The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28279846 |
36 |
Design, synthesis, and biological evaluation of novel 4-anilinoquinazoline derivatives bearing amino acid moiety as potential EGFR kinase inhibitors. |
Xuzhou Medical University |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
28109791 |
44 |
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. |
Chugai Pharmaceutical |
28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
27816515 |
143 |
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors. |
Merck |
28011202 |
21 |
Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors. |
Shenyang Pharmaceutical University |
27490023 |
25 |
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
27474925 |
40 |
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
Shenyang Pharmaceutical University |
27391135 |
28 |
3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents. |
Egyptian Russian University |
27299736 |
37 |
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules. |
St. John'S University |
27187857 |
17 |
Synthesis and biological evaluation of 4-(2-fluorophenoxy)-3,3'-bipyridine derivatives as potential c-met inhibitors. |
Shenyang Pharmaceutical University |
27396929 |
11 |
Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors. |
Shanghai University of Traditional Chinese Medicine |
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 |
27131066 |
36 |
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
Chinese Academy of Sciences |
27258622 |
47 |
Novel c-Met inhibitory olive secoiridoid semisynthetic analogs for the control of invasive breast cancer. |
University of Louisiana At Monroe |
27155466 |
12 |
Discovery of a novel 6,7-disubstituted-4-(2-fluorophenoxy)quinolines bearing 1,2,3-triazole-4-carboxamide moiety as potent c-Met kinase inhibitors. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
27068889 |
26 |
Design, synthesis and biological evaluation of 4-aminopyrimidine-5-cabaldehyde oximes as dual inhibitors of c-Met and VEGFR-2. |
China Pharmaceutical University |
27184766 |
5 |
Synthesis, antitumor evaluation and molecular docking studies of [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine derivatives. |
Taizhou Vocational & Technical College |
26555154 |
36 |
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. |
University of Edinburgh |
27003761 |
120 |
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. |
Nerviano Medical Sciences |
27117263 |
51 |
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors. |
Takeda Pharmaceutical |
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 |
27106709 |
92 |
Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening. |
Korea Research Institute of Chemical Technology |
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) |
27043268 |
16 |
Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Ka/mTOR inhibitors. |
Jiangxi Science & Technology Normal University |
27017548 |
23 |
Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors. |
Shanghai Institute of Materia Medica |
26812066 |
34 |
Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity. |
Amgen |
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 |
26964675 |
5 |
Synthesis, and docking studies of phenylpyrimidine-carboxamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors. |
Jiangxi Science & Technology Normal University |
26923692 |
34 |
Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors. |
Jiangxi Science and Technology Normal University |
26944614 |
14 |
Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 2-oxo-4-chloro-1,2-dihydroquinoline-3-carboxamide moiety. |
Jiangxi Science and Technology Normal University |
26897090 |
18 |
Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors. |
Shenyang Pharmaceutical University |
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 |
26526740 |
111 |
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors. |
Univ. Lille |
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 |
26344595 |
26 |
Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors. |
Xi'An Jiaotong University |
26243370 |
25 |
Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004. |
Laboratoires Chemrf Inc/Chemrf Laboratories |
26112445 |
12 |
Design and synthesis of constrained analogs of LCRF-0004 as potent RON tyrosine kinase inhibitors. |
Laboratoires Chemrf Inc/Chemrf Laboratories |
26277759 |
31 |
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors. |
China Pharmaceutical University |
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 |
26169763 |
39 |
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
25282672 |
18 |
Design and optimization of novel 4-(2-fluorophenoxy)quinoline derivatives bearing a hydrazone moiety as c-Met kinase inhibitors. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
25082515 |
44 |
Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2. |
China Pharmaceutical University |
25007344 |
73 |
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics. |
Christian-Albrechts-University of Kiel |
26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute of The Novartis Research Foundation |
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 |
25953155 |
16 |
Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor. |
Chemrf Laboratories |
25827399 |
52 |
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis. |
Chinese Academy of Sciences |
25699405 |
57 |
Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors. |
Amgen |
25827523 |
275 |
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors. |
Vertex Pharmaceuticals |
25736998 |
37 |
Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors. |
Merck Serono |
25461320 |
46 |
Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
Korea University of Science and Technology |
25537530 |
37 |
Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d]isoxazole or 3-aminoindazole scaffold. |
