216 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
28692292	73	Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.	Sichuan University and Collaborative Innovation Center For Biotherapy
28279847	40	Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.	Carna Biosciences
28011204	65	Structure-guided development of covalent TAK1 inhibitors.	Harvard Medical School
27816515	143	Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.	Merck
27994729	18	Macrocyclic Inhibitors of ERK2 Kinase.	Dart Neuroscience
27078757	121	Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).	Astrazeneca
27288183	130	Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.	Southeast University
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
27106711	87	Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).	Green Valley Research Institute
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
26733474	5	Identification of allosteric ERK2 inhibitors through in silico biased screening and competitive binding assay.	Osaka Prefecture 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
26338362	40	Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.	Genentech
26298497	4	Recent progress on MAP kinase pathway inhibitors.	Ontario Institute For Cancer Research
26259804	23	Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase.	Novartis Institutes For Biomedical Research
26144345	16	Ligand efficient tetrahydro-pyrazolopyridines as inhibitors of ERK2 kinase.	Novartis Institutes For Biomedical Research
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
25730262	195	10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.	Technische Universit£T Braunschweig
25977981	76	Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.	TBA
25778995	63	Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38aMAPK and ERK1/2 inhibitory activity.	Cairo 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
25763473	108	The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.	Entremed
25603482	54	Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.	Array Biopharma
25716905	38	Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors.	Merck Research Laboratories
25022204	78	Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.	Universit£
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
25589930	62	Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.	Lexicon Pharmaceuticals
25529738	4	5Z-7-Oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner.	Osaka Prefecture University
25462247	20	In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.	Fudan University
25313996	91	Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.	Merck Research Laboratories
24813737	107	Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.	Array Biopharma
24139169	175	Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.	Nerviano Medical Sciences
24650640	43	Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.	Martin-Luther-University Halle-Wittenberg
24100158	148	Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).	Nerviano Medical Sciences
24125851	48	Novel acetamidothiazole derivatives: synthesis and in vitro anticancer evaluation.	University of Mansoura
24044867	86	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.	Califia Bio
23352510	37	Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.	Roche Palo Alto
23920481	25	Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.	The Institute of Cancer Research
24900713	3	ERK2 Inhibitors May Provide Treatment for Cancer.	Therachem Research Medilab (India)
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
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
23419007	8	Incorporation of rapid thermodynamic data in fragment-based drug discovery.	The University of Tokyo
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
19303774	87	1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.	Glaxosmithkline
17194588	92	N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.	Glaxosmithkline
22621397	39	Irreversible protein kinase inhibitors: balancing the benefits and risks.	Covalution Pharma
23103095	125	Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.	Abbott Laboratories
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
24936234	42	Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist.	TBA
23116168	42	Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.	Sichuan University
22727637	85	Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.	Abbott Laboratories
22554206	33	Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.	Pfizer
22168626	32	Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.	Ambit Biosciences
24900264	106	The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.	TBA
21353571	26	Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.	Hanyang University
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
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20138512	82	Discovery of potent and bioavailable GSK-3beta inhibitors.	Roche Palo Alto
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
20038108	19	Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.	Wyeth Research
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
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
18221871	24	Pyrazinoindolone inhibitors of MAPKAP-K2.	Boehringer Ingelheim Pharmaceuticals
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
16460940	13	Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.	Hoffmann-La Roche
11784156	20	Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1).	University of Utah
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
16249345	25	Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.	Glaxosmithkline
15953730	13	RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.	Hoffmann-La Roche
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
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
21982796	108	Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.	The Institute of Cancer Research
22014755	36	Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.	Hanyang University
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
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
21813278	95	Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.	Elan Pharmaceuticals
20674350	63	Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.	Merck Research Laboratories
21080703	20	A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.	Imperial College
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
24900231	22	Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.	TBA
21316234	133	Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.	Elan Pharmaceuticals
21273066	83	Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.	National University of Ireland
24900250	81	Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277	TBA
21112785	151	Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.	Elan Pharmaceuticals
21071223	190	Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.	Elan Pharmaceuticals
21038853	133	4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.	Novartis Institutes For Biomedical Research
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
20462263	127	Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.	Cyclacel
