The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.![EBI](/images/logo_chembl.png) |
Merck |
27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.![EBI](/images/logo_chembl.png) |
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.![EBI](/images/logo_chembl.png) |
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).![EBI](/images/logo_chembl.png) |
Icahn School of Medicine At Mount Sinai |
25180768 |
11 |
2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.![EBI](/images/logo_chembl.png) |
Vanderbilt University Medical Center |
24650640 |
43 |
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.![EBI](/images/logo_chembl.png) |
Martin-Luther-University Halle-Wittenberg |
23394126 |
170 |
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).![EBI](/images/logo_chembl.png) |
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.![EBI](/images/logo_chembl.png) |
Astrazeneca |
23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.![EBI](/images/logo_chembl.png) |
Abbott Laboratories |
22934575 |
124 |
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.![EBI](/images/logo_chembl.png) |
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.![EBI](/images/logo_chembl.png) |
Arqule |
24900264 |
106 |
The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.![EBI](/images/logo_chembl.png) |
TBA |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity.![EBI](/images/logo_chembl.png) |
Ambit Biosciences |
18054229 |
35 |
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.![EBI](/images/logo_chembl.png) |
Merck |
18479914 |
52 |
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
18296048 |
50 |
Rapid assembly of diverse and potent allosteric Akt inhibitors.![EBI](/images/logo_chembl.png) |
Merck Research Laboratories |
17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.![EBI](/images/logo_chembl.png) |
Abbott Laboratories |
16876403 |
85 |
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.![EBI](/images/logo_chembl.png) |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
17018693 |
30 |
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.![EBI](/images/logo_chembl.png) |
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).![EBI](/images/logo_chembl.png) |
Ansaris |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity.![EBI](/images/logo_chembl.png) |
Ambit Biosciences |
20810279 |
86 |
Discovery of pyrrolopyrimidine inhibitors of Akt.![EBI](/images/logo_chembl.png) |
Array Biopharma |
19465931 |
12 |
Inhibitor hijacking of Akt activation.![EBI](/images/logo_chembl.png) |
University of California |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).![EBI](/images/logo_chembl.png) |
Ambit Biosciences |
20481595 |
48 |
Design of selective, ATP-competitive inhibitors of Akt.![EBI](/images/logo_chembl.png) |
Pfizer |
19179070 |
89 |
Aminofurazans as potent inhibitors of AKT kinase.![EBI](/images/logo_chembl.png) |
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.![EBI](/images/logo_chembl.png) |
Abbott Laboratories |
20166671 |
85 |
Selectively nonselective kinase inhibition: striking the right balance.![EBI](/images/logo_chembl.png) |
Schering-Plough |
19800227 |
31 |
Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases.![EBI](/images/logo_chembl.png) |
University of Tartu |
20006500 |
60 |
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.![EBI](/images/logo_chembl.png) |
Glaxosmithkline |
20005102 |
34 |
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.![EBI](/images/logo_chembl.png) |
Glaxosmithkline |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.![EBI](/images/logo_chembl.png) |
Abbott Laboratories |
19361991 |
80 |
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.![EBI](/images/logo_chembl.png) |
Vertex Pharmaceuticals |
19604696 |
6 |
Discovery of a novel protein kinase B inhibitor by structure-based virtual screening.![EBI](/images/logo_chembl.png) |
Torrey Pines Institute For Molecular Studies |
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.![EBI](/images/logo_chembl.png) |
University of Illinois At Chicago |
19285393 |
90 |
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.![EBI](/images/logo_chembl.png) |
Glaxosmithkline |
19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.![EBI](/images/logo_chembl.png) |
Glaxosmithkline |
18818075 |
25 |
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.![EBI](/images/logo_chembl.png) |
Glaxosmithkline |
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.![EBI](/images/logo_chembl.png) |
Glaxosmithkline |
16765046 |
63 |
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.![EBI](/images/logo_chembl.png) |
Chiron |
30660827 |
70 |
Quinolone hybrids and their anti-cancer activities: An overview.![EBI](/images/logo_chembl.png) |
Qilu University of Technology (Shandong Academy of Sciences) |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png) |
Merck |
27491711 |
422 |
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.![EBI](/images/logo_chembl.png) |
Merck And |
27305487 |
105 |
Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.![EBI](/images/logo_chembl.png) |
Arqule |
31298542 |
108 |
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.![EBI](/images/logo_chembl.png) |
Chinese Academy of Sciences |
31693351 |
473 |
Discovery of 4![EBI](/images/logo_chembl.png) |
TBA |
30384048 |
365 |
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.![EBI](/images/logo_chembl.png) |
University of Florida |
31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.![EBI](/images/logo_chembl.png) |
Takeda Pharmaceutical |
26509640 |
234 |
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.![EBI](/images/logo_chembl.png) |
Abbvie Bioresearch Center |
30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png) |
Vertex Pharmaceuticals |
29945794 |
193 |
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.![EBI](/images/logo_chembl.png) |
Vertex Pharmaceuticals |
28506751 |
4 |
Recent progress towards clinically relevant ATP-competitive Akt inhibitors.![EBI](/images/logo_chembl.png) |
Merck |
22938723 |
4 |
Oxygenation of monoenoic fatty acids by CYP175A1, an orphan cytochrome P450 from Thermus thermophilus HB27.![BDB](/images/logo_bindingdb.png) |
Tata Institute of Fundamental Research |
7965746 |
33 |
[125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors.![BDB](/images/logo_bindingdb.png) |
U. 109 |
17581239 |
25 |
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.![BDB](/images/logo_bindingdb.png) |
Pfizer |
20444281 |
18 |
Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility.![BDB](/images/logo_bindingdb.png) |
University of Pittsburgh |
11451670 |
11 |
Hexosaminidase inhibitors as new drug candidates for the therapy of osteoarthritis.![BDB](/images/logo_bindingdb.png) |
The Scripps Research Institute |