141 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
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27517803	29	Optimization and biological evaluation of aminopyrimidine-based I¿B kinaseß inhibitors with potent anti-inflammatory effects.	Korea Advanced Institute of Science and Technology (Kaist)
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
27017554	4	New IKK inhibitors: Synthesis of new imidazo[1,2-a]quinoxaline derivatives using microwave assistance and biological evaluation as IKK inhibitors.	Lebanese University
26826731	28	Identification and characterization of potent, selective and metabolically stable IKKß inhibitor.	The Catholic University of Korea
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
25662701	23	Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.	Zhejiang University
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
25027934	4	Synthesis of lantadene analogs with marked in vitro inhibition of lung adenocarcinoma and TNF-a induced nuclear factor-kappa B (NF-¿B) activation.	Jaypee University of Information Technology
24980703	296	Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.	Nerviano Medical Sciences
24913714	53	Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.	Merck Research Laboratories
25369270	93	Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.	Galapagos
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24813730	20	Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKß inhibitors.	Yonsei University
24685542	67	Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.	Bristol-Myers Squibb Research and Development
23906342	14	Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.	Takeda Pharmaceutical
24457265	4	Novel lung adenocarcinoma and nuclear factor-kappa B (NF-¿B) inhibitors: synthesis and evaluation of lantadene congeners.	Jaypee University of Information Technology
24457093	12	Inhibition of I¿B kinase-ß and I¿B kinase-a by heterocyclic adamantyl arotinoids.	Universidade De Vigo
24389511	25	Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.	Zhejiang University
23994329	12	Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3ß (GSK-3ß) inhibitors.	Zhejiang University
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
23602398	43	Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.	Merck Research Laboratories
23587425	37	Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.	Merck Research Laboratories
23535330	83	Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.	Merck Research Laboratories
23501112	160	Novel IKKß inhibitors discovery based on the co-crystal structure by using binding-conformation-based and ligand-based method.	China Pharmaceutical University
23490150	48	Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.	Takeda Pharmaceutical
23301767	154	Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.	University of Nottingham
23550937	72	Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.	Emory University
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
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
19303774	87	1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.	Glaxosmithkline
19349179	47	4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.	Glaxosmithkline
23147077	23	Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.	Takeda Pharmaceutical
23142618	66	Discovery of a novel series of 4-quinolone JNK inhibitors.	Roche Palo Alto
23127890	96	SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.	Exelixis
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
22801646	49	4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.	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
22858099	52	Discovery of potent and selective rhodanine type IKKß inhibitors by hit-to-lead strategy.	Korea 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
24900358	69	Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.	TBA
21334796	4	Structure-based design and biological profile of (E)-N-(4-Nitrobenzylidene)-2-naphthohydrazide, a novel small molecule inhibitor of I¿B kinase-ß.	Universidade Federal Do Rio De Janeiro
21128646	88	Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.	Merck Research Laboratories
15975507	13	Features of selective kinase inhibitors.	University of California San Francisco
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20044255	5	Inhibition of IKK-beta: a new development in the mechanism of the anti-obesity effects of PTP1B inhibitors SA18 and SA32.	Inha University
20153204	109	Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.	Nerviano Medical Sciences
19716697	110	The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.	Boehringer Ingelheim Pharmaceuticals
17850214	99	The selectivity of protein kinase inhibitors: a further update.	University of Dundee
19394223	50	Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.	Glaxosmithkline
18501602	32	Synthesis and structure-activity relationship of aminopyrimidine IKK2 inhibitors.	Ucb Pharma
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
18313304	50	Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1).	Takeda Pharmaceutical
18088098	1	NF-kappaB-inhibiting naphthopyrones from the Fijian echinoderm Comanthus parvicirrus.	University of Aberdeen
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
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
12617920	41	Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1.	Kyoto 619-0216
22472167	11	Studies on gambogic acid (IV): Exploring structure-activity relationship with I¿B kinase-beta (IKKß).	China Pharmaceutical University
22310227	89	5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.	Glaxosmithkline
17018693	30	Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.	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
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
22018461	41	Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).	Bristol-Myers Squibb Research and Development
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
21999461	90	1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.	RhôNe-Poulenc Rorer
