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 |
| 30893553 |
62 |
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
Bristol-Myers Squibb Research and Development |
| 32292564 |
138 |
Efficacy and Tolerability of Pyrazolo[1,5- |
The Genomics Institute of The Novartis Research Foundation |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 27491711 |
422 |
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. |
Merck And |
| 27531604 |
55 |
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177). |
Bristol-Myers Squibb Research and Development |
| 31381333 |
302 |
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
TBA |
| 31138459 |
50 |
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens. |
Biogen |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 32083858 |
145 |
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
TBA |
| 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 |
| 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 |
| 28139931 |
85 |
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. |
Pfizer |
| 28986130 |
11 |
Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents. |
Dalian Medical University |
| 30423248 |
226 |
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. |
Pfizer |
| 30097367 |
96 |
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series. |
Bristol-Myers Squibb |
| 30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
| 29715023 |
56 |
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. |
China Pharmaceutical University |
| 28279528 |
53 |
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis. |
Advinus Therapeutics |
| 29631132 |
33 |
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
Shaanxi University of Science & Technology |
| 28628824 |
98 |
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors. |
University of Science and Technology of China |
| 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 |
| 28282122 |
9 |
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
High Magnetic Field Laboratory |
| 28337328 |
6 |
Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent. |
Dana-Farber Cancer Institute |
| 28438385 |
24 |
Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth. |
Indiana University School of Medicine |
| 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 |
| 11303063 |
11 |
Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland. |
Creighton University |
| 9832156 |
13 |
Characterization of (2S,2'R,3'R)-2-(2',3'-[3H]-dicarboxycyclopropyl)glycine binding in rat brain. |
F. Hoffmann-La Roche |
| 8996185 |
121 |
Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. |
SynthÉLabo Recherche |
| 16492149 |
16 |
Structure-based optimization of MurF inhibitors. |
Abbott Laboratories |
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