The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28249207 |
78 |
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis. |
East China Normal University |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
28109791 |
44 |
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. |
Chugai Pharmaceutical |
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 |
27668758 |
17 |
Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors. |
Kasetsart University |
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 |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
27209235 |
8 |
Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors. |
Sookmyung Women'S University |
27089211 |
38 |
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
Zhejiang 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 |
27041399 |
32 |
Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors. |
Ewha Womans University |
26951753 |
336 |
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
26348881 |
54 |
Identification of Substituted Naphthotriazolediones as Novel Tryptophan 2,3-Dioxygenase (TDO) Inhibitors through Structure-Based Virtual Screening. |
National Health Research Institutes |
26318056 |
25 |
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2. |
Universit£ |
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 |
26320619 |
88 |
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
26318067 |
34 |
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
Hanyang University |
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 |
26258521 |
104 |
Development of Selective Covalent Janus Kinase 3 Inhibitors. |
Harvard Medical School |
26077498 |
9 |
Fluorescent photoaffinity probes for mitotic protein kinase Aurora A. |
University of Tartu |
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 |
26030457 |
64 |
Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors. |
Shanghai Chempartner |
26101579 |
45 |
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series. |
Genentech |
26081023 |
55 |
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations. |
National Health Research Institutes |
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 |
25763473 |
108 |
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents. |
Entremed |
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 |
25723005 |
111 |
The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent. |
TBA |
25771484 |
5 |
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold. |
Zhejiang University |
25369539 |
116 |
SAR156497, an exquisitely selective inhibitor of aurora kinases. |
Sanofi |
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 |
25042558 |
38 |
Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors. |
Zhejiang 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 |
24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
24811300 |
20 |
Biased and unbiased strategies to identify biologically active small molecules. |
Institut De Chimie Des Substances Naturelles |
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 |
25270403 |
44 |
Discovery of 4-aminoquinazoline--urea derivatives as Aurora kinase inhibitors with antiproliferative activity. |
Southeast University |
24918870 |
74 |
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors. |
Genentech |
24534486 |
56 |
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
24565968 |
1 |
Polyphenols bearing cinnamaldehyde scaffold showing cell growth inhibitory effects on the cisplatin-resistant A2780/Cis ovarian cancer cells. |
Konkuk University |
24389511 |
25 |
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors. |
Zhejiang University |
24359159 |
60 |
Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. |
Astrazeneca |
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 |
23994329 |
12 |
Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3ß (GSK-3ß) inhibitors. |
Zhejiang University |
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 |
24044867 |
86 |
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
Califia Bio |
23937569 |
22 |
Selectivity data: assessment, predictions, concordance, and implications. |
Eli Lilly |
23920481 |
25 |
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases. |
The Institute of Cancer Research |
23829549 |
145 |
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. |
Entremed |
23755884 |
23 |
Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics. |
Takeda Pharmaceutical |
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 |
22749643 |
69 |
Structure-based optimization of oxadiazole-based GSK-3 inhibitors. |
Technische Universit£T Darmstadt |
23618709 |
70 |
Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
National Health Research Institutes |
23570792 |
61 |
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors. |
Emd-Serono Research Institute |
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 |
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 |
23265875 |
78 |
Design and synthesis of tricyclic cores for kinase inhibition. |
Abbott Bioresearch Center |
24900658 |
10 |
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors. |
Hoffmann-La Roche |
23312943 |
166 |
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
23312472 |
129 |
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
21429745 |
49 |
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-ß. |
Glaxosmithkline |
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 |
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 |
22380736 |
90 |
Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index. |
Ambit Biosciences |
23025996 |
4 |
Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents. |
Nanjing University |
22695126 |
98 |
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. |
Abbott Laboratories |
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 |
22727637 |
85 |
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors. |
Abbott Laboratories |
22726931 |
113 |
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
National Health Research Institutes |
22533818 |
84 |
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a. |
Technische Universit£T Darmstadt |
22632936 |
42 |
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors. |
