355 articles for thisTarget

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PMID	Data	Article Title	Organization
28005359	66	Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.	Newcastle University
28109791	44	Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.	Chugai Pharmaceutical
28049589	159	A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.	Sri International
28280261	84	Non-kinase targets of protein kinase inhibitors.	The University of Sydney
27643641	1	[1,2]Oxazolo[5,4-e]isoindoles as promising tubulin polymerization inhibitors.	Universit£
27391135	28	3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents.	Egyptian Russian University
27171036	164	Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.	University of Nebraska Medical Center
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
26900761	4	Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS).	Monash University (Parkville Campus)
27189674	84	RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.	Beni-Suef University
26851505	65	5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.	Palack£
26741853	95	Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.	University of Tours
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
26318056	25	Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.	Universit£
26318067	34	Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.	Hanyang University
26115571	38	Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.	Eli Lilly
25262942	189	Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.	Astrazeneca
25768699	1	Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action.	Universit£
24811300	20	Biased and unbiased strategies to identify biologically active small molecules.	Institut De Chimie Des Substances Naturelles
25589930	62	Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.	Lexicon Pharmaceuticals
24798019	30	Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.	Institut De Chimie Des Substances Naturelles
24793884	151	Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.	Amgen
24773549	20	Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.	Development Center For Biotechnology
24641103	104	Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.	Amgen
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
24417566	43	Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).	Icahn School of Medicine At Mount Sinai
24120542	90	The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.	Amgen
24185375	76	Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.	University of Nottingham
24157370	22	The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.	Chugai Pharmaceutical
24044867	86	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.	Califia Bio
23919303	3	Novel 1H-pyrrolo[2,3-b]pyridine derivative nortopsentin analogues: synthesis and antitumor activity in peritoneal mesothelioma experimental models.	Universit£
23994326	9	6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity.	Universit£
23933045	20	Synthesis, biological evaluation and molecular docking studies of pyrazole derivatives coupling with a thiourea moiety as novel CDKs inhibitors.	Nanjing University
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
23829517	30	A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.	Palack£
23600925	12	Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.	H. Lee Moffitt Cancer Center and Research Institute
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
23399722	30	Synthesis and biological evaluation of guanidino analogues of roscovitine.	Palack£
23354070	18	Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.	Universitat De Barcelona
23252711	46	Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.	University of Oxford
23218601	100	Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling.	University of Paris
20146435	60	Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors.	University of St. Andrews
24900493	12	Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.	TBA
22995819	4	Synthesis and evaluation of novel anti-proliferative pyrroloazepinone and indoloazepinone oximes derived from the marine natural product hymenialdisine.	TBA
20627562	1	Cell cycle arrest and cytochrome c-mediated apoptotic induction by MCS-5A is associated with up-regulation of p16(INK4a) in HL-60 cells.	Kyunggi-Do
19879023	1	Synthesis and cytotoxic activity of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidine derivatives.	Universidad Nacional Aut£Noma De M£Xico
18232654	8	Pyrrolo[2,3-a]carbazoles as potential cyclin dependent kinase 1 (CDK1) Inhibitors. Synthesis, biological evaluation, and binding mode through docking simulations.	University of Patras
23082860	69	Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.	The Institute of Cancer Research
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
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
21381769	56	Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.	Universite£
24936234	42	Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist.	TBA
23083119	57	Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.	Universit£
23063403	21	Recent results in protein kinase inhibition for tropical diseases.	Montclair State University
23039927	44	Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.	Martin-Luther-University Halle-Wittenberg
23021994	108	Identification of pyrimidine derivatives as hSMG-1 inhibitors.	Pfizer
22548342	210	Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.	Exelixis
23085105	30	Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents.	University of Nottingham
22795331	51	Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.	Janssen Pharmaceutical Companies of Johnson & Johnson
24900482	32	Targeted kinase selectivity from kinase profiling data.	TBA
22372864	25	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.	Hanmi Research Center
22607669	45	Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors.	Biogen Idec
24900346	90	Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.	TBA
22326168	67	Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1.	Biogen Idec
24900361	27	Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.	TBA
