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 |
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 |
26270416 |
70 |
Discovery of Potent and Selective RSK Inhibitors as Biological Probes. |
Novartis Institutes For Biomedical Research |
25147152 |
1 |
Kaempferol, a potential cytostatic and cure for inflammatory disorders. |
Npo-International Laboratory of Biochemistry |
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 |
25589938 |
5 |
Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101. |
Northeastern University |
25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
24534486 |
56 |
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors. |
Novartis Institutes For Biomedical Research |
23535330 |
83 |
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors. |
Merck Research Laboratories |
23434140 |
35 |
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis. |
East China University of Science and Technology |
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 |
23519677 |
8 |
Improving the affinity of SL0101 for RSK using structure-based design. |
Vanderbilt University |
22765894 |
223 |
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. |
Exelixis |
22621397 |
39 |
Irreversible protein kinase inhibitors: balancing the benefits and risks. |
Covalution Pharma |
23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
22726925 |
216 |
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease. |
Cellzome |
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 |
22564207 |
44 |
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. |
Cephalon |
22503250 |
128 |
Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity. |
Amri |
22464132 |
8 |
Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability. |
University of Virginia |
24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
22342124 |
9 |
Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors. |
Exelixis |
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 |
14593182 |
34 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
Pfizer |
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 |
17350261 |
16 |
Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
16876403 |
85 |
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
15999997 |
85 |
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase. |
Serono Pharmaceutical Research Institute |
22100312 |
70 |
Indole RSK inhibitors. Part 1: discovery and initial SAR. |
Boehringer Ingelheim Pharmaceuticals |
22056746 |
53 |
Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. |
Boehringer Ingelheim Pharmaceuticals |
21794960 |
194 |
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
Universit£ |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
20674350 |
63 |
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
21488662 |
18 |
SHAFTS: a hybrid approach for 3D molecular similarity calculation. 2. Prospective case study in the discovery of diverse p90 ribosomal S6 protein kinase 2 inhibitors to suppress cell migration. |
East China University of Science and Technology |
21375264 |
77 |
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors |
Roche Palo Alto |
20855207 |
26 |
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
17259979 |
5 |
A clickable inhibitor reveals context-dependent autoactivation of p90 RSK. |
University of California |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
17166835 |
12 |
Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors. |
Istituto Di Ricerche Di Biologia Molecolare &Quot;P. Angeletti |
15919995 |
4 |
Structural bioinformatics-based design of selective, irreversible kinase inhibitors. |
University of California |
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 |
17303421 |
56 |
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
Roche Research Center |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
15149684 |
59 |
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3. |
Johnson & Johnson Pharmaceutical Research & Development |
27996267 |
22 |
Covalent Modifiers: A Chemical Perspective on the Reactivity of?,?-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions. |
University of Pittsburgh |
20028980 |
8 |
Inhibition of AcpA phosphatase activity with ascorbate attenuates Francisella tularensis intramacrophage survival. |
University of Florida |
17630989 |
9 |
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies. |
Abbott Laboratories |
16249185 |
8 |
The structure of dimeric ROCK I reveals the mechanism for ligand selectivity. |
Vertex Pharmaceuticals |
15755666 |
18 |
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase. |
Biocryst Pharmaceuticals |