The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 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 |
| 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 |
| 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 |
| 26071372 |
89 |
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3. |
Astellas Pharma |
| 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 |
| 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 |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 17684099 |
4 |
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
Center For Molecular Medicine of The Austrian Academy of Sciences |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 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 |
| 18819794 |
53 |
Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead. |
Johnson & Johnson |
| 17499505 |
78 |
Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
| 16682193 |
62 |
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 16260132 |
6 |
Synthesis of N-benzylated-2-aminoquinolines as ligands for the Tec SH3 domain. |
The University of Adelaide |
| 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 |
| 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 |
| 31922756 |
106 |
Developing Inhibitors of the p47phox-p22phox Protein-Protein Interaction by Fragment-Based Drug Discovery. |
University of Copenhagen |
| 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 |
| 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 |
| 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 |
| 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 |
| 30034582 |
72 |
Covalent Inhibitors of the TEC Family of Kinases and Their Methods of Use. |
Temple University |
| 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 |
| 29631132 |
33 |
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
Shaanxi University of Science & Technology |
| 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 |
| 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 |
| 28433531 |
69 |
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping. |
Wuxi Apptec (Shanghai) |
| 27791347 |
41 |
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. |
Pfizer |
| 23594111 |
7 |
Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer. |
Chinese Academy of Sciences |
Search and Browse
