The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28109791 |
44 |
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. |
Chugai Pharmaceutical |
| 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 |
| 26286460 |
25 |
Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration. |
University of Michigan |
| 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 |
| 25022204 |
78 |
Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells. |
Universit£ |
| 25589926 |
20 |
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase. |
Astex Pharmaceuticals |
| 22819505 |
46 |
Discovery and characterization of novel allosteric FAK inhibitors. |
Takeda Pharmaceutical |
| 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 |
| 23253074 |
38 |
Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography. |
University of Zurich |
| 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 |
| 22827572 |
67 |
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). |
Glaxosmithkline |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 17850214 |
99 |
The selectivity of protein kinase inhibitors: a further update. |
University of Dundee |
| 18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
| 17371799 |
12 |
Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr |
Targegen |
| 18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
| 18311895 |
27 |
Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. |
Targegen |
| 17113292 |
73 |
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. |
Targegen |
| 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 |
| 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 |
| 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 |
| 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 |
| 20961062 |
42 |
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity. |
Pfizer |
| 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 |
| 20655209 |
18 |
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities. |
Université |
| 20218623 |
68 |
Emerging targets in osteoporosis disease modification. |
Amgen |
| 20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
| 19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
| 16931012 |
61 |
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors. |
Targegen |
| 15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
| 15615512 |
21 |
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. |
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 |
| 11527723 |
32 |
A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain. |
Ariad Pharmaceuticals |
| 31818631 |
13 |
Exploring structure-promiscuity relationships using dual-site promiscuity cliffs and corresponding single-site analogs. |
Rheinische Friedrich-Wilhelms-Universit£T |
| 30769179 |
24 |
Pharmacological urate-lowering approaches in chronic kidney disease. |
West China Hospital of Sichuan University |
| 31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 31268308 |
36 |
Multistage Screening Reveals 3-Substituted Indolin-2-one Derivatives as Novel and Isoform-Selective c-Jun N-terminal Kinase 3 (JNK3) Inhibitors: Implications to Drug Discovery for Potential Treatment of Neurodegenerative Diseases. |
Peking University |
| 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 |
| 23787099 |
20 |
Identification of potent Yes1 kinase inhibitors using a library screening approach. |
Frederick National Laboratory For Cancer Research |
| 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 |
| 28259529 |
31 |
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
The Ohio State University |
| 23935099 |
16 |
Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket. |
Glaxosmithkline |
| 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 |
Search and Browse