22037378	31824	Comprehensive analysis of kinase inhibitor selectivity.	Ambit Biosciences
21708416	59	Combination of pharmacophore model development and binding mode analyses: identification of ligand features essential for I¿B kinase-beta (IKKß) inhibitors and virtual screening based on it.	China Pharmaceutical University
21699136	16	Selectivity of kinase inhibitor fragments.	Glaxosmithkline
21705219	23	Discovery of imidazo[1,2-b]pyridazines as IKKß inhibitors. Part 3: exploration of effective compounds in arthritis models.	Daiichi Sankyo
21705217	60	Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.	Bristol-Myers Squibb
20674350	63	Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
21620699	51	Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.	Pfizer
21489792	26	Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.	Korea Institute of Science and Technology
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
21316233	33	Novel dihydrothieno[2,3-e]indazole derivatives as I&x3ba;B kinase inhibitors.	Kyorin Pharmaceutical
21236687	41	Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure-activity relationship.	Pfizer
21232950	19	Discovery of imidazo[1,2-b]pyridazines as IKKß inhibitors. Part 2: improvement of potency in vitro and in vivo.	Daiichi Sankyo
21087862	32	Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.	Bristol-Myers Squibb
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
20855207	26	Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
20817473	57	Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.	Nerviano Medical Sciences Oncology
19654408	2521	AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).	Ambit Biosciences
20675134	88	Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.	Daiichi Sankyo
20488717	4	IKKbeta inhibitors identification part II: ligand and structure-based virtual screening.	Institute of Science and Technology
20471256	53	Synthesis and biological evaluation of tricyclic anilinopyrimidines as IKKbeta inhibitors.	Pfizer
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
20361800	22	5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.	Institute of Science and Technology
20307980	22	B-Raf kinase inhibitors: hit enrichment through scaffold hopping.	Wyeth Research
19884006	47	Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.	Wyeth Research
19864136	45	Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.	Wyeth Research
19854649	49	Discovery of highly potent and selective type I B-Raf kinase inhibitors.	Wyeth Research
19914076	37	Aminopyridinecarboxamide-based inhibitors: Structure-activity relationship.	Pfizer
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
19775160	79	2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.	Takeda Pharmaceutical
19481464	41	Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.	Zhejiang University
19376699	24	Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.	Bristol-Myers Squibb Research and Development
19338355	104	From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.	University of Illinois At Chicago
19327989	40	Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.	Pfizer
19317452	155	Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.	Wyeth Research
19285872	9	IKKbeta inhibitors identification part I: homology model assisted structure based virtual screening.	Institute of Science and Technology
19035792	85	Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.	Glaxosmithkline
18815050	34	4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.	Wyeth Research
18702457	1	Inhibition of IkappaB kinase-beta and anticancer activities of novel chalcone adamantyl arotinoids.	Universidade De Vigo
18606543	68	2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.	Wyeth Research
17848581	13	Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.	Wyeth Research
17658776	109	Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.	Abbott Laboratories
17570666	64	Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).	Pfizer
17407812	2	PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta).	Inha University
17027260	41	Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.	Glaxosmithkline
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
16236504	87	Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK.	Novartis Institutes For Biomedical Research
16216497	67	Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.	Abbott Bioresearch Center
16162000	42	Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.	Takeda Pharmaceutical
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
15225718	35	Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents.	Kyoto 619-0216
15225717	23	Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 2: Improvement of in vitro activity.	Kyoto 619-0216
14698170	46	A novel series of potent and selective IKK2 inhibitors.	Celltech R&D
12672234	64	Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active 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
11934592	24	Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.	Merck Research Laboratories
9014146	35	Pharmacological properties of recombinant "diazepam-insensitive" GABAA receptors.	National Institute of Diabetes, Digestive and Kidney Diseases
8382063	12	Activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists at cloned human 5-HT1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells.	Janssen Research Foundation
8100352	4	Cloning and expression of a human somatostatin-14-selective receptor variant (somatostatin receptor 4) located on chromosome 20.	University of Toronto
8100134	109	Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics.	Mayo Foundation
2970277	11	Quantitative autoradiography of serotonin uptake sites in rat brain using [3H]cyanoimipramine.	Veterans Administration Medical Center
2850065	27	Characterization of the binding of [3H]-CGS 19755: a novel N-methyl-D-aspartate antagonist with nanomolar affinity in rat brain.	Ciba-Geigy
2848779	9	Highly potent and selective ligands for a new class H3 of histamine receptor.	UnitÉ
17040210	10	BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo.	University of Dundee