The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28291695 |
36 |
Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy. |
Takeda California |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
28005359 |
66 |
Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines. |
Newcastle University |
28131714 |
119 |
Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-a/ß. |
Novartis Institutes For Biomedical Research |
28109791 |
44 |
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. |
Chugai Pharmaceutical |
28039836 |
41 |
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities. |
East China Normal University |
28039837 |
21 |
Explicit treatment of active-site waters enhances quantum mechanical/implicit solvent scoring: Inhibition of CDK2 by new pyrazolo[1,5-a]pyrimidines. |
Masaryk University |
28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
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 |
27363938 |
2 |
A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties. |
India Academy of Scientific & Innovative Research (Acsir) |
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 |
27297568 |
50 |
Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy. |
University of South Carolina |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
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 |
27055065 |
92 |
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. |
The Institute of Cancer Research |
27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang 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 |
27117263 |
51 |
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors. |
Takeda Pharmaceutical |
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 |
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£ |
26706349 |
12 |
Synthesis and pharmacological evaluation of dehydroabietic acid thiourea derivatives containing bisphosphonate moiety as an inducer of apoptosis. |
Southeast University |
26706352 |
2 |
Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents. |
Egyptian Russian University |
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 |
26614408 |
106 |
Identification of azabenzimidazoles as potent JAK1 selective inhibitors. |
Astrazeneca |
25914804 |
20 |
Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9. |
Chinese Academy of Medical Sciences and Peking Union Medical College |
26408454 |
51 |
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis. |
University of South Australia |
26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
26320619 |
88 |
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
26318067 |
34 |
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
Hanyang University |
26316466 |
8 |
Discovery of novel nonpeptide allosteric inhibitors interrupting the interaction of CDK2/cyclin A3 by virtual screening and bioassays. |
Dalian Medical University |
26222319 |
192 |
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. |
Nerviano Medical Sciences |
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 |
25007344 |
73 |
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics. |
Christian-Albrechts-University of Kiel |
25730262 |
195 |
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A. |
Technische Universit£T Braunschweig |
26071372 |
89 |
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3. |
Astellas Pharma |
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 |
25738750 |
84 |
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. |
Astrazeneca |
25827523 |
275 |
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors. |
Vertex Pharmaceuticals |
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 |
25383627 |
85 |
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation. |
Genentech |
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 |
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 |
24798019 |
30 |
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors. |
Institut De Chimie Des Substances Naturelles |
25010935 |
1 |
Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents. |
Jamia Hamdard (Hamdard University) |
24973661 |
10 |
9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma. |
Technische Universit£T Braunschweig |
24793884 |
151 |
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. |
Amgen |
24681986 |
42 |
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
Siedlce University of Natural Sciences and Humanities |
24462666 |
105 |
Discovery of 6-aryl-azabenzimidaoles that inhibit the TBK1/IKK-e kinases. |
Astrazeneca |
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 |
24295046 |
1 |
Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3ß inhibitors. |
Universit£ |
24256217 |
177 |
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). |
The Institute of Cancer Research |
24332088 |
79 |
Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor. |
Merck Research Laboratories |
24286762 |
34 |
Fragment based discovery of arginine isosteres through REPLACE: towards non-ATP competitive CDK inhibitors. |
University of South Carolina |
24120542 |
90 |
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7. |
Amgen |
23454515 |
66 |
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. |
Universit£ |
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 |
23481650 |
78 |
N-substituted azaindoles as potent inhibitors of Cdc7 kinase. |
Amgen |
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 |
23362959 |
72 |
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo. |
Sichuan University |
23249297 |
75 |
Trimeric hemibastadin congener from the marine sponge Ianthella basta. |
Heinrich-Heine University |
24900658 |
10 |
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors. |
Hoffmann-La Roche |
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 |
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 |
22910137 |
1 |
Synthesis and identification of novel indolo[2,3-a]pyrimido[5,4-c]carbazoles as a new class of anti-cancer agents. |
TBA |
21764580 |
51 |
