The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
| 28109791 |
44 |
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. |
Chugai Pharmaceutical |
| 28076826 |
27 |
Identification of new pyrrolo[2,3-d]pyrimidines as Src tyrosine kinase inhibitors in vitro active against Glioblastoma. |
Universit£ |
| 27884697 |
65 |
3-Cyano-6-(5-methyl-3-pyrazoloamino) pyridines (Part 2): A dual inhibitor of Aurora kinase and tubulin polymerization. |
Cxs |
| 27994749 |
47 |
Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. |
Astrazeneca |
| 27115835 |
85 |
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
University of Edinburgh |
| 27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
| 27010810 |
24 |
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
Oribase Pharma |
| 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 |
| 26396681 |
58 |
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma. |
Novartis Institutes For Biomedical Research |
| 26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
| 26288682 |
64 |
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors. |
Bristol-Myers Squibb Research & Development |
| 25965804 |
80 |
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
Eli Lilly |
| 25923950 |
23 |
Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors. |
Universit£ |
| 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 |
| 25205190 |
66 |
Discovery of (E)-5-(benzylideneamino)-1H-benzo[d]imidazol-2(3H)-one derivatives as inhibitors for PTK6. |
Yonsei University |
| 24904961 |
27 |
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
Qilu Pharmaceutical |
| 22819505 |
46 |
Discovery and characterization of novel allosteric FAK inhibitors. |
Takeda Pharmaceutical |
| 23398373 |
88 |
Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases. |
Vertex Pharmaceuticals |
| 23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
| 22726925 |
216 |
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease. |
Cellzome |
| 23061660 |
92 |
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. |
Genentech |
| 22738630 |
76 |
Structure-based optimization of aminopyridines as PKC¿ inhibitors. |
Vertex Pharmaceuticals |
| 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 |
| 22465635 |
95 |
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. |
Abbott Laboratories |
| 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 |
| 18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
| 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 |
| 18023347 |
74 |
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors. |
Abbott Laboratories |
| 17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
| 17315853 |
14 |
Homology modeling of human Fyn kinase structure: discovery of rosmarinic acid as a new Fyn kinase inhibitor and in silico study of its possible binding modes. |
Glaxosmithkline |
| 16460940 |
13 |
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. |
Hoffmann-La Roche |
| 22269278 |
50 |
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation. |
Chugai Pharmaceutical |
| 15953730 |
13 |
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation. |
Hoffmann-La Roche |
| 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 |
| 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 |
| 21958547 |
108 |
Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. |
Pfizer |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 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 |
| 21536449 |
16 |
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin. |
The Institute of Cancer Research |
| 21605975 |
31 |
Discovery of a macrocyclic o-aminobenzamide Hsp90 inhibitor with heterocyclic tether that shows extended biomarker activity and in vivo efficacy in a mouse xenograft model. |
Pfizer |
| 20573509 |
23 |
3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. |
Mitsubishi Tanabe Pharma |
| 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 |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 19039322 |
50 |
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. |
Center For Molecular Medicine of The Austrian Academy of Sciences |
| 16783341 |
34 |
Rational design of inhibitors that bind to inactive kinase conformations. |
Novartis Research Foundation |
| 16408016 |
6 |
Assignment of protein function in the postgenomic era. |
The Scripps Research Institute |
| 17334377 |
23 |
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. |
University of California |
| 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 |
| 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 |
| 19884006 |
47 |
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. |
Wyeth Research |
| 19879134 |
94 |
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4. |
Cgi Pharmaceuticals |
| 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 |
| 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 |
| 19857964 |
3 |
Structural basis for the inhibitor recognition of human Lyn kinase domain. |
Osaka Prefecture University |
| | 14 |
Covalent binding of catechols to src family SH2 domains |
TBA |
| 19364658 |
113 |
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). |
Wyeth Research |
| 19111463 |
46 |
Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors. |
Wyeth Research |
| 19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
| 18606543 |
68 |
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta. |
Wyeth Research |
| 15919995 |
4 |
Structural bioinformatics-based design of selective, irreversible kinase inhibitors. |
University of California |
| 17425296 |
161 |
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel. |
Abbott Laboratories |
| 17391959 |
100 |
Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors. |
Abbott Laboratories |
| 17303421 |
56 |
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
Roche Research Center |
| 17234410 |
82 |
Discovery of thienopyridines as Src-family selective Lck inhibitors. |
Abbott Bioresearch Center |
| 16931012 |
61 |
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors. |
Targegen |
| 16682193 |
62 |
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 16366598 |
51 |
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. |
Johnson & Johnson Pharmaceutical Research and Development |
| 16216497 |
67 |
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. |
Abbott Bioresearch Center |
| 15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
| 15546730 |
9 |
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 15317463 |
16 |
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 14684325 |
154 |
Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase. |
Sugen |
| 14592495 |
60 |
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 12941315 |
19 |
Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines. |
Wyeth Research |
| 12852972 |
79 |
Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 12482439 |
51 |
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase. |
Merck Research Laboratories |
| 12217360 |
27 |
Design and characterization of non-phosphopeptide inhibitors for Src family SH2 domains. |
Mogam Biotechnology Research Institute |
| 12086485 |
10 |
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. |
Boehringer Ingelheim Pharmaceuticals |
| 12039590 |
51 |
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck. |
Abbott Bioresearch Center |
| 11934592 |
24 |
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. |
Merck Research Laboratories |
| 11909733 |
30 |
Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
Institute of Molecular and Cell Biology |
| 31818631 |
13 |
Exploring structure-promiscuity relationships using dual-site promiscuity cliffs and corresponding single-site analogs. |
Rheinische Friedrich-Wilhelms-Universit£T |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 11012022 |
102 |
Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II. |
Basf Bioresearch |
| 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 |
| 30562697 |
84 |
The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
University of Silesia In Katowice |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 31400706 |
6 |
Identification of a new family of pyrazolo[3,4-d]pyrimidine derivatives as multitarget Fyn-Blk-Lyn inhibitors active on B- and T-lymphoma cell lines. |
University of Siena |
| 30875504 |
34 |
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
Sichuan University and Collaborative Innovation Center |
| 31260299 |
14 |
Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis. |
Tsinghua University |
| 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 |
| 31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
| 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 |
| 10072676 |
15 |
Acquisition of high-affinity, SH2-targeted ligands via a spatially focused library. |
The Albert Einstein College of Medicine of Yeshiva University |
| 30114661 |
3 |
Pyrrolopyrimidines: An update on recent advancements in their medicinal attributes. |
Indo-Soviet Friendship College of Pharmacy (Isfcp) |
| 28814374 |
19 |
From bench (laboratory) to bed (hospital/home): How to explore effective natural and synthetic PAK1-blockers/longevity-promoters for cancer therapy. |
Pak Research Center |
| 30480444 |
85 |
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model. |
Sichuan University/Collaborative Innovation Center of Biotherapy |
| 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 |
| 28734581 |
37 |
Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
Sichuan University and Collaborative Innovation Center |
| 28720503 |
146 |
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis. |
Merck |
| 28945083 |
33 |
In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery. |
National Institute of Biological Sciences, Beijing |
| 16051698 |
5 |
Characterization of isoprenaline- and salmeterol-stimulated interactions between beta2-adrenoceptors and beta-arrestin 2 using beta-galactosidase complementation in C2C12 cells. |
Institute of Cell Signaling |
| 15590769 |
16 |
Inverse agonism and neutral antagonism at wild-type and constitutively active mutant delta opioid receptors. |
I.G.B.M.C. |
| 12616631 |
18 |
D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. |
University of Queensland Brisbane |
| 16492149 |
16 |
Structure-based optimization of MurF inhibitors. |
Abbott Laboratories |
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