China Pharmaceutical University |
25068800 |
34 |
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. |
University of North Carolina At Chapel Hill |
25036791 |
56 |
Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor. |
National Taiwan University |
24980703 |
296 |
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors. |
Nerviano Medical Sciences |
24951334 |
34 |
Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors. |
Central China Normal University |
24913714 |
53 |
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres. |
Merck Research Laboratories |
24882675 |
12 |
Design, synthesis and biological evaluation of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 4-oxo-3,4-dihydrophthalazine-1-carboxamide moieties as c-Met kinase inhibitors. |
Shenyang Pharmaceutical University |
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 |
25529740 |
12 |
Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
Soochow University |
25438768 |
44 |
Discovery andw biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
25409491 |
83 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
Zhejiang University |
25313996 |
91 |
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. |
Merck Research Laboratories |
25282552 |
30 |
Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors. |
Sungkyunkwan University |
25200979 |
31 |
Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors. |
Shanghai Institute of Materia Medica (Simm) |
25148209 |
58 |
Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer. |
Hutchison Medipharma |
24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
24996144 |
20 |
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
24944742 |
63 |
Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity. |
Shanghai Institute of Materia Medica |
24792774 |
24 |
Discovery of novel type II c-Met inhibitors based on BMS-777607. |
Fudan University |
24773549 |
20 |
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties. |
Development Center For Biotechnology |
24900831 |
62 |
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities. |
State Key Laboratory of Drug Research |
24900830 |
46 |
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
Vichem Chemie Research |
24569110 |
11 |
Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk. |
University of Zurich |
23906342 |
14 |
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. |
Takeda Pharmaceutical |
24485123 |
43 |
Discovery of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety as c-Met kinase inhibitors. |
Shenyang Pharmaceutical University |
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 |
24216091 |
24 |
Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors. |
Takeda Pharmaceutical |
24210504 |
106 |
Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. |
Korea Research Institute of Chemical Technology |
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 |
24100158 |
148 |
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). |
Nerviano Medical Sciences |
23993328 |
41 |
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
Chinese Academy of Sciences |
24044867 |
86 |
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
Califia Bio |
24012712 |
10 |
Design, synthesis, and structure-activity relationships of novel 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
23944843 |
60 |
Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats. |
Pfizer |
23838381 |
38 |
Discovery and optimization of novel 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazones as c-Met kinase inhibitors. |
Shenyang Pharmaceutical University |
23937569 |
22 |
Selectivity data: assessment, predictions, concordance, and implications. |
Eli Lilly |
23920481 |
25 |
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases. |
The Institute of Cancer Research |
23773865 |
49 |
Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. |
Osi Pharmaceuticals |
23742252 |
81 |
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase |
Genomics Institute of The Novartis Research Foundation |
23702473 |
10 |
Indazoles as potential c-Met inhibitors: design, synthesis and molecular docking studies. |
Guangdong Pharmaceutical University |
23644189 |
12 |
Design, synthesis and antitumour activity of bisquinoline derivatives connected by 4-oxy-3-fluoroaniline moiety. |
Shenyang Pharmaceutical University |
23628470 |
40 |
Discovery of novel 4-(2-fluorophenoxy)quinoline derivatives bearing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety as c-Met kinase inhibitors. |
Shenyang Pharmaceutical University |
23602398 |
43 |
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors. |
Merck Research Laboratories |
23587425 |
37 |
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors. |
Merck Research Laboratories |
23535330 |
83 |
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors. |
Merck Research Laboratories |
23474386 |
26 |
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors. |
Chinese Academy of Sciences |
23490150 |
48 |
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. |
Takeda Pharmaceutical |
23434140 |
35 |
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis. |
East China University of Science and Technology |
23403296 |
2 |
Olive secoiridoids and semisynthetic bioisostere analogues for the control of metastatic breast cancer. |
University of Louisiana At Monroe |
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 |
23249297 |
75 |
Trimeric hemibastadin congener from the marine sponge Ianthella basta. |
Heinrich-Heine University |
24900685 |
8 |
Anthraquinone Derivatives as Potent Inhibitors of c-Met Kinase and the Extracellular Signaling Pathway. |
Soochow University |
23379595 |
55 |
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met. |
Merck |
23312472 |
129 |