Myrexis |
22452518 |
22 |
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. |
Sichuan University |
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 |
22372864 |
25 |
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases. |
Hanmi Research Center |
22607669 |
45 |
Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors. |
Biogen Idec |
22579487 |
53 |
Synthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors. |
Korea Research Institute of Chemical Technology |
22572580 |
26 |
Synthesis, biological evaluation, and molecular docking studies of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives as anticancer agents. |
Nanjing University |
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 |
24900346 |
90 |
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. |
TBA |
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 |
22230199 |
12 |
Unbiased binding assays for discovering small-molecule probes and drugs. |
Broad Institute of Harvard and Mit |
22148921 |
48 |
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c |
Cephalon |
21664013 |
8 |
Single step synthesis of new fused pyrimidine derivatives and their evaluation as potent Aurora-A kinase inhibitors. |
Umm Al-Qura University |
21608528 |
166 |
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. |
Merck Research Laboratories |
21128645 |
60 |
Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase. |
Evotec (Uk) |
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 |
20000735 |
12 |
Through the"gatekeeper door": exploiting the active kinase conformation. |
Nerviano Medical Sciences |
20153646 |
28 |
Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells. |
Institute of Science and Technology |
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 |
20097066 |
53 |
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme. |
Schering-Plough Research Institute |
18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
19320489 |
125 |
Discovery and development of aurora kinase inhibitors as anticancer agents. |
Vertex Pharmaceuticals |
18502127 |
77 |
2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3). |
Kemia |
17360485 |
10 |
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. |
Millennium Pharmaceuticals |
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 |
17983756 |
55 |
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors. |
Osi Pharmaceuticals |
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 |
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 |
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 |
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 |
22310227 |
89 |
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors. |
Glaxosmithkline |
22004849 |
9 |
Selection of cyclic-peptide inhibitors targeting Aurora kinase A: problems and solutions. |
University of Arizona |
22136433 |
67 |
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. |
Ludwig-Maximilians University of Munich |
22040023 |
63 |
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1). |
Pfizer |
22169262 |
26 |
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase. |
Shenyang Pharmaceutical University |
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 |
22119469 |
107 |
Novel and selective spiroindoline-based inhibitors of Sky kinase. |
Pfizer |
22101132 |
41 |
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases. |
Shionogi |
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 |
22001029 |
28 |
Design and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors. |
Korea Research Institute of Chemical Technology |
22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
21794960 |
194 |
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
Universit£ |
22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
21970471 |
66 |
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia. |
Vertex Pharmaceuticals |
21936542 |
143 |
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. |
Novartis Institute For Biomedical Research |
21823617 |
58 |
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors. |
Chugai Pharmaceutical |
21807510 |
31 |
Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas. |
Technische Universit£T Darmstadt |
21802948 |
125 |
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors. |
Ambit Biosciences |
21798738 |
44 |
Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I). |
Biogen Idec |
21699136 |
16 |
Selectivity of kinase inhibitor fragments. |
Glaxosmithkline |
21536449 |
16 |
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin. |
The Institute of Cancer Research |
21723120 |
100 |
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. |
Nerviano Medical Sciences |
21708468 |
101 |
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). |
National Health Research Institutes |
20674350 |
63 |
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
21620699 |
51 |
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors. |
Pfizer |
21561767 |
48 |
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
Ariad Pharmaceuticals |
21561771 |
39 |
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors. |
Chugai Pharmaceutical |
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 |
21391610 |
139 |
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors. |
Vertex Pharmaceuticals |
21341675 |
266 |
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors. |
Glaxosmithkline |
21353776 |
5 |
8-Hydroxynaphthalene-1,4-dione derivative as novel compound for glioma treatment. |
University of Padova |
21414779 |
64 |
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors. |
Amgen |
24900231 |
22 |
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. |
TBA |
24900229 |
41 |
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery. |
TBA |
21093113 |
58 |
Molecular modeling studies on imidazo[4,5-b]pyridine derivatives as Aurora A kinase inhibitors using 3D-QSAR and docking approaches. |
Jinan University |
24900250 |
81 |
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277 |
TBA |
21194953 |
15 |
Computational approach to the identification of novel Aurora-A inhibitors. |
Korea Institute of Science and Technology |
21035334 |
55 |
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors. |