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3ß inhibitors. |
Glaxosmithkline |
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 |
23099093 |
84 |
Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases. |
Mrc Technology |
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£ |
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 |
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 |
22746295 |
91 |
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach. |
Teijin Pharma |
23021994 |
108 |
Identification of pyrimidine derivatives as hSMG-1 inhibitors. |
Pfizer |
22554206 |
33 |
Discovery of pyrroloaminopyrazoles as novel PAK inhibitors. |
Pfizer |
24900464 |
66 |
Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization. |
TBA |
22738630 |
76 |
Structure-based optimization of aminopyridines as PKC¿ inhibitors. |
Vertex Pharmaceuticals |
22404346 |
52 |
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. |
The Institute of Cancer Research |
22339472 |
148 |
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth |
S Bio |
24900442 |
51 |
Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode. |
TBA |
22437109 |
31 |
2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1. |
S*Bio |
24900264 |
106 |
The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor. |
TBA |
22305584 |
145 |
Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKe kinases. |
Astrazeneca R&D Boston |
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 |
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 |
20932759 |
100 |
4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors. |
Nerviano Medical Sciences |
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 |
20621725 |
9 |
Structure-based optimization of potent PDK1 inhibitors. |
Nerviano Medical Sciences |
20627564 |
51 |
Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases. |
Walter Reed Army Institute of Research |
20000735 |
12 |
Through the"gatekeeper door": exploiting the active kinase conformation. |
Nerviano Medical Sciences |
20138514 |
93 |
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta. |
Vertex Pharmaceuticals |
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 |
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 |
20030405 |
7 |
Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode. |
Peking University |
19854650 |
70 |
Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II. |
Amri |
19846305 |
86 |
Biaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part I. |
Amri |
19778024 |
31 |
Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development. |
Bristol-Myers Squibb |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
17850214 |
99 |
The selectivity of protein kinase inhibitors: a further update. |
University of Dundee |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
9677190 |
49 |
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. |
University of California |
14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
18789685 |
172 |
Kinase array design, back to front: biaryl amides. |
Glaxosmithkline |
18321716 |
7 |
ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds. |
Institute of Molecular Physiology |
18680271 |
8 |
NMR screening for lead compounds using tryptophan-mutated proteins. |
Institute For Biochemistry |
18359226 |
50 |
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors. |
Bristol-Myers Squibb Research and Development |
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 |
18232649 |
60 |
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex. |
University of Oxford |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
17339109 |
33 |
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. |
Astellas Pharma |
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 |
16451062 |
46 |
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. |
Astrazeneca |
15857136 |
4 |
Conformation mining: an algorithm for finding biologically relevant conformations. |
Rational Discovery |
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 |
15267232 |
65 |
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. |
Eli Lilly |
15214773 |
76 |
Fragment-based drug discovery. |
Sunesis Pharmaceuticals |
15115396 |
112 |
General model for estimation of the inhibition of protein kinases using Monte Carlo simulations. |
Yale University |
12672248 |
50 |
Kinase inhibitors: not just for kinases anymore. |
Northwestern University |
12954055 |
47 |
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors. |
Johnson and Johnson Pharmaceutical Research and Development |
12852764 |
20 |
Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors. |
Novo Nordisk |
15013000 |
31 |
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. |
Glaxosmithkline |
10743948 |
22 |
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. |
Ewha Womans University |
| 76 |
Synthesis and activity of 2,6,9-trisubstituted purines |
TBA |
22377675 |
44 |
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors. |
Westf£Lische Wilhelms-Universit£T M£Nster |
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 |
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 |
22004849 |
9 |
Selection of cyclic-peptide inhibitors targeting Aurora kinase A: problems and solutions. |
University of Arizona |
22148278 |
132 |
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase |
S Bio |
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 |
22119465 |
18 |
Structure-based design of PDK1 inhibitors. |
S Bio |
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 |
22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
22000924 |
25 |
Design, synthesis and biological study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors. |
National Organization For Drug Control & Research |
21986585 |
2 |
A modular approach to trim cellular targets in anticancer drug discovery. |
Instituto Universitario De Bio-Org£Nica Antonio Gonz£Lez (Iubo-Ag) |
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 |
21907583 |
48 |
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. |