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
Pfizer |
21835616 |
41 |
The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach. |
Astrazeneca |
23123015 |
22 |
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors. |
Takeda Pharmaceutical |
23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
22883026 |
34 |
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives. |
Takeda Pharmaceutical |
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 |
23116168 |
42 |
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations. |
Sichuan University |
23098265 |
46 |
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. |
University of Genoa |
22934600 |
1 |
Potent HGF/c-Met axis inhibitors from Eucalyptus globulus: the coupling of phloroglucinol and sesquiterpenoid is essential for the activity. |
Chinese Academy of Sciences |
22924734 |
87 |
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of |
Pfizer |
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 |
22548342 |
210 |
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. |
Exelixis |
22985853 |
22 |
Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: synthesis and SAR study as tyrosine kinase c-Met inhibitors. |
China Pharmaceutical University |
22980219 |
55 |
Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy. |
Takeda Pharmaceutical |
22863529 |
31 |
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors. |
Chinese Academy of Sciences |
22727637 |
85 |
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors. |
Abbott Laboratories |
22738630 |
76 |
Structure-based optimization of aminopyridines as PKC¿ inhibitors. |
Vertex Pharmaceuticals |
22452518 |
22 |
Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. |
Sichuan University |
22439974 |
79 |
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders. |
Takeda Pharmaceutical |
22404346 |
52 |
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. |
The Institute of Cancer Research |
22372864 |
25 |
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases. |
Hanmi Research Center |
22595176 |
31 |
Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors. |
Amgen |
22579487 |
53 |
Synthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors. |
Korea Research Institute of Chemical Technology |
22320343 |
21 |
Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives. |
Amgen |
22320327 |
250 |
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series. |
Amgen |
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 |
24900358 |
69 |
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors. |
TBA |
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 |
21429632 |
43 |
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
University of The Pacific |
21353571 |
26 |
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells. |
Hanyang University |
21128646 |
88 |
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure. |
Merck Research Laboratories |
21123062 |
48 |
Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors. |
Cephalon |
18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
20570525 |
56 |
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase. |
Chinese Academy of Sciences |
20570511 |
22 |
Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors. |
Korea Research Institute of Chemical Technology |
20420387 |
118 |
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. |
Glaxosmithkline |
20153646 |
28 |
Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells. |
Institute of Science and Technology |
20138514 |
93 |
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta. |
Vertex Pharmaceuticals |
20153204 |
109 |
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. |
Nerviano Medical Sciences |
19716697 |
110 |
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II. |
Boehringer Ingelheim Pharmaceuticals |
19854051 |
56 |
N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors. |
Methylgene |
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 |
18324759 |
133 |
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors. |
Amgen |
18311900 |
89 |
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis. |
Amgen |
18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
18278858 |
93 |
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity. |
Amgen |
15177483 |
33 |
SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity. |
Novartis Institutes For Biomedical Research |
22377675 |
44 |
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors. |
Westf£Lische Wilhelms-Universit£T M£Nster |
22221201 |
32 |
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
University of Kentucky |
16476733 |
18 |
Inhibition of S/G2 phase CDK4 reduces mitotic fidelity. |
University of Queensland |
22381355 |
16 |
Design, synthesis and molecular docking studies of some novel spiro[indoline-3, 4'-piperidine]-2-ones as potential c-Met inhibitors. |
Southern Medical University |
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 |
22225917 |
44 |
Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802). |
Chugai Pharmaceutical |
21967808 |
52 |
Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group. |
Cephalon |
22154349 |
123 |
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors. |
Nerviano Medical Sciences |
22119469 |
107 |
Novel and selective spiroindoline-based inhibitors of Sky kinase. |
Pfizer |
22138308 |
18 |
Identification of new aminoacid amides containing the imidazo[2,1-b]benzothiazol-2-ylphenyl moiety as inhibitors of tumorigenesis by oncogenic Met signaling. |
University of The Mediterranean |
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 |
22003817 |
71 |
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. |
Takeda Pharmaceutical |
22001029 |
28 |
Design and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors. |
Korea Research Institute of Chemical Technology |
21982797 |
128 |
