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 |
28094183 |
25 |
Discovering novel 7-azaindole-based series as potent AXL kinase inhibitors. |
Oribase Pharma |
28082036 |
23 |
Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate. |
Takeda California |
27994735 |
163 |
Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors. |
University of North Carolina At Chapel Hill |
27299736 |
37 |
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules. |
St. John'S University |
27131066 |
36 |
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
Chinese Academy of Sciences |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
26555154 |
36 |
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. |
University of Edinburgh |
27061987 |
40 |
Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor. |
Chinese Academy of Sciences (Cas) |
26951753 |
336 |
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
26717201 |
68 |
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs. |
Shenyang Pharmaceutical University |
26698536 |
56 |
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
Chinese Academy of Sciences |
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 |
26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
26005523 |
37 |
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors. |
Shanghai Institute of Materia Medica |
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 |
25827399 |
52 |
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis. |
Chinese Academy of Sciences |
25633741 |
67 |
Discovery and profiling of a selective and efficacious Syk inhibitor. |
Novartis Institutes For Biomedical Research |
25068800 |
34 |
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. |
University of North Carolina At Chapel Hill |
24785465 |
80 |
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
Chinese Academy of Sciences |
24904961 |
27 |
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
Qilu Pharmaceutical |
24479418 |
39 |
Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia. |
Heinrich Heine Universit£T |
24328302 |
94 |
Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum. |
Heinrich-Heine-Universit£T D£Sseldorf |
24219778 |
139 |
Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. |
Eshelman School of Pharmacy�Department of Pharmacology�Lineberger Compreh |
24195762 |
135 |
Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. |
University of North Carolina At Chapel Hill |
24900750 |
14 |
Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors. |
Southern Medical University |
24157370 |
22 |
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors. |
Chugai Pharmaceutical |
23993328 |
41 |
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
Chinese Academy of Sciences |
22749189 |
24 |
Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
Institut Curie |
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 |
23312472 |
129 |
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
22932313 |
9 |
Design and synthesis of diarylamines and diarylethers as cytotoxic antitumor agents. |
Beijing Institute of Pharmacology & Toxicology |
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 |
22734674 |
81 |
The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer. |
Amgen |
22039836 |
188 |
Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141). |
Johnson & Johnson Pharmaceutical Research & Development |
22863529 |
31 |
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors. |
Chinese Academy of Sciences |
22662287 |
116 |
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia. |
TBA |
22247788 |
40 |
Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. |
TBA |
24900361 |
27 |
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets. |
TBA |
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 |
18342505 |
43 |
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
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 |
22221201 |
32 |
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
University of Kentucky |
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 |
22119469 |
107 |
Novel and selective spiroindoline-based inhibitors of Sky kinase. |
Pfizer |
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 |
21982797 |
128 |
9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp. |
Peking University |
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 |
21812414 |
106 |
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
Pfizer |
21741249 |
32 |
Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp. |
Heinrich Heine Universit£T |
24900250 |
81 |
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277 |
TBA |
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 |
20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
19053831 |
39 |
Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles. |
Institute of General Genetics |
19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
18248988 |
16 |
Entry into a new class of protein kinase inhibitors by pseudo ring design. |
Novartis Institutes For Biomedical Research |
18242992 |
30 |
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents. |
Johnson & Johnson Pharmaceutical Research & Development |
16934458 |
124 |
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors. |
Valeant Pharmaceuticals Research & Development |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
27448775 |
102 |
Discovery and optimization of a series of imidazo[4,5-b]pyrazine derivatives as highly potent and exquisitely selective inhibitors of the mesenchymal-epithelial transition factor (c-Met) protein kinase. |
Shanghai Pharmaceuticals Holding |
27379978 |
140 |
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors. |
Chinese Academy of Sciences |
30685094 |
22 |
Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)amino)pyrazine core. |
Shanghai University |
31693351 |
473 |
Discovery of 4 |
TBA |
31677447 |
44 |
Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold. |
Central China Normal University |
29928803 |
92 |
Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors. |
Vichem Chemie Research |
31207462 |
42 |
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. |
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital |
30987781 |
88 |
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. |
Southeast University |
30503936 |
10 |
Discovery of N |
Zhuhai Campus of Zunyi Medical University |
30188734 |
41 |
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. |
University of Arkansas For Medical Sciences |
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 |
30340900 |
37 |
Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors. |
Korea University |
31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
30347155 |
155 |
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group. |
Unc Eshelman School of Pharmacy |
30170943 |
35 |
Design and synthesis of potent RSK inhibitors. |
Novartis Institutes For Biomedical Research |
30309671 |
12 |
Design, synthesis, biological evaluation and cellular imaging of imidazo[4,5-b]pyridine derivatives as potent and selective TAM inhibitors. |
Psl Research University |
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 |
29466002 |
193 |
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening. |
University of Edinburgh |
29407963 |
47 |
Identification of novel N |
Zhuhai Campus of Zunyi Medical University |
28755635 |
25 |
Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors. |
China Pharmaceutical University |
28929759 |
83 |
Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease. |
Wuxi Apptec |
28711351 |
74 |
Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. |
Rigel Pharmaceuticals |
28460311 |
8 |
The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3? inhibitors for the treatment of ovarian cancer. |
Fudan University |
28411455 |
45 |
Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization. |
Shanghai Pharmaceuticals Holding |
28714692 |
232 |
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
University of Chinese Academy of Sciences |
11714892 |
4 |
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract. |
Recordati |
11408556 |
2 |
Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors. |
Astrazeneca Pharmaceuticals |
17512966 |
4 |
Structure-based discovery of a new class of Bcl-xL antagonists. |
Burnham Institute For Medical Research |
9650799 |
159 |
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
Novartis Pharma |
19270684 |
3 |
Transition state analogs of 5'-methylthioadenosine nucleosidase disrupt quorum sensing. |
Albert Einstein College of Medicine |
18370373 |
48 |
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo. |
Irbm/Merck Research Laboratories |
16439135 |
24 |
Chlamydocin analogs bearing carbonyl group as possible ligand toward zinc atom in histone deacetylases. |
Kyushu Institute of Technology |
15916442 |
52 |
Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles. |
Wyeth Research |
11728184 |
20 |
Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity. |
Biocryst Pharmaceuticals |