University of South Florida |
21824779 |
67 |
Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2. |
Amgen |
21699136 |
16 |
Selectivity of kinase inhibitor fragments. |
Glaxosmithkline |
21775140 |
69 |
Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase. |
Astrazeneca |
21723120 |
100 |
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
Nerviano Medical Sciences |
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 |
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 |
21620699 |
51 |
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors. |
Pfizer |
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 |
21561767 |
48 |
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
Ariad Pharmaceuticals |
21493067 |
22 |
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. |
Astrazeneca R&D Boston |
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 |
21417417 |
8 |
Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity. |
Palacky£? University and Institute of Experimental Botany Ascr |
21353545 |
39 |
Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors. |
Harvard Medical School |
21414779 |
64 |
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors. |
Amgen |
24900229 |
41 |
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery. |
TBA |
24900250 |
81 |
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277 |
TBA |
21094608 |
74 |
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1. |
Merck Research Laboratories |
21094607 |
66 |
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2. |
Merck Research Laboratories |
21144757 |
15 |
Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25. |
Duquesne University |
21080629 |
153 |
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity. |
University of Regensburg |
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 |
20855207 |
26 |
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
20832307 |
43 |
Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors. |
Hoffmann-La Roche |
20817473 |
57 |
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. |
Nerviano Medical Sciences Oncology |
20684549 |
76 |
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor. |
Amgen |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
18559524 |
21 |
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
Boehringer Ingelheim Austria |
16408016 |
6 |
Assignment of protein function in the postgenomic era. |
The Scripps Research Institute |
15958589 |
2 |
Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1. |
Cyclacel |
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 |
20472447 |
45 |
Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK). |
Nycomed Pharma |
20483608 |
139 |
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck. |
Novartis Institute of Biomedical Research |
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 |
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 |
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 |
20137943 |
60 |
Azole-based inhibitors of AKT/PKB for the treatment of cancer. |
Amgen |
20137932 |
47 |
2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics. |
Amgen |
20045222 |
40 |
Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors. |
National Organization For Drug Control & 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 |
19854645 |
87 |
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles. |
Wyeth Research |
20060294 |
21 |
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy. |
Novartis Institutes For Biomedical 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 |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19857966 |
62 |
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors. |
Astrazeneca R&D Boston |
19954867 |
2 |
Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors. |
Institute of Radiopharmacy |
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 |
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 |
19361991 |
80 |
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors. |
Vertex Pharmaceuticals |
19632122 |
54 |
Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1. |
University of Leicester |
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 |
18835709 |
91 |
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors. |
Glaxosmithkline |
19414255 |
58 |
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase. |
Vertex Pharmaceuticals |
19358610 |
2 |
Halogen bonding--a novel interaction for rational drug design? |
Chinese Academy of Sciences |
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 |
19211246 |
320 |
N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping. |
4Sc |
19097792 |
24 |
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity. |
Astrazeneca R&D Boston |
19053831 |
39 |
Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles. |
Institute of General Genetics |
18996007 |
30 |
The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing. |
Astrazeneca Pharmaceuticals |
18986805 |
39 |
Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. |
Astrazeneca Pharmaceuticals |
18938080 |
102 |
Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK). |
Vertex Pharmaceuticals |
18929484 |
26 |
Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1. |
Glaxosmithkline |
18926699 |
30 |
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio. |
Sunesis Pharmaceuticals |
18818075 |
25 |
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors. |
Glaxosmithkline |
18815031 |
41 |
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors. |
Astrazeneca |
18691885 |
60 |
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors. |
Ariad Pharmaceuticals |
18650093 |
88 |
Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4. |
University of Leicester |
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 |
18617397 |
21 |
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode. |
Astrazeneca Pharmaceuticals |
18529047 |
156 |
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. |