9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp. |
Peking University |
22014755 |
36 |
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
Hanyang University |
21794960 |
194 |
Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
Universit£ |
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 |
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 |
21641696 |
450 |
Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met. |
Sichuan University |
21741249 |
32 |
Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp. |
Heinrich Heine Universit£T |
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 |
21708465 |
141 |
Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition. |
St. Jude Children'S Research Hospital |
21705217 |
60 |
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors. |
Bristol-Myers Squibb |
20674350 |
63 |
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
21524503 |
73 |
Dual IGF-1R/SRC inhibitors based on a N'-aroyl-2-(1H-indol-3-yl)-2-oxoacetohydrazide structure. |
Technische Universit£T Braunschweig |
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 |
21561768 |
12 |
Identification and synthesis of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase. |
Chinese Academy of Sciences |
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 |
21414779 |
64 |
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors. |
Amgen |
24900250 |
81 |
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277 |
TBA |
21190849 |
53 |
2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines. |
Cephalon |
21038853 |
133 |
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6. |
Novartis Institutes For Biomedical Research |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
20855207 |
26 |
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. |
Merck Research Laboratories |
20817473 |
57 |
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. |
Nerviano Medical Sciences Oncology |
20684549 |
76 |
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor. |
Amgen |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
20483608 |
139 |
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck. |
Novartis Institute of Biomedical Research |
20397705 |
208 |
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. |
Nerviano Medical Sciences |
20382527 |
26 |
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors. |
Bristol-Myers Squibb Research and Development |
20363625 |
69 |
Identification of a novel series of potent RON receptor tyrosine kinase inhibitors. |
Methylgene |
19894727 |
164 |
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent. |
Wyeth Research |
20188552 |
75 |
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). |
Wyeth Research |
19854649 |
49 |
Discovery of highly potent and selective type I B-Raf kinase inhibitors. |
Wyeth Research |
20148563 |
42 |
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring. |
The Institute of Cancer Research |
20141146 |
234 |
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. |
Nerviano Medical Sciences |
20093027 |
92 |
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
Chugai Pharmaceutical |
20071170 |
36 |
Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups. |
Methylgene |
19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
19896842 |
54 |
N3-arylmalonamides: a new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases. |
Methylgene |
19819693 |
50 |
Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. |
Amgen |
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 |
19839593 |
4 |
Tea catechins inhibit hepatocyte growth factor receptor (MET kinase) activity in human colon cancer cells: kinetic and molecular docking studies. |
Oregon State University |
19791746 |
14 |
Kinase inhibitor data modeling and de novo inhibitor design with fragment approaches. |
Eli Lilly |
19775160 |
79 |
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability. |
Takeda Pharmaceutical |
19369077 |
70 |
Discovery of 4-azaindoles as novel inhibitors of c-Met kinase. |
Ucb Pharma |
19362847 |
51 |
Design and synthesis of a novel tyrosine kinase inhibitor template. |
St. Jude Children'S Research Hospital |
19199650 |
5 |
Directed discovery of agents targeting the Met tyrosine kinase domain by virtual screening. |
National Cancer Institute-Frederick |
19414255 |
58 |
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase. |
Vertex Pharmaceuticals |
19269177 |
21 |
Syntheses of novel 2,3-diaryl-substituted 5-cyano-4-azaindoles exhibiting c-Met inhibition activity. |
Technical University of Darmstadt |
19211249 |
95 |
N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors. |
Methylgene |
19059779 |
32 |
Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase. |
Ucb Pharma |
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 |
18682324 |
33 |
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors. |
Amgen |
18610999 |
24 |
Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening. |
Institute of Materia Medica |
18606543 |
68 |
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta. |
Wyeth Research |
18529047 |
156 |
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors. |
Eberhard-Karls University |
18479916 |
24 |
Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors. |
Bristol-Myers Squibb Research and Development |
18313174 |
26 |
Synthesis and biological evaluation of diversely substituted indolin-2-ones. |
Université |
17964000 |
16 |
Structure activity relationships of quinoline-containing c-Met inhibitors. |
Pfizer |
17185414 |
30 |
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
Genomics Institute of The Novartis Research Foundation |
18289854 |
44 |
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase. |
Bristol-Myers Squibb Research and Development |
18248988 |
16 |
Entry into a new class of protein kinase inhibitors by pseudo ring design. |
