharmaceuticals
12039590	51	Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.	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.	Ariad Pharmaceuticals
11012021	69	Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.	Basf Bioresearch
10612598	29	4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.	Celltech Therapeutics
10571165	30	Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70.	Ariad Pharmaceuticals
9871587	8	Solid phase synthesis of a biased mini tetrapeptoid-library for the discovery of monodentate ITAM mimics as ZAP-70 inhibitors.	Preclinical Research Novartis
28043720	9	Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.	China Pharmaceutical University
27231830	27	Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.	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.	The University Of Texas
15590769	16	Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors.	I.G.B.M.C.
21609408	6	Pyrone-based inhibitors of metalloproteinase types 2 and 3 may work as conformation-selective inhibitors.	University Of California San Diego
16632353	14	Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.	Abbott Laboratories
15808463	35	Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.	Abbott Laboratories