108 articles for thisTarget

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PMID	Data	Article Title	Organization
27362616	41	G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.	Universit£
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
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
26896709	113	Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.	Saarland University
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
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
25000588	72	Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit.	Abbvie Bioresearch Center
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
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
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
21797275	139	Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.	Novartis Institutes For Biomedical Research
22078216	146	2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.	Novartis Institutes For Biomedical Research
22625994	28	Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.	Kyoto University
22738630	76	Structure-based optimization of aminopyridines as PKC¿ inhibitors.	Vertex Pharmaceuticals
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
19703774	56	C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.	Wyeth Research
9677190	49	Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.	University Of California
18434148	43	Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.	Wyeth Research
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
17977729	40	Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.	Kyoto University
17350261	16	Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
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
15267232	65	Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.	Eli Lilly
15380221	58	Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.	Central Pharmaceutical Research Institute
12672248	50	Kinase inhibitors: not just for kinases anymore.	Northwestern University
12954055	47	Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.	Johnson And Johnson Pharmaceutical Research And Development
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
10999477	40	Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.	Kyoto University
10360754	26	Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.	Tartu University
	80	Synthesis and PKC inhibitory activities of balanol analogs with a cyclopentane substructure	TBA
16249345	25	Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.	Glaxosmithkline
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
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
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
21696964	12	Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.	Keio University
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
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
21035336	42	5-amino-pyrazoles as potent and selective p38a inhibitors.	Bristol-Myers Squibb Research And Development
20965724	57	Identification of potent ITK inhibitors through focused compound library design including structural information.	Nycomed
20873740	111	Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.	Nerviano Medical Sciences
20817520	40	Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.	Kyoto University
20817473	57	Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.	Nerviano Medical Sciences Oncology
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
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
19884006	47	Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.	Wyeth Research
20153643	68	Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.	Wyeth Research
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
19854645	87	Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.	Wyeth Research
19762237	58	First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.	Wyeth Research
19682896	49	C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.	Wyeth Research
8176401	21	Anti-AIDS Agents, 11. Betulinic Acid and Platanic Acid as Anti-HIV Principles from Syzigium claviflorum, and the Anti-HIV Activity of Structurally Related Triterpenoids	TBA
	77	Synthesis and protein kinase C inhibitory activities of indane analogs of balanol	TBA
	70	Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety	TBA
	40	Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanol	TBA
	4	Synthesis of bisindolylmaleimide macrocycles	TBA
	88	Novel PKC inhibitory analogs of balanol with replacement of the ester functionality	TBA
	40	Protein kinase C inhibitory activities of balanol analogs bearing carboxylic acid replacements	TBA
	2	2-aryl-indolyl maleimides - novel and potent inhibitors of protein kinase C	TBA
19447612	59	Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.	Wyeth Research
19379015	40	Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths.	National Cancer Institute-Frederick
19111463	46	Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.	Wyeth Research
19109017	4	(-)-Cercosporamide derivatives as novel antihyperglycemic agents.	Daiichi Sankyo
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
18606543	68	2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.	Wyeth Research
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
17395590	2	Minocycline down-regulates MHC II expression in microglia and macrophages through inhibition of IRF-1 and protein kinase C (PKC)alpha/betaII.	University Of Wisconsin
18072722	42	Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.	Kyoto University
17826092	37	Optimization of triarylimidazoles for Tie2: influence of conformation on potency.	Glaxosmithkline
16682193	62	Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.	Bristol-Myers Squibb Pharmaceutical Research Institute
16640328	13	Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.	Kyoto University
16216497	67	Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.	Abbott Bioresearch Center
15771419	134	Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.	Johnson & Johnson Pharmaceutical Research & Development
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
15261294	17	Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.	Michigan State University
15149684	59	3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
14552791	35	Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.	Eli Lilly
12954072	46	New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.	Georgetown University Medical Center
12941331	96	Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
12941324	66	Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.	Kyoto University
12749884	126	Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.	Eli Lilly
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.	Boehringer Ingelheim Pharmaceuticals
11909733	30	Beta-carbolines as specific inhibitors of cyclin-dependent kinases.	Institute Of Molecular And Cell Biology
11597418	47	Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.	Glaxosmithkline
11327599	25	Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.	Georgetotwn University
11266178	39	The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.	Kyoto University
11266177	26	The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.	Kyoto University
10397502	36	Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.	Stanford University
9135029	29	Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.	Georgetown University Medical Center
9003521	249	Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.	Eli Lilly
8709095	87	(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.	Eli Lilly
27943581	8	Reverse Biosynthesis: Generating Combinatorial Pools of Drug Leads from Enzyme-Mediated Fragmentation of Natural Products.	The University Of Sydney
26469307	7	Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.	University Of Leipzig
11121615	32	Synthesis and in vitro opioid activity profiles of DALDA analogues.	Clinical Research Institute Of Montreal
16236500	26	Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.	Johnson & Johnson Pharmaceutical
16279769	28	Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)- pyrazole derivatives.	Sapienza University Of Rome
15689148	19	Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.	Shanghai Institute Of Materia Medica
15664516	21	Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.	University Of Dundee
15026054	55	Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.	Cnrs