The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
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 |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
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 |
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 |
24517277 |
4 |
Therapeutic melting pot of never in mitosis gene a related kinase 2 (Nek2): a perspective on Nek2 as an oncology target and recent advancements in Nek2 small molecule inhibition. |
The University of Arizona |
25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
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 |
24650640 |
43 |
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors. |
Martin-Luther-University Halle-Wittenberg |
24479418 |
39 |
Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia. |
Heinrich Heine Universit£T |
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 |
24328302 |
94 |
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
Heinrich-Heine-Universit£T D£Sseldorf |
24007918 |
6 |
A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway. |
University of Edinburgh Cancer Research Centre In The Institute of Genetics and Molecular Medicine |
23602398 |
43 |
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors. |
Merck Research Laboratories |
23535330 |
83 |
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors. |
Merck Research Laboratories |
23394126 |
170 |
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). |
Exelixis |
23312943 |
166 |
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
22726925 |
216 |
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease. |
Cellzome |
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 |
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 |
24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
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 |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
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 |
21982797 |
128 |
9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp. |
Peking University |
21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
21741249 |
32 |
Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp. |
Heinrich Heine Universit£T |
21627121 |
22 |
Irreversible Nek2 kinase inhibitors with cellular activity. |
University of California |
21366329 |
29 |
Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship. |
The Institute of Cancer Research |
20965724 |
57 |
Identification of potent ITK inhibitors through focused compound library design including structural information. |
Nycomed |
20936789 |
56 |
Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization. |
The Institute of Cancer Research |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
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 |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
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 |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
22645149 |
12 |
Novel Anti-inflammatory Activity of Epoxyazadiradione against Macrophage Migration Inhibitory Factor: INHIBITION OF TAUTOMERASE AND PROINFLAMMATORY ACTIVITIES OF MACROPHAGE MIGRATION INHIBITORY FACTOR. |
Council of Scientific and Industrial Research (Csir) Indian Institute of Chemical Biology |