The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28279846 |
36 |
Design, synthesis, and biological evaluation of novel 4-anilinoquinazoline derivatives bearing amino acid moiety as potential EGFR kinase inhibitors. |
Xuzhou Medical University |
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 |
27884697 |
65 |
3-Cyano-6-(5-methyl-3-pyrazoloamino) pyridines (Part 2): A dual inhibitor of Aurora kinase and tubulin polymerization. |
Cxs |
27573544 |
43 |
Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design. |
Taiwan National Health Research Institutes |
27391133 |
76 |
Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening. |
University Of Berne |
27774127 |
75 |
Discovery of a Series of 5,11-Dihydro-6 |
Dana-Farber Cancer Institute |
27335255 |
33 |
Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK. |
Entremed |
27209235 |
8 |
Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors. |
Sookmyung Women'S 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 |
27041399 |
32 |
Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors. |
Ewha Womans University |
26890118 |
8 |
Discovery of antitumor anthra[2,3-b]furan-3-carboxamides: Optimization of synthesis and evaluation of antitumor properties. |
Mendeleyev University Of Chemical Technology |
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 |
26384287 |
65 |
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors. |
Kangwon National University |
26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
26320624 |
45 |
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model. |
Novartis Institutes For Biomedical Research |
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 |
26048792 |
4 |
Identification of 3,5,6-substituted indolin-2-one's inhibitors of Aurora B by development of a luminescent kinase assay. |
Chinese Academy Of Medical Sciences And Peking Union Medical College |
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 |
26101564 |
20 |
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors. |
Takeda Pharmaceutical |
25812967 |
6 |
Synthesis and biological evaluation of 2,4-diaminopyrimidines as selective Aurora A kinase inhibitors. |
Lanzhou University |
25791677 |
15 |
Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges. |
Zhengzhou University |
25766633 |
9 |
Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor. |
The University Of Michigan Medical School |
25369539 |
116 |
SAR156497, an exquisitely selective inhibitor of aurora kinases. |
Sanofi |
25089810 |
79 |
Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia. |
National Taiwan University |
25043312 |
104 |
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides. |
University Health Network |
25042560 |
18 |
Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors. |
Ewha Womans University |
25036791 |
56 |
Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor. |
National Taiwan University |
25022204 |
78 |
Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells. |
Universit£ |
24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
24867403 |
156 |
The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. |
Entremed |
25462247 |
20 |
In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor. |
Fudan University |
25456085 |
4 |
Synthesis and biological evaluation of novel oxindole-based RTK inhibitors as anti-cancer agents. |
Wenzhou Medical University |
25383627 |
85 |
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation. |
Genentech |
25270403 |
44 |
Discovery of 4-aminoquinazoline--urea derivatives as Aurora kinase inhibitors with antiproliferative activity. |
Southeast University |
24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
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 |
24681066 |
35 |
Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors. |
Sun Yat-Sen University |
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 |
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 |
24195668 |
57 |
Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells. |
The Institute Of Cancer Research |
24100158 |
148 |
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). |
Nerviano Medical Sciences |
24900590 |
55 |
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy. |
Glaxosmithkline |
24044867 |
86 |
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
Califia Bio |
23856049 |
50 |
Discovery of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1: optimization of kinase selectivity and pharmacokinetics. |
Osi Pharmaceuticals |
23829549 |
145 |
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
Entremed |
23773865 |
49 |
Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. |
Osi Pharmaceuticals |
23707920 |
3 |
A thienopyrimidine derivative induces growth inhibition and apoptosis in human cancer cell lines via inhibiting Aurora B kinase activity. |
Fudan University |
23808327 |
29 |
Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine Aurora kinase inhibitor. |
National Health Research Institutes |
23664099 |
32 |
Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors. |
Xuzhou Medical College |
23570792 |
61 |
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors. |
Emd-Serono Research Institute |
23490150 |
48 |
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. |
Takeda Pharmaceutical |
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 |
23414845 |
44 |
Structure-based discovery of cellular-active allosteric inhibitors of FAK. |
Takeda Pharmaceutical |
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 |
21903390 |
79 |
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
Glaxosmithkline |
19349179 |
47 |
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors. |
Glaxosmithkline |
23099093 |
84 |
Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases. |
Mrc Technology |
23043539 |
60 |
Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. |
The Institute Of Cancer Research |
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 |
22920039 |
9 |
Crystal structure of human aurora B in complex with INCENP and VX-680. |
University Of Oxford |
22827572 |
67 |
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). |
Glaxosmithkline |
22380736 |
90 |
Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index. |
Ambit Biosciences |
22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
22980219 |
55 |
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy. |
Takeda Pharmaceutical |
22695126 |
98 |
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. |
Abbott Laboratories |
22727637 |
85 |
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors. |
Abbott Laboratories |
22632936 |
42 |
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors. |
Myrexis |
22439974 |
79 |
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders. |
Takeda Pharmaceutical |
22560627 |
70 |
2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
Technische Universit£T Braunschweig |
22607669 |
45 |
Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors. |
Biogen Idec |
22320327 |
250 |
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series. |
Amgen |
22168626 |
32 |
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. |
Ambit Biosciences |
22247788 |
40 |
Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. |
TBA |
22503250 |
128 |
Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity. |
Amri |
22465635 |
95 |
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. |
Abbott Laboratories |
22326168 |
67 |
Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1. |
Biogen Idec |
22305584 |
145 |
Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKe kinases. |
Astrazeneca R&D Boston |
21128645 |
60 |
Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase. |
Evotec (Uk) |
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 |
18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
20570526 |
84 |
Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
National Taiwan University |
20565112 |
55 |
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. |
The Institute Of Cancer Research |
20420387 |
118 |
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. |
Glaxosmithkline |
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 |
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 |
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 |
19320489 |
125 |
Discovery and development of aurora kinase inhibitors as anticancer agents. |
Vertex Pharmaceuticals |
18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
17360485 |
10 |
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. |
Millennium Pharmaceuticals |
18324761 |
65 |
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation. |
Amgen |
18324759 |
133 |
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors. |
Amgen |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University Of Oxford |
18243698 |
11 |
Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold. |
National Health Research Institutes |
16451062 |
46 |
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. |
Astrazeneca |
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 |
22153662 |
137 |
Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. |
Astrazeneca |
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 |
22003817 |
71 |
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. |
Takeda Pharmaceutical |
21982797 |
128 |
9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp. |
Peking University |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
21855335 |
185 |
Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. |
Merck Research Laboratories |
21802948 |
125 |
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors. |
Ambit Biosciences |
21741249 |
32 |
Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp. |
Heinrich Heine Universit£T |
20674350 |
63 |
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
20573509 |
23 |
3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. |
Mitsubishi Tanabe Pharma |
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 |
21341675 |
266 |
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors. |
Glaxosmithkline |
24900229 |
41 |
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery. |
TBA |
21288717 |
131 |
Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions. |
Abbott Laboratories |
21282054 |
178 |
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions. |
Abbott Laboratories |
20965724 |
57 |
Identification of potent ITK inhibitors through focused compound library design including structural information. |
Nycomed |
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 |
20833547 |
19 |
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells. |
The Institute Of Cancer Research |
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 |
16783341 |
34 |
Rational design of inhibitors that bind to inactive kinase conformations. |
Novartis Research Foundation |
20681538 |
61 |
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile. |
Development Center For Biotechnology |
20462263 |
127 |
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. |
Cyclacel |
20459125 |
60 |
Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index. |
Amgen |
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 |
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 |
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 |
20338758 |
39 |
Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors. |
S*Bio |
20335034 |
7 |
Discovery of a new series of Aurora inhibitors through truncation of GSK1070916. |
Glaxosmithkline |
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 |
20167481 |
66 |
Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2. |
Sanofi-Aventis |
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 |
19646866 |
35 |
2-Aminobenzimidazoles as potent Aurora kinase inhibitors. |
Sunesis Pharmaceuticals |
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 |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19692247 |
295 |
Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization. |
4Sc |
19857966 |
62 |
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors. |
Astrazeneca R&D Boston |
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 |
19447622 |
128 |
The discovery of the potent aurora inhibitor MK-0457 (VX-680). |
Vertex Pharmaceuticals |
19364658 |
113 |
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). |
Wyeth Research |
19211246 |
320 |
N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping. |
4Sc |
19101143 |
70 |
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). |
Glaxosmithkline |
19062275 |
39 |
Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase. |
Amgen |
19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
18682324 |
33 |
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors. |
Amgen |
18606543 |
68 |
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta. |
Wyeth Research |
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 |
18524423 |
16 |
Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors. |
Eberhard-Karls University |
17933533 |
36 |
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases. |
The Institute Of Cancer Research |
17665890 |
60 |
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins. |
University Of Athens |
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 |
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 |
16970394 |
147 |
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. |
Amgen |
29518312 |
78 |
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer. |
Nankai University |
27450574 |
3 |
Structure-based virtual screening toward the discovery of novel inhibitors of the DNA repair activity of the human apurinic/apyrimidinic endonuclease 1. |
Universidade De Lisboa |
10353842 |
147 |
Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R). |
National Institute Of Diabetes And Digestive And Kidney Diseases |
9650799 |
159 |
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
Novartis Pharma |
7890738 |
3 |
Expression of recombinant homo-oligomeric 5-hydroxytryptamine3 receptors provides new insights into their maturation and structure. |
Medical Research Council Centre |
19807733 |
6 |
Active site ring-opening of a thiirane moiety and picomolar inhibition of gelatinases. |
University Of Notre Dame |
19703036 |
15 |
Antiproliferative activity against MCF-7 breast cancer cells by diamino-triazaspirodiene antifolates. |
National University Of Singapore |
6266565 |
14 |
The binding of [3H]-prostacyclin to membranes of a neuronal somatic hybrid. |
Royal Postgraduate Medical School |
17630989 |
9 |
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies. |
Abbott Laboratories |
21513882 |
3 |
Sequential mechanism of assembly of multidrug efflux pump AcrAB-TolC. |
University Of Oklahoma |
18849972 |
45 |
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase. |
The Scripps Research Institute |
19877603 |
51 |
Identification and Biological Evaluation of a Series of 1H-Benzo[de]isoquinoline-1,3(2H)-diones as Hepatitis C Virus NS5B Polymerase Inhibitors. |
Irbm, Mrl Rome |
15974572 |
14 |
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. |
Vernalis (R&D) |
15723556 |
4 |
Use of binding enthalpy to drive an allosteric transition. |
University Of Maryland |