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 |
| 28109791 |
44 |
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. |
Chugai Pharmaceutical |
| 27750146 |
58 |
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
Chinese Academy of Sciences |
| 28523108 |
113 |
2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors. |
Chinese Academy of Sciences |
| 27914362 |
54 |
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
The First Affiliated Hospital of Zhengzhou University |
| 27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
| 27933954 |
122 |
Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor. |
Chugai Pharmaceutical |
| 27348537 |
60 |
Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
East China University of Science & Technology |
| 27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
| 27011159 |
97 |
Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
Experimental Therapeutics Centre |
| 27117427 |
77 |
Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
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 |
| 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 |
| 26318067 |
34 |
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors. |
Hanyang University |
| 25474320 |
10 |
Nintedanib: from discovery to the clinic. |
Boehringer Ingelheim Pharma |
| 25736993 |
65 |
Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
Health Science Center Xi'An Jiaotong University |
| 25409491 |
83 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
Zhejiang University |
| 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 |
| 23362959 |
72 |
Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo. |
Sichuan University |
| 22621397 |
39 |
Irreversible protein kinase inhibitors: balancing the benefits and risks. |
Covalution Pharma |
| 23098265 |
46 |
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. |
University of Genoa |
| 22695126 |
98 |
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. |
Abbott Laboratories |
| 21608528 |
166 |
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. |
Merck Research Laboratories |
| 20570525 |
56 |
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase. |
Chinese Academy of Sciences |
| 18183025 |
12060 |
A quantitative analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
| 18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
| 18324761 |
65 |
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation. |
Amgen |
| 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 |
| 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 |
| 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 |
| 22056746 |
53 |
Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. |
Boehringer Ingelheim Pharmaceuticals |
| 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 |
| 22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang 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 |
| 21823617 |
58 |
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors. |
Chugai Pharmaceutical |
| 21561767 |
48 |
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. |
Ariad Pharmaceuticals |
| 21517068 |
45 |
Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity. |
East China University of Science and Technology |
| 21561771 |
39 |
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors. |
Chugai Pharmaceutical |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 18559524 |
21 |
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. |
Boehringer Ingelheim Austria |
| 20143778 |
70 |
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. |
Curis |
| 20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
| 19888761 |
52 |
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer. |
Hanmi Research Center |
| 15999992 |
25 |
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors. |
Johnson & Johnson Pharmaceutical Research and Development |
| 15743179 |
79 |
Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas. |
Kirin Brewery |
| 15711537 |
653 |
A small molecule-kinase interaction map for clinical kinase inhibitors. |
Ambit Biosciences |
| 15012985 |
31 |
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
Kirin Brewery |
| 11934592 |
24 |
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. |
Merck Research Laboratories |
| 32278710 |
48 |
Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2. |
Astellas Pharma |
| 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 |
| 27326339 |
92 |
Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
Shanghai Institute of Materia Medica |
| 30403487 |
21 |
Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. |
Jinan University |
| 29522671 |
80 |
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
Chinese Academy of Sciences |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 30888810 |
48 |
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
Sun Yat-Sen University |
| 30763817 |
39 |
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach. |
University of Naples Federico Ii |
| 30987781 |
88 |
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. |
Southeast University |
| 30529543 |
57 |
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance. |
China Pharmaceutical 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 |
| 31934767 |
42 |
Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an |
Chinese Academy of Sciences |
| 31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
| 31335138 |
56 |
Discovery and Development of a Series of Pyrazolo[3,4- |
Shanghai University |
| 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 |
| 29775937 |
52 |
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
Chinese Academy of Sciences |
| 30170943 |
35 |
Design and synthesis of potent RSK inhibitors. |
Novartis Institutes For Biomedical Research |
| 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 |
| 29259745 |
29 |
Identification of an Indazole-Based Pharmacophore for the Inhibition of FGFR Kinases Using Fragment-Led |
University of Leeds |
| 28687204 |
32 |
Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
Fudan University |
| 28521156 |
65 |
2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors. |
Guangzhou Institutes of Biomedicine and Health |
| 29499108 |
118 |
Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors. |
Chinese Academy of Sciences |
| 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 |
| 27231830 |
27 |
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies. |
Aimst University |
| 11828475 |
5 |
Dynamic deconvolution of a pre-equilibrated dynamic combinatorial library of acetylcholinesterase inhibitors. |
UniversitÉ |
| 17718712 |
11 |
Crystal structure of the T315I mutant of AbI kinase. |
Ariad Pharmaceuticals |
| 20632 |
7 |
Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding. |
TBA |
| 10322128 |
13 |
Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3. |
Ligand Pharmaceuticals |
| 21079602 |
5 |
Ultrasensitive in situ visualization of active glucocerebrosidase molecules. |
Leiden University |
| | 48 |
Thermodynamic and Nuclear Magnetic Resonance Study of the Reactions of α- and β-Cyclodextrin with Acids, Aliphatic Amines, and Cyclic Alcohols |
Nist |
| 19836248 |
35 |
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3. |
Wyeth Research |
| 19167883 |
5 |
Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines. |
Gilead Sciences |
| 19012392 |
15 |
Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases. |
Shanghai Institute of Organic Chemistry |
| 16509577 |
52 |
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors. |
Gsk |
| 17681466 |
61 |
Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists. |
Boehringer Ingelheim Pharmaceuticals |
| 11567092 |
4 |
Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors. |
Gsk |
| 16495061 |
8 |
Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent. |
Johnson & Johnson Pharmaceutical |
| 17570665 |
19 |
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping. |
Vernalis (R&D) |
| 16945533 |
33 |
p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design. |
Merck Research Laboratories |
| 16913712 |
21 |
Novel small-molecule inhibitors of anthrax lethal factor identified by high-throughput screening. |
Montana State University |
| 16759095 |
56 |
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors. |
Abbott Laboratories |
| 11063609 |
36 |
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
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