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
19894727	164	Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.	Wyeth Research
20346655	117	Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.	Abbott Laboratories
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
20188552	75	Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).	Wyeth Research
19884006	47	Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.	Wyeth Research
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
20141146	234	Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.	Nerviano Medical Sciences
19945867	39	Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.	Taisho Pharmaceutical
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19888761	52	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.	Hanmi Research Center
19877644	6	Identification of death-associated protein kinases inhibitors using structure-based virtual screening.	Pharmadesign
19361991	80	Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.	Vertex Pharmaceuticals
19414255	58	Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.	Vertex Pharmaceuticals
19364658	113	Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).	Wyeth Research
18835158	9	Identification of novel inhibitors of extracellular signal-regulated kinase 2 based on the structure-based virtual screening.	Sejong University
18606543	68	2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.	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
17303421	56	Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.	Roche Research Center
17287122	79	Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.	Abbott Laboratories
17000106	4	Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.	University of Maryland
16516473	444	Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.	Astrazeneca
16366598	51	(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.	Johnson & Johnson Pharmaceutical Research and Development
16242327	4	Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative.	Fujisawa Pharmaceutical
15999996	3	Identification of novel extracellular signal-regulated kinase docking domain inhibitors.	University of Maryland
15999992	25	Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.	Johnson & Johnson Pharmaceutical Research and Development
15261294	17	Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.	Michigan State University
12941331	96	Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
12086491	116	Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.	Pharmaceutical Research Institute
12036347	116	Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.	Aventis Pharma Deutschland
31757666	314	Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.	Merck
27491711	422	Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.	Merck And
27329786	68	Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.	Merck
27227380	86	Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.	Array Biopharma
30755337	95	Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.	Japan Tobacco
30707835	18	Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase I? and ?.	Korea Institute of Science and Technology
30605831	39	Discovery of potent, orally bioavailable ERK1/2 inhibitors with isoindolin-1-one structure by structure-based drug design.	China Pharmaceutical University
31550662	109	Progress in the development of more effective and safer analgesics for pain management.	University of Catania
31693351	473	Discovery of 4	TBA
31381325	46	Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.	Chengdu University
29400967	136	Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.	Bristol-Myers Squibb
30763817	39	Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.	University of Naples Federico Ii
30384048	365	ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.	University of Florida
31710489	55	Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).	Astrazeneca
26505898	123	Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.	Novartis Institutes For Biomedical Research
26509640	234	Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.	Abbvie Bioresearch Center
30082069	359	ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.	Vertex Pharmaceuticals
29945794	193	ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.	Vertex Pharmaceuticals
29748051	24	Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.	Merck
29545102	159	Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.	Merck
30034615	46	MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.	Merck
29775310	22	Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.	Astex Pharmaceuticals
29107425	90	Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.	Korea Institute of Science & Technology (Kist)
29510947	20	A combination of	The University of Tokyo
28376306	145	Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.	Astrazeneca
28740606	9	Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.	Sanford Burnham Prebys Medical Discovery Institute
28351607	43	Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth.	The University of Texas At Austin
29016121	44	Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.	Novartis Institutes For Biomedical Research
28714692	232	Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.	University of Chinese Academy of Sciences
22957720	5	Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.	Ankara University
21381887	3	Synthesis and biological evaluation of fused oxepinocoumarins as free radicals scavengers.	Aristotle University of Thessaloniki
20807084	24	Hyperbolic mixed-type inhibition of acetylcholinesterase by tetracyclic thienopyrimidines.	University of Bonn
	18	Efficient synthesis of novel dialkyl-3-cyanopropylphosphate derivatives and evaluation of their anticholinesterase activity	University of Carthage
27607918	4	Targeting Bacterial Nitric Oxide Synthase with Aminoquinoline-Based Inhibitors.	University of California Irvine
19170619	14	Design of a carbonic anhydrase IX active-site mimic to screen inhibitors for possible anticancer properties.	University of Florida
11961071	4	Agonist, antagonist, and inverse agonist characteristics of TIPP (H-Tyr-Tic-Phe-Phe-OH), a selective delta-opioid receptor ligand.	University of Arkansas
9400006	184	Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.	Emory University
8398139	29	A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms.	The Scripps Research Institute
1857334	1	Cloning and expression of an A1 adenosine receptor from rat brain.	National Institute of Mental Health
17168554	15	Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist.	University of California San Francisco
19170521	30	Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.	Universita Di Siena
19119014	12	Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference.	Universita Degli Studi Di Firenze
16640335	39	Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX.	University of Namur
15115390	8	Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.	Merck Research Laboratories
15755666	18	Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.	Biocryst Pharmaceuticals
7658435	49	Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor.	University of Auckland