21353571	26	Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.	Hanyang University
16584130	95	Selectivity and potency of cyclin-dependent kinase inhibitors.	Georgetown University
15559249	55	Pharmacological inhibitors of glycogen synthase kinase 3.	The Rockefeller University
18469809	41	A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.	Nerviano Medical Sciences Oncology
20627564	51	Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases.	Walter Reed Army Institute of Research
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
20097066	53	Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.	Schering-Plough Research Institute
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
19906467	109	Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).	Technische Universit£T Braunschweig
19397322	58	Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.	National Cancer Institute-Bethesda
19522465	102	Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).	Boehringer Ingelheim Pharma
9677190	49	Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.	University of California
18816110	27	Soluble 3',6-substituted indirubins with enhanced selectivity toward glycogen synthase kinase -3 alter circadian period.	University of Athens
18639462	22	Nitrogen-containing flavonoid analogues as CDK1/cyclin B inhibitors: synthesis, SAR analysis, and biological activity.	Dalian University of Technology
18077425	197	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.	Harvard Medical School
17360485	10	Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.	Millennium Pharmaceuticals
18077363	314	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.	University of Oxford
18271520	423	Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.	University of Zurich
18191399	57	Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases.	University of Auckland
17935989	146	Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.	Abbott Laboratories
17887663	34	Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.	Pfizer
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
16451062	46	Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.	Astrazeneca
15163202	16	Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.	Vanderbilt University School of Medicine
12593668	6	Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties.	Martin-Luther-University Halle-Wittenberg
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
12930149	37	Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinases.	Institute of Research
12477352	85	Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.	Novartis Pharma
11063606	137	3D-QSAR CoMFA on cyclin-dependent kinase inhibitors.	Institut Curie
12941319	15	2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors.	Academy of Sciences of The Czech Republic
12392733	13	Synthesis and biological activity of olomoucine II.	Palack£
10843211	38	Structure-activity relationship studies of flavopiridol analogues.	Mitotix
9990463	69	2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.	Novartis Pharmaceuticals
16476733	18	Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.	University of Queensland
22269278	50	Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.	Chugai Pharmaceutical
15953730	13	RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.	Hoffmann-La Roche
22169262	26	Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.	Shenyang Pharmaceutical University
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
22036212	8	Synthesis of 6-(het) ary Xylocydine analogues and evaluating their inhibitory activities of CDK1 and CDK2 in vitro.	Jilin University
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
21986585	2	A modular approach to trim cellular targets in anticancer drug discovery.	Instituto Universitario De Bio-Org£Nica Antonio Gonz£Lez (Iubo-Ag)
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
21907583	48	CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.	University of South Florida
21798738	44	Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).	Biogen Idec
20810192	1	Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities--development of highly efficacious cytotoxic agents.	Guru Nanak Dev University
21684737	48	Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors.	Keimyung University
21627121	22	Irreversible Nek2 kinase inhibitors with cellular activity.	University of California
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
20630752	40	Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.	Millennium Pharmaceuticals
20621478	37	Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.	Trinity College
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
21174434	13	Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.	Cylene Pharmaceuticals
20965724	57	Identification of potent ITK inhibitors through focused compound library design including structural information.	Nycomed
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
20684549	76	Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.	Amgen
20638755	15	Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay.	University of Jordan
20188579	42	Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.	Temple University
18559524	21	BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.	Boehringer Ingelheim Austria
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
20363627	56	Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.	Universit£
20361800	22	5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.	Institute of Science and Technology
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
20167481	66	Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.	Sanofi-Aventis
20166671	85	Selectively nonselective kinase inhibition: striking the right balance.	Schering-Plough
20137943	60	Azole-based inhibitors of AKT/PKB for the treatment of cancer.	Amgen
19994845	4	Synthesis and antiproliferative activity of 7-azaindirubin-3'-oxime, a 7-aza isostere of the natural indirubin pharmacophore.	University of Athens
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
20097074	5	New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme.	Schering-Plough Research Institute