Eberhard-Karls University |
18494457 |
160 |
4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4). |
Wyeth Research |
18457385 |
41 |
Recent developments in fragment-based drug discovery. |
Astex Therapeutics |
18393402 |
2 |
Natural products as leads to potential drugs: an old process or the new hope for drug discovery? |
National Cancer Institute-Frederick |
18313174 |
26 |
Synthesis and biological evaluation of diversely substituted indolin-2-ones. |
Université |
18037537 |
53 |
An efficient tool for identifying inhibitors based on 3D-QSAR and docking using feature-shape pharmacophore of biologically active conformation--a case study with CDK2/cyclinA. |
Institute of Chemical Biology (Csir) |
17707953 |
23 |
Selectivity criterion for pyrazolo[3,4-b]pyrid[az]ine derivatives as GSK-3 inhibitors: CoMFA and molecular docking studies. |
National Institute of Pharmaceutical Education and Research |
18353638 |
71 |
Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors. |
Keimyung University |
18289854 |
44 |
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase. |
Bristol-Myers Squibb Research and Development |
18248988 |
16 |
Entry into a new class of protein kinase inhibitors by pseudo ring design. |
Novartis Institutes For Biomedical Research |
18055203 |
51 |
Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA. |
Bristol-Myers Squibb Research and Development |
17826092 |
37 |
Optimization of triarylimidazoles for Tie2: influence of conformation on potency. |
Glaxosmithkline |
17459703 |
111 |
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. |
Ucb Pharma |
17303421 |
56 |
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
Roche Research Center |
17291769 |
133 |
Clubbed thiazoles by MAOS: a novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer's disease. |
Dr. Reddys Laboratories |
17178224 |
28 |
3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation. |
Keimyung University |
17149885 |
20 |
Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor. |
Eberhard-Karls University |
17123821 |
21 |
Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues. |
University of Kansas |
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 |
16913703 |
2 |
Novel structural features of CDK inhibition revealed by an ab initio computational method combined with dynamic simulations. |
University of Cambridge |
16789733 |
41 |
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16750360 |
36 |
CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation. |
De Montfort University |
16682193 |
62 |
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
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 |
16384702 |
35 |
CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads. |
Genentech |
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 |
16216502 |
119 |
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors. |
Abbott Laboratories |
16213715 |
4 |
Structural basis for the GSK-3beta binding affinity and selectivity against CDK-2 of 1-(4-aminofurazan-3yl)-5-dialkylaminomethyl-1H-[1,2,3] triazole-4-carboxylic acid derivatives. |
Universidade Do Porto |
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 |
15955699 |
33 |
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors. |
Glaxosmithkline |
15943473 |
136 |
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
15615512 |
21 |
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15566294 |
5 |
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. |
Università |
15546730 |
9 |
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15482916 |
64 |
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease. |
Pfizer |
15149684 |
59 |
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
14592495 |
60 |
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
14552791 |
35 |
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
Eli Lilly |
14505655 |
61 |
A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors. |
Pharmacia |
12941335 |
8 |
Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases. |
Ariad Pharmaceuticals |
12852762 |
10 |
A computational model of binding thermodynamics: the design of cyclin-dependent kinase 2 inhibitors. |
University of California |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
12182847 |
12 |
Peptide inhibitors of CDK2-cyclin A that target the cyclin recruitment-site: structural variants of the C-terminal Phe. |
University of Nottingham |
12036347 |
116 |
Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes. |
Aventis Pharma Deutschland |
11934592 |
24 |
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. |
Merck Research Laboratories |
11909733 |
30 |
Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
Institute of Molecular and Cell Biology |
11378364 |
34 |
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. |
Research Biomet. Glaxo Wellcome Medicines Research Centre |
10633045 |
1 |
Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase. |
Glaxo Wellcome |
28487075 |
36 |
N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1?/? inhibitors: Synthesis, biological evaluation and molecular modeling studies. |
Rajiv Gandhi Proudyogiki Vishwavidyalaya |
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 |
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 |
21985426 |
27 |
Chromone containing sulfonamides as potent carbonic anhydrase inhibitors. |
Ondokuz Mayis University |
28262558 |
62 |
Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. |
University of Oxford |
24327656 |
9 |
The molecular chaperone Hsp70 activates protein phosphatase 5 (PP5) by binding the tetratricopeptide repeat (TPR) domain. |
University of Michigan |
27359042 |
29 |
IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 Inhibitors |
Institut De Ge??Ne??Tique Et De Biologie Mole??Culaire Et Cellulaire |
22366955 |
11 |
Blind prediction of host-guest binding affinities: a new SAMPL3 challenge. |
University of California San Diego |
25346162 |
16 |