Novartis Institutes For Biomedical Research |
18055203 |
51 |
Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA. |
Bristol-Myers Squibb Research and Development |
17826092 |
37 |
Optimization of triarylimidazoles for Tie2: influence of conformation on potency. |
Glaxosmithkline |
17606372 |
66 |
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17499505 |
78 |
Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors. |
Boehringer Ingelheim Pharmaceuticals |
17350837 |
59 |
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors. |
Amgen |
17270437 |
68 |
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17239587 |
43 |
1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors. |
Cephalon |
16765046 |
63 |
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies. |
Chiron |
16750628 |
47 |
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors. |
Abbott Laboratories |
16249085 |
26 |
Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity. |
Novartis Institutes For Biomedical Research |
16134929 |
22 |
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. |
Bristol-Myers Squibb |
16111887 |
104 |
New dual inhibitors of EGFR and HER2 protein tyrosine kinases. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
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 |
15177482 |
90 |
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis. |
Novartis Institutes For Biomedical Research |
15012985 |
31 |
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors. |
Kirin Brewery |
12941313 |
20 |
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. |
Novartis Pharma |
12672234 |
64 |
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. |
Boehringer Ingelheim Pharmaceuticals |
12039590 |
51 |
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck. |
Abbott Bioresearch Center |
32173195 |
5 |
Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment. |
Jiangxi Science & Technology Normal University |
32371098 |
15 |
Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors. |
Sungkyunkwan University |
31714773 |
2 |
Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies. |
Astrazeneca |
32292564 |
138 |
Efficacy and Tolerability of Pyrazolo[1,5- |
The Genomics Institute of The Novartis Research Foundation |
31836443 |
11 |
Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 4-oxoquinoline moiety as potential antitumor inhibitor. |
Shanghai Institute of Technology |
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 |
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 |
30826508 |
47 |
Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors. |
Mansoura University |
27524312 |
27 |
Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold. |
Fudan University |
27379978 |
140 |
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors. |
Chinese Academy of Sciences |
27355974 |
198 |
Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844). |
Sanofi-Aventis Germany |
30755337 |
95 |
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952. |
Japan Tobacco |
31629631 |
4 |
Design, synthesis, and biological evaluation of 4-phenoxyquinoline derivatives as potent c-Met kinase inhibitor. |
Shenyang Pharmaceutical University |
31492532 |
48 |
An exploration of solvent-front region high affinity moiety leading to novel potent ALK & ROS1 dual inhibitors with mutant-combating effects. |
Shenyang Pharmaceutical University |
31300317 |
14 |
1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview. |
Chinese Academy of Sciences |
29522671 |
80 |
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
Chinese Academy of Sciences |
31693351 |
473 |
Discovery of 4 |
TBA |
31419130 |
69 |
Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK). |
Zhejiang University |
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 |
31531204 |
14 |
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors. |
Astrazeneca |
31229873 |
32 |
2,7-naphthyridinone-based MET kinase inhibitors: A promising novel scaffold for antitumor drug development. |
Central China Normal University |
30927566 |
52 |
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
Shenyang Pharmaceutical University |
32184955 |
49 |
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage. |
Bristol-Myers Squibb Research & Development |
31546197 |
1 |
1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
Guizhou University of Traditional Chinese Medicine |
31079967 |
43 |
Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors. |
School of Marine Science and Technology |
31078412 |
33 |
Structure based designing of triazolopyrimidone-based reversible inhibitors for kinases involved in NSCLC. |
Punjabi 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 |
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 |
31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
31520926 |
28 |
Discovery of a potent p38?/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies. |
University of Sharjah |
31335138 |
56 |
Discovery and Development of a Series of Pyrazolo[3,4- |
Shanghai University |
26810712 |
25 |
Design, synthesis, and docking studies of phenylpicolinamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors. |
Jiangxi Science & Technology Normal 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 |
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 |
19271717 |
96 |
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium. |
Heinrich-Heine-Universitat |
18494522 |
244 |
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense. |
Heinrich-Heine-Universit£T |
30248654 |
71 |
Exploration of novel pyrrolo[2,1-f][1,2,4]triazine derivatives with improved anticancer efficacy as dual inhibitors of c-Met/VEGFR-2. |
China Pharmaceutical University |
30216852 |
16 |
Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 1,8-naphthyridin-2-one moiety. |
