The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28291695 |
36 |
Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy. |
Takeda California |
| 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 |
| 27491023 |
286 |
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. |
University of Auckland |
| 27132165 |
29 |
Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor. |
Southern Medical University |
| 27131066 |
36 |
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
Chinese Academy of Sciences |
| 27387355 |
32 |
6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR. |
Zhejiang 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 |
| 27288180 |
83 |
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives. |
Harvard Medical School |
| 27190603 |
73 |
Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation. |
Astrazeneca |
| 27010810 |
24 |
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
Oribase Pharma |
| 27234887 |
84 |
Discovery of new [1,4]dioxino[2,3-f]quinazoline-based inhibitors of EGFR including the T790M/L858R mutant. |
Beijing University of Technology |
| 27131639 |
26 |
Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
Fudan University |
| 27106709 |
92 |
Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening. |
Korea Research Institute of Chemical Technology |
| 26968253 |
24 |
Recent progress on third generation covalent EGFR inhibitors. |
Pfizer |
| 26756222 |
70 |
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
Pfizer |
| 26819674 |
66 |
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR. |
Genentech |
| 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 |
| 26879314 |
26 |
Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors. |
Beijing University of Technology |
| 26829280 |
26 |
Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines. |
Dalian Medical University |
| 26639762 |
55 |
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase. |
Genentech |
| 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 |
| 26396685 |
19 |
Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. |
Amgen |
| 26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan University |
| 26313252 |
22 |
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
Astrazeneca |
| 25975640 |
60 |
Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR. |
Technische Universit£T Dortmund |
| 25827399 |
52 |
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis. |
Chinese Academy of Sciences |
| 25409491 |
83 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
Zhejiang University |
| 25383627 |
85 |
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation. |
Genentech |
| 25271963 |
93 |
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. |
Astrazeneca |
| 24915291 |
73 |
Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. |
Peking University |
| 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 |
| 23490150 |
48 |
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors. |
Takeda Pharmaceutical |
| 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 |
| 23103095 |
125 |
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors. |
Abbott Laboratories |
| 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 |
| 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 |
| 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 |
| 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 |
| 19821562 |
34 |
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases. |
Bristol-Myers Squibb Research and Development |
| 19397322 |
58 |
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
National Cancer Institute-Bethesda |
| 18789685 |
172 |
Kinase array design, back to front: biaryl amides. |
Glaxosmithkline |
| 18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
| 18077363 |
314 |
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
University of Oxford |
| 17935989 |
146 |
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. |
Abbott Laboratories |
| 16279804 |
40 |
Anilinodialkoxyquinazolines: screening epidermal growth factor receptor tyrosine kinase inhibitors for potential tumor imaging probes. |
Lawrence Berkeley National Laboratory |
| 16480284 |
126 |
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors. |
Pfizer |
| 16249345 |
25 |
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. |
Glaxosmithkline |
| 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 |
| 21958547 |
108 |
Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. |
Pfizer |
| 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 |
| 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 |
| 21733693 |
7 |
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. |
Glaxosmithkline |
| 21