20093027	92	Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.	Chugai Pharmaceutical
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
19926477	100	2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.	Abbott Laboratories
19954867	2	Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors.	Institute of Radiopharmacy
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
19616945	55	Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency.	Pfizer
19616942	45	Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency.	Pfizer
19203813	48	Synthesis and biological evaluation of 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as a novel class of potential anti-tumor agents.	National Organization For Drug Control and Research
18842409	28	A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.	Sunesis Pharmaceuticals
	4	Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK II	TBA
	42	A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation	TBA
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
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
19286381	23	Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.	Johnson & Johnson Pharmaceutical Research & Development
18996007	30	The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing.	Astrazeneca Pharmaceuticals
18926699	30	Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.	Sunesis Pharmaceuticals
18718756	44	7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.	Johnson & Johnson Pharmaceutical Research and Development
18678484	57	A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.	Johnson & Johnson Pharmaceutical Research and Development
18625560	3	Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.	Piramal Life Sciences
18606543	68	2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.	Wyeth Research
18586356	40	Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors.	Université
18494457	160	4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4).	Wyeth Research
18393402	2	Natural products as leads to potential drugs: an old process or the new hope for drug discovery?	National Cancer Institute-Frederick
17981370	45	Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.	Université
17869387	158	Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.	University of Auckland
17395594	10	Cellular characterization of a novel focal adhesion kinase inhibitor.	University of Virginia
11325241	2	Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species.	Harbor Branch Oceanographic Institution
18353638	71	Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors.	Keimyung University
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
17606372	66	5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.	Bristol-Myers Squibb Pharmaceutical Research Institute
17532631	105	Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.	Johnson & Johnson Pharmaceutical Research & Development
17481894	64	4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.	Johnson & Johnson Pharmaceutical Research and Development
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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
17270437	68	New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.	Bristol-Myers Squibb Pharmaceutical Research Institute
17178224	28	3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.	Keimyung University
16870444	23	Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.	Johnson & Johnson Pharmaceutical Research & Development
16682186	16	Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.	Johnson & Johnson Pharmaceutical Research & Development
16682184	25	Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9.	Banyu Tsukuba Research Institute
16644220	29	Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3.	Université
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15149684	59	3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
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14552791	35	Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.	Eli Lilly
12941331	96	Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.	Johnson & Johnson Pharmaceutical Research & Development
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11378364	34	Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.	Research Biomet. Glaxo Wellcome Medicines Research Centre
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10741555	9	2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity.	UniversitäT Hamburg
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31514062	80	Recent advances in the development of cyclin-dependent kinase 7 inhibitors.	Tianjin University of Science and Technology
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30986571	66	Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.	Zhejiang University
30909021	21	Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore.	Jamia Hamdard
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31693351	473	Discovery of 4	TBA
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9871700	15	Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure.	Kyushu University
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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
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25835357	22	Novel arylazopyrazole inhibitors of cyclin-dependent kinases.	Palack�
25368960	17	Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity.	De Montfort University
24304238	22	8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode.	University of Oxford
31200237	95	Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.	Shanghai Pharmaceuticals Holding
28911822	24	Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.	Central University of Punjab
28803677	5	Indole-fused azepines and analogues as anticancer lead molecules: Privileged findings and future directions.	Babasaheb Bhimrao Ambedkar University
30197029	27	Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors.	Jiangnan University
29985601	64	Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.	Seoul National University
30253346	46	Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.	Chinese Academy of Sciences