Jiangxi Science & Technology Normal 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 |
29331754 |
9 |
Synthesis and bioevaluation and doking study of 1H-pyrrolo[2,3-b]pyridine derivatives bearing aromatic hydrazone moiety as c-Met inhibitors. |
Jiangxi Science & Technology Normal University |
29197731 |
14 |
Synthesis and antiproliferative activity of pyrrolo[2,3-b]pyridine derivatives bearing the 1,8-naphthyridin-2-one moiety. |
Jiangxi Science & Technology Normal University |
30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
29602036 |
25 |
Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
China Pharmaceutical University |
29549836 |
47 |
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. |
Universit£ |
29545102 |
159 |
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor. |
Merck |
28987604 |
3 |
Discovery and synthesis of novel Wogonin derivatives with potent antitumor activity in vitro. |
China Pharmaceutical University |
28938137 |
30 |
Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors. |
Shanghai Institute of Pharmaceutical Industry |
28835797 |
36 |
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives. |
Chinese Academy of Sciences |
29466002 |
193 |
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening. |
University of Edinburgh |
29203143 |
8 |
Synthesis and bioevaluation study of novel N-methylpicolinamide and thienopyrimidine derivatives as selectivity c-Met kinase inhibitors. |
Jiangxi Science & Technology Normal University |
29146452 |
12 |
Design, synthesis, and biological evaluation of thieno[2,3-d]pyrimidine derivatives as novel dual c-Met and VEGFR-2 kinase inhibitors. |
China Pharmaceutical University |
28927801 |
16 |
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold. |
Jiangxi Science & Technology Normal University |
29407963 |
47 |
Identification of novel N |
Zhuhai Campus of Zunyi Medical University |
29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
29202410 |
11 |
Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
China Pharmaceutical University |
29032031 |
91 |
Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors. |
Xi'An Jiaotong University |
29107421 |
9 |
Discovery of novel pyrrolo-pyridine/pyrimidine derivatives bearing pyridazinone moiety as c-Met kinase inhibitors. |
Jiangxi Science & Technology Normal University |
29174809 |
52 |
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
Shenyang Pharmaceutical University |
29102175 |
91 |
Discovery of novel anti-angiogenesis agents. Part 7: Multitarget inhibitors of VEGFR-2, TIE-2 and EphB4. |
Xi'An Jiaotong 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 |
28716639 |
24 |
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors. |
Shenyang Pharmaceutical University |
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 |
28787156 |
5 |
Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. |
Universit£ |
28384549 |
38 |
Discovery of novel 7-azaindole derivatives bearing dihydropyridazine moiety as c-Met kinase inhibitors. |
Jiangxi Science and Technology Normal University |
28412159 |
46 |
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors. |
Hangzhou Xixi Hospital |
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 |
34426525 |
6 |
DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 M |
Baylor College of Medicine |
28376302 |
12 |
Multimodal Recognition of Diverse Peptides by the C-Terminal SH2 Domain of Phospholipase C-¿1 Protein. |
University of Colorado Boulder |
| 15 |
Discovery of 3,3-di(indolyl)indolin-2-one as a novel scaffold for a-glucosidase inhibitors: In silico studies and SAR predictions |
Jishou University |
28043720 |
9 |
Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
China Pharmaceutical University |
27914694 |
32 |
Synthesis of novel chromenones linked to 1,2,3-triazole ring system: Investigation of biological activities against Alzheimer's disease. |
Tehran University of Medical Sciences |
24194515 |
1 |
Insights into distinct modulation of a7 and a7ß2 nicotinic acetylcholine receptors by the volatile anesthetic isoflurane. |
University of Pittsburgh |
23897821 |
60 |
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability. |
Genentech |
27496071 |
4 |
Design and synthesis of new 2-anilinoquinolines bearing N-methylpicolinamide moiety as potential antiproliferative agents. |
Korea Institute of Science and Technology |
27231830 |
27 |
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies. |
Aimst University |
15131245 |
86 |
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization. |
Sanofi-Synthelabo Recherche |
7805764 |
11 |
The pharmacological profile of cloned and stably expressed alpha 1b-adrenoceptor in CHO cells. |
National Children'S Medical Research Center |
7109844 |
11 |
The binding of [3H]nitrendipine to receptors for calcium channel antagonists in the heart, cerebral cortex, and ileum of rats. |
University of Arizona |
1353247 |
71 |
Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. |
University of Nebraska |
16492149 |
16 |
Structure-based optimization of MurF inhibitors. |
Abbott Laboratories |
1320692 |
19 |
Comparison of antagonist and agonist binding to the leukotriene B4 receptor intact human polymorphonuclear neutrophils (PMN). |
Ciba-Geigy |
20416509 |
14 |
Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation. |
Weill Medical College of Cornell University |
20338520 |
24 |
A structure-guided approach to creating covalent FGFR inhibitors. |
Harvard Medical School |
20189109 |
42 |
Affinity reagents that target a specific inactive form of protein kinases. |
University of Washington |
20189103 |
36 |
Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs. |
University of California San Francisco |
19270684 |
3 |
Transition state analogs of 5'-methylthioadenosine nucleosidase disrupt quorum sensing. |
Albert Einstein College of Medicine |