Synthesis, Biological Evaluation, and Molecular Simulation of Chalcones and Aurones as Selective MAO-B Inhibitors. |
Pontificia Universidad Catolica De Chile |
24403173 |
12 |
Long residence times revealed by Aurora A kinase-targeting fluorescent probes derived from inhibitors MLN8237 and VX-689. |
University of Tartu |
| 113 |
CDK2-CyclinA in CSAR_FULL_RELEASE_3JULY2012 |
Csar |
17616524 |
6 |
Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors. |
University of WÜRzburg |
16492568 |
12 |
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design. |
Cyclacel |
16242653 |
33 |
A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. |
Gpc Biotech |
19827834 |
93 |
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control. |
Vertex Pharmaceuticals |
19097791 |
44 |
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor. |
Pfizer |
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 |
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 |
17697781 |
29 |
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. |
Amgen |
17570665 |
19 |
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping. |
Vernalis (R&D) |
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) |
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 |
16616492 |
3 |
A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor. |
Nerviano Medical Sciences |
16290148 |
44 |
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors. |
Nerviano Medical Sciences |
16942020 |
12 |
Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. |
University of Oxford |
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) |
15686876 |
17 |
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2. |
Vernalis (R&D) |
15985434 |
18 |
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. |
Chinese Academy of Sciences |
10891109 |
19 |
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2. |
Palacky University |
12852944 |
26 |
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors. |
Hoffmann-La Roche |
15012993 |
22 |
A new series of potent oxindole inhibitors of CDK2. |
Hoffmann-La Roche |
12659774 |
20 |
Synthesis of potent oxindole CDK2 inhibitors. |
Hoffmann-La Roche |
15225695 |
64 |
4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors. |
Tsukuba Research Laboratories |
12941317 |
25 |
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis. |
Glaxosmithkline |
12941333 |
61 |
6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). |
Glaxosmithkline |
12699760 |
19 |
5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3). |
Glaxosmithkline |
15341487 |
213 |
N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. |
Glaxosmithkline |
15261277 |
30 |
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors. |
Cyclacel |
15027857 |
66 |
2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity. |
Cyclacel |
11728181 |
188 |
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis. |
Glaxosmithkline |
15081018 |
14 |
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors. |
Astrazeneca |
15081017 |
17 |
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors. |
Astrazeneca |
12941325 |
18 |
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation. |
Astrazeneca |
12941312 |
58 |
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines. |
Astrazeneca |
12941311 |
34 |
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines. |
Astrazeneca |
11960485 |
18 |
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics. |
Novartis Pharmaceuticals |
15664865 |
37 |
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes. |
Martin-Luther-University Halle-Wittenberg |
12749903 |
69 |
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors. |
Sugen |
15713378 |
72 |
Benzodipyrazoles: a new class of potent CDK2 inhibitors. |
Nerviano Medical Sciences |
15189033 |
48 |
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. |
Pharmacia Italia |
15828833 |
29 |
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization. |
Nerviano Medical Sciences |
11311054 |
14 |
Indenopyrazoles as novel cyclin dependent kinase (CDK) inhibitors. |
Dupont Pharmaceuticals |
11354366 |
81 |
Quinazolines as cyclin dependent kinase inhibitors. |
Dupont Pharmaceuticals |
15482910 |
53 |
Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors. |
Dupont Pharmaceuticals |
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 |
12824014 |
284 |
Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
Eli Lilly |
14552792 |
53 |
Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
Eli Lilly |
15149644 |
37 |
Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors. |
Eli Lilly |
15149678 |
32 |
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors. |
Eli Lilly |
15225699 |
27 |
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase 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 |
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 |
15801831 |
94 |
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
Pfizer |
11101352 |
88 |
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
Parke-Davis Pharmaceutical Research |
14698155 |
68 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3. |
Bristol-Myers Squibb |
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 |
15027863 |
17 |
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent. |
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 |
12431050 |
76 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern. |
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 |
12431051 |
114 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2). |
Bristol-Myers Squibb |
12941338 |
18 |
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. |
University of Newcastle |
10956187 |
18 |
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. |
University of Newcastle |
12482427 |
36 |
4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2. |
University of Newcastle |
15239650 |
90 |
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. |
University of Newcastle |
12139449 |
114 |
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. |
University of Newcastle |