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 |
| 27769623 |
21 |
Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
Ocean University of China |
| 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 |
| 27106711 |
87 |
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2). |
Green Valley Research Institute |
| 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 |
| 26222319 |
192 |
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. |
Nerviano Medical Sciences |
| 25965804 |
80 |
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. |
Eli Lilly |
| 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 |
| 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 |
| 25124116 |
19 |
4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors. |
Korea Research Institute of Chemical Technology |
| 24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
| 24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
| 24900886 |
66 |
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors. |
Chinese Academy of Sciences |
| 24565969 |
69 |
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors. |
Chinese Academy of Sciences |
| 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 |
| 24167659 |
15 |
Design and Synthesis of Potent Bivalent Peptide Agonists Targeting the EphA2 Receptor. |
State University of New York |
| 23489211 |
44 |
Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor. |
Universit£ |
| 23312943 |
166 |
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
| 22765894 |
223 |
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. |
Exelixis |
| 23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
| 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 |
| 22863529 |
31 |
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors. |
Chinese Academy of Sciences |
| 22168626 |
32 |
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. |
Ambit Biosciences |
| 20570525 |
56 |
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase. |
Chinese Academy of Sciences |
| 19716697 |
110 |
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II. |
Boehringer Ingelheim Pharmaceuticals |
| 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 |
| 17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott 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 |
| 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 |
| 21999461 |
90 |
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase. |
RhôNe-Poulenc Rorer |
| 22037378 |
31824 |
Comprehensive analysis of kinase inhibitor selectivity. |
Ambit Biosciences |
| 21665484 |
37 |
Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold. |
Chinese Academy of Sciences |
| 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 |
| 21470862 |
110 |
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. |
Nerviano Medical Sciences |
| 21405128 |
47 |
Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent. |
Chinese Academy of Sciences |
| 21341678 |
49 |
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. |
Millennium Pharmaceuticals |
| 20932747 |
61 |
The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity. |
Ansaris |
| 19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
| 20346655 |
117 |
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases. |
Abbott Laboratories |
| 19879134 |
94 |
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4. |
Cgi Pharmaceuticals |
| 20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
| 19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
| 19788238 |
36 |
Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). |
University of Zurich |
| 19356929 |
17 |
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
| 19035792 |
85 |
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. |
Glaxosmithkline |
| 19019675 |
52 |
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK? |
Pfizer |
| 17360676 |
3 |
c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
Harvard Medical School |
| 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 |
| 32202781 |
37 |
Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads. |
Bicycletx |
| 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 |
| 29522671 |
80 |
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
Chinese Academy of Sciences |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 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 |
| 31335138 |
56 |
Discovery and Development of a Series of Pyrazolo[3,4- |
Shanghai University |
| 26509640 |
234 |
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders. |
Abbvie Bioresearch Center |
| 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 |
| 28780190 |
11 |
Targeting Eph/ephrin system in cancer therapy. |
University of Parma |
| 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 |
| 29470068 |
4 |
Reduction of Circulating Cancer Cells and Metastases in Breast-Cancer Models by a Potent EphA2-Agonistic Peptide-Drug Conjugate. |
University of California |
| 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 |
| 30075624 |
71 |
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2. |
Jinan 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 |
| 29111705 |
4 |
One-Bead-Two-Compound Thioether Bridged Macrocyclic?-AApeptide Screening Library against EphA2. |
University of South Florida |
| 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 |
| 18387300 |
90 |
Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition. |
Pfizer |
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