The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28712298 |
2 |
The Fragment Network: A Chemistry Recommendation Engine Built Using a Graph Database. |
Astex Pharmaceuticals |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang University |
26945110 |
3 |
Synthesis and evaluation of the cytotoxic activity of novel ethyl 4-[4-(4-substitutedpiperidin-1-yl)]benzyl-phenylpyrrolo[1,2-a]quinoxaline-carboxylate derivatives in myeloid and lymphoid leukemia cell lines. |
University Of Bordeaux |
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 |
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 |
25409491 |
83 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
Zhejiang University |
25180768 |
11 |
2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites. |
Vanderbilt University Medical Center |
24650640 |
43 |
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors. |
Martin-Luther-University Halle-Wittenberg |
23550937 |
72 |
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties. |
Emory University |
23394126 |
170 |
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). |
Exelixis |
23394218 |
159 |
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases. |
Astrazeneca |
23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
22934575 |
124 |
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. |
Array Biopharma |
22533986 |
181 |
Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors. |
Arqule |
22320327 |
250 |
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series. |
Amgen |
22342124 |
9 |
Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors. |
Exelixis |
15975507 |
13 |
Features of selective kinase inhibitors. |
University Of California San Francisco |
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 |
18345609 |
57 |
Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration. |
The Institute Of Cancer Research |
18054229 |
35 |
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity. |
Merck |
18479914 |
52 |
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. |
Merck Research Laboratories |
18296048 |
50 |
Rapid assembly of diverse and potent allosteric Akt inhibitors. |
Merck Research Laboratories |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
16876403 |
85 |
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
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 |
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 |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
20630752 |
40 |
Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors. |
Millennium Pharmaceuticals |
20810279 |
86 |
Discovery of pyrrolopyrimidine inhibitors of Akt. |
Array Biopharma |
19465931 |
12 |
Inhibitor hijacking of Akt activation. |
University Of California |
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 |
20481595 |
48 |
Design of selective, ATP-competitive inhibitors of Akt. |
Pfizer |
19179070 |
89 |
Aminofurazans as potent inhibitors of AKT kinase. |
Glaxosmithkline |
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 |
20166671 |
85 |
Selectively nonselective kinase inhibition: striking the right balance. |
Schering-Plough |
20151677 |
67 |
Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt). |
The Institute Of Cancer Research |
20006500 |
60 |
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines. |
Glaxosmithkline |
20005102 |
34 |
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. |
Glaxosmithkline |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19604696 |
6 |
Discovery of a novel protein kinase B inhibitor by structure-based virtual screening. |
Torrey Pines Institute For Molecular Studies |
19285393 |
90 |
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors. |
Glaxosmithkline |
19097777 |
55 |
Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity. |
Merck Research Laboratories |
18550373 |
97 |
The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity. |
Merck Research Laboratories |
18539456 |
106 |
Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors. |
Merck Research Laboratories |
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 |
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 |
16765046 |
63 |
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies. |
Chiron |
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 |
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 |
12941327 |
24 |
Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade. |
Wyeth Research |
11206452 |
14 |
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth. |
Georgetown University Medical Center |
28506751 |
4 |
Recent progress towards clinically relevant ATP-competitive Akt inhibitors. |
Merck |
28221775 |
5 |
Electrostatic Interactions as Mediators in the Allosteric Activation of Protein Kinase A RIa. |
University Of California San Diego |
20718440 |
7 |
Novel benzimidazole inhibitors bind to a unique site in the kinesin spindle protein motor domain. |
Merck Research Laboratories |
17581239 |
25 |
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors. |
Pfizer |
20444281 |
18 |
Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility. |
University Of Pittsburgh |
11701096 |
24 |
Di-, tri- and tetra-5'-O-phosphorothioadenosyl substituted polyols as inhibitors of Fhit: Importance of the alpha-beta bridging oxygen and beta phosphorus replacement. |
Kimmel Cancer Center |
11451670 |
11 |
Hexosaminidase inhibitors as new drug candidates for the therapy of osteoarthritis. |
The Scripps Research Institute |
18343106 |
12 |
Beta-lactam congeners of orlistat as inhibitors of fatty acid synthase. |
Texas A&M University |