The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28665128 |
86 |
Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. |
Principia Biopharma |
| 28140585 |
52 |
Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor. |
High Magnetic Field Laboratory |
| 27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
| 27583770 |
82 |
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke |
Bristol-Myers Squibb Research And Development |
| 26555154 |
36 |
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. |
University Of Edinburgh |
| 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 |
| 26675441 |
46 |
Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability. |
Genentech |
| 26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
| 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 |
| 26087137 |
30 |
Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase. |
Takeda California |
| 26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute Of The Novartis Research Foundation |
| 25205190 |
66 |
Discovery of (E)-5-(benzylideneamino)-1H-benzo[d]imidazol-2(3H)-one derivatives as inhibitors for PTK6. |
Yonsei University |
| 24915291 |
73 |
Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
Peking University |
| 24685542 |
67 |
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases. |
Bristol-Myers Squibb Research And Development |
| 24900590 |
55 |
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy. |
Glaxosmithkline |
| 23490150 |
48 |
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. |
Takeda Pharmaceutical |
| 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 |
| 22394077 |
19 |
Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
Hoffmann-La Roche |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
| 18667312 |
24 |
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
The Scripps Research Institute |
| 17185414 |
30 |
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
Genomics Institute Of The Novartis Research Foundation |
| 17499505 |
78 |
Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
| 15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
| 28315597 |
85 |
Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor. |
University Of Science And Technology Of China |
| 29457982 |
80 |
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
Genentech |
| 28945083 |
33 |
In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery. |
National Institute Of Biological Sciences, Beijing |
| 27231830 |
27 |
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies. |
Aimst University |
| 19269962 |
3 |
Reduced expression of CD45 protein-tyrosine phosphatase provides protection against anthrax pathogenesis. |
United States Army Medical Research Institute Of Infectious Diseases |
| 16492149 |
16 |
Structure-based optimization of MurF inhibitors. |
Abbott Laboratories |
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