29247857	102	A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.	Beijing Normal University
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
29549836	47	Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.	Universit£
29547832	12	New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors.	Universit£
29459274	69	Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.	Shanghai Haihe Pharmaceutical
28688277	2	Synthesis, antitumor activity and CDK1 inhibiton of new thiazole nortopsentin analogues.	Universit£
29429832	77	Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships.	Beijing University of Technology
29273417	26	An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.	University of Kwazulu-Natal
29074254	52	Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors.	Shanghai Haihe Pharmaceutial
29107425	90	Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.	Korea Institute of Science & Technology (Kist)
29853338	31	Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells.	Shihezi University
29357250	80	Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.	China Pharmaceutical University
29370702	41	Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.	Csir-Indian Institute of Integrative Medicine
28827110	54	Synthesis and biological evaluation of N9-cis-cyclobutylpurine derivatives for use as cyclin-dependent kinase (CDK) inhibitors.	Korea Research Institute of Chemical Technology
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
28557430	45	Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.	University of Kaiserslautern
34651447	87	A patent review on SARS coronavirus main protease (3CLpro) inhibitors.	Experimental Drug Development Centre
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
24327656	9	The molecular chaperone Hsp70 activates protein phosphatase 5 (PP5) by binding the tetratricopeptide repeat (TPR) domain.	University of Michigan
25346381	6	Identification of Novel Selective Lysine-Specific Demethylase 1 (LSD1) Inhibitors Using a Pharmacophore-Based Virtual Screening Combined with Docking.	China Pharmaceutical University
23603658	33	Structure-guided design of a selective BCL-X(L) inhibitor.	Walter and Eliza Hall Institute of Medical Research
22296826	4	New active HIV-1 protease inhibitors derived from 3-hexanol: conformation study of the free inhibitors in crystalline state and in complex with the enzyme.	Technical University of LÓDz
16242653	33	A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.	Gpc Biotech
19572549	30	Identification of inhibitors of checkpoint kinase 1 through template screening.	The Institute of Cancer Research
19200745	35	Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.	Takeda Pharmaceutical
19603809	59	Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor.	Nerviano Medical Sciences
19128055	24	Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.	Universite De Lyon
19143567	49	Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.	Astex
18307303	75	Discovery of selective aminothiazole aurora kinase inhibitors.	Novartis
17098432	10	Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).	Paradigm Pharmaceuticals
18656911	39	Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.	Astex
12244092	12	Structural basis for Chk1 inhibition by UCN-01.	Glaxosmithkline
16289938	24	Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.	Vernalis (R&D)
15974586	29	Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.	Vernalis (R&D)
17064073	78	Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.	Hoffmann-La Roche
16290148	44	3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.	Nerviano Medical Sciences
17064068	36	4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.	Palacky University
11170642	12	Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.	Lawrence Berkeley National Laboratory
16325401	25	Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.	Vernalis (R&D)
15026054	55	Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.	Cnrs
12941317	25	Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.	Glaxosmithkline
15261277	30	Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.	Cyclacel
11881998	32	First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease.	Instituto De Quimica Medica (Csic)
11728181	188	Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.	Glaxosmithkline
15189033	48	3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.	Pharmacia Italia
15837297	33	3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.	Johnson & Johnson Pharmaceutical
15974571	62	1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.	Johnson & Johnson Pharmaceutical
12747775	56	Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.	Eli Lilly
15546737	59	Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.	Avenida De La Industria
15780638	45	Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.	Eli Lilly
11741480	41	A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues.	Banyu Tsukuba Research Institute
15771433	30	Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.	Johnson & Johnson Pharmaceutical
16033269	98	Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.	Johnson & Johnson Pharmaceutical
15801830	127	Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.	Pfizer
15993068	101	2-Aminoquinazoline inhibitors of cyclin-dependent kinases.	Naeja Pharmaceutical
11101352	88	Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.	Parke-Davis Pharmaceutical Research
15537345	171	Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.	Bristol-Myers Squibb
12643928	24	1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.	Bristol-Myers Squibb
12824044	41	1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.	Bristol-Myers Squibb
15125971	24	Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.	Bristol-Myers Squibb
11063609	36	Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.	Bristol-Myers Squibb Pharmaceutical Research Institute
12190313	94	Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.	Bristol-Myers Squibb Pharmaceutical Research Institute
9357527	141	Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines.	Novartis Pharmaceuticals