Martin-Luther-University Halle-Wittenberg |
20965724 |
57 |
Identification of potent ITK inhibitors through focused compound library design including structural information. |
Nycomed |
20934346 |
46 |
Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine and benzo[4,5]imidazo[1,2-a]pyrimidine compounds as dual KSP and Aurora-A kinase inhibitors for anti-cancer agents. |
China Pharmaceutical University |
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 |
20833055 |
44 |
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation. |
Takeda Pharmaceutical |
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 |
20655209 |
18 |
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities. |
Université |
20681538 |
61 |
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile. |
Development Center For Biotechnology |
20550212 |
25 |
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification. |
National Health Research Institutes |
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 |
20361800 |
22 |
5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. |
Institute of Science and Technology |
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 |
20050669 |
61 |
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. |
Genentech |
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 |
20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
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 |
19481464 |
41 |
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors. |
Zhejiang University |
19447622 |
128 |
The discovery of the potent aurora inhibitor MK-0457 (VX-680). |
Vertex Pharmaceuticals |
19414255 |
58 |
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase. |
Vertex Pharmaceuticals |
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 |
19019675 |
52 |
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK? |
Pfizer |
18718756 |
44 |
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity. |
Johnson & Johnson Pharmaceutical Research and Development |
18682324 |
33 |
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors. |
Amgen |
18678484 |
57 |
A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity. |
Johnson & Johnson Pharmaceutical Research and Development |
18579375 |
3 |
Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. |
Sunesis Pharmaceuticals |
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 |
18457385 |
41 |
Recent developments in fragment-based drug discovery. |
Astex Therapeutics |
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 |
17574416 |
39 |
Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
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 |
17157005 |
6 |
Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors. |
Activesight |
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 |
16934458 |
124 |
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors. |
Valeant Pharmaceuticals Research & Development |
16884290 |
13 |
Accurate prediction of the relative potencies of members of a series of kinase inhibitors using molecular docking and MM-GBSA scoring. |
Astrazeneca R&D Boston |
16198560 |
19 |
Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases. |
Imclone Systems |
15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
32371117 |
20 |
Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights. |
Jouf University |
32035750 |
28 |
Synthesis, biological evaluation and molecular modeling study of 2-amino-3,5-disubstituted-pyrazines as Aurora kinases inhibitors. |
Lanzhou University |
31862411 |
12 |
Discovery of novel 2,4-disubstituted pyrimidines as Aurora kinase inhibitors. |
Lanzhou University |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
27515719 |
8 |
Discovery of N-(benzyloxy)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives as potential antiproliferative agents by inhibiting MEK. |
Anhui Agricultural University |
27429068 |
54 |
Evolution of a Novel, Orally Bioavailable Series of PI3K? Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease. |
Glaxosmithkline R&D |
27578246 |
158 |
Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors. |
Glaxosmithkline R&D |
27592744 |
64 |
Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3'-indolin]-2'-ones as potent PLK4 inhibitors with oral antitumor efficacy. |
Entremed |
27476140 |
4 |
Colorectal anticancer activities of polymethoxylated 3-naphthyl-5-phenylpyrazoline-carbothioamides. |
Konkuk University |
27379978 |
140 |
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors. |
Chinese Academy of Sciences |
26914744 |
24 |
Chemical Space of DNA-Encoded Libraries. |
University of Utah |
30755337 |
95 |
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952. |
Japan Tobacco |
31381325 |
46 |
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents. |
Chengdu University |
29400967 |
136 |
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. |
Bristol-Myers Squibb |
30728112 |
6 |
Synthesis and biological evaluation of nitroxide labeled pyrimidines as Aurora kinase inhibitors. |
Lanzhou University |
31200236 |
6 |
Tetrazole hybrids with potential anticancer activity. |
Henan University of Chinese Medicine |
31401008 |
34 |
Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review. |
Y. B. Chavan College of Pharmacy |
30888810 |
48 |
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
Sun Yat-Sen University |
31077998 |
81 |
Targeting tropomyosin receptor kinase for cancer therapy. |
China Pharmaceutical University |
30878832 |
57 |
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
Arromax Pharmatech |
31647655 |
114 |
Kinase Chemodiversity from the Arctic: The Breitfussins. |
Uit - The Arctic University of Norway |
30384048 |
365 |
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
University of Florida |
30343954 |
16 |
Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy. |
Eppley Institute For Research In Cancer and Allied Diseases |
30340900 |
37 |
Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors. |
Korea University |
31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
31614258 |
178 |
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
Vichem Chemie Research |
30502115 |
43 |
Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors. |
Lanzhou University |
30234987 |
232 |
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
Palack£ |
26505898 |
123 |
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. |
Novartis Institutes For Biomedical Research |
26509640 |
234 |
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders. |
Abbvie Bioresearch Center |
23275831 |
121 |
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). |
Moffitt Cancer Center |
31200237 |
95 |
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
Shanghai Pharmaceuticals Holding |
19271717 |
96 |
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium. |
Heinrich-Heine-Universitat |
19140666 |
26 |
Structure-based drug design of novel Aurora kinase A inhibitors: structural basis for potency and specificity. |
National Health Research Institutes |
18494522 |
244 |
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense. |
Heinrich-Heine-Universit£T |
30196060 |
39 |
Structure-based drug design: Synthesis and biological evaluation of quinazolin-4-amine derivatives as selective Aurora A kinase inhibitors. |
Sun Yat-Sen University |
30249354 |
112 |
Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. |
Glaxosmithkline R&D |
30241010 |
59 |
Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
East China Normal University |
30143423 |
20 |
Discovery and optimization of novel benzothiophene-3-carboxamides as highly potent inhibitors of Aurora kinases A and B. |
Mta-Se Pathobiochemistry Research Group |
28918096 |
47 |
A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies. |
Nirma University |
29764757 |
72 |
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition. |
The Institute of Cancer Research |
30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
29945794 |
193 |
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups. |
Vertex Pharmaceuticals |
29549836 |
47 |
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. |
Universit£ |
29547832 |
12 |
New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors. |
Universit£ |
29705376 |
12 |
Synthesis and biological evaluation of 2,4-disubstituted phthalazinones as Aurora kinase inhibitors. |
Lanzhou University |
29545102 |
159 |
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor. |
Merck |
29746776 |
14 |
From Cancer to Pain Target by Automated Selectivity Inversion of a Clinical Candidate. |
Heidelberg University |
29466002 |
193 |
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening. |
University of Edinburgh |
28818446 |
21 |
Characterization of a highly selective inhibitor of the Aurora kinases. |
Harvard Medical School |
29656197 |
62 |
Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition. |
National Health Research Institutes |
29358147 |
24 |
Synthesis and biological evaluation of aurora kinases inhibitors based on N-trisubstituted pyrimidine scaffold. |
Sun Yat-Sen University |
29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
29653895 |
210 |
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model. |
Glaxosmithkline |
29437386 |
111 |
Tozasertib Analogues as Inhibitors of Necroptotic Cell Death. |
University of Antwerp |
27726390 |
41 |
Natural-Based Indirubins Display Potent Cytotoxicity toward Wild-Type and T315I-Resistant Leukemia Cell Lines. |
Beckman Research Institute |
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 |
28135235 |
71 |
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. |
Novartis Institutes For Biomedical Research |
24403173 |
12 |
Long residence times revealed by Aurora A kinase-targeting fluorescent probes derived from inhibitors MLN8237 and VX-689. |
University of Tartu |
23534475 |
27 |
De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments. |
University of Dundee |
23279802 |
15 |
Synthesis and Quantum Chemical Studies of New 4-aminoquinazoline Derivatives as Aurora A/B Kinase Inhibitors. |
Southeast University |
22803810 |
79 |
Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors. |
Moffitt Cancer Center |
19359241 |
26 |
Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks. |
University of Manchester |
22248356 |
20 |
A novel mechanism by which small molecule inhibitors induce the DFG flip in Aurora A. |
Moffitt Cancer Center |
21992004 |
78 |
Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen. |
Harvard Medical School |
19199284 |
24 |
Development and biological evaluation of a novel aurora A kinase inhibitor. |
Parc De Recerca Biomedica De Barcelona |
21802008 |
10 |
High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. |
Harvard Medical School |
20426425 |
2 |
Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237. |
University of Sheffield |
19648931 |
16 |
Design, synthesis and selection of DNA-encoded small-molecule libraries. |
Praecis Pharmaceuticals |
19827834 |
93 |
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control. |
Vertex Pharmaceuticals |
19402633 |
53 |
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. |
Genentech |
19603809 |
59 |
Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor. |
Nerviano Medical Sciences |
19143567 |
49 |
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. |
Astex |
18294849 |
11 |
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity. |
Astrazeneca |
17373783 |
62 |
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. |
Astrazeneca |
18307303 |
75 |
Discovery of selective aminothiazole aurora kinase inhibitors. |
Novartis |
18287029 |
12 |
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. |
Plexxikon |
18793847 |
33 |
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors. |
Sunesis Pharmaceuticals |
18630890 |
24 |
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability. |
Genentech |
18656911 |
39 |
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design. |
Astex |
14981513 |
6 |
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. |
Vertex Pharmaceuticals |
17125279 |
15 |
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. |
Nerviano Medical Sciences |
16337122 |
11 |
SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors. |
Astrazeneca |
15828847 |
8 |
Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. |
Nerviano Medical Sciences |
16290148 |
44 |
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors. |
Nerviano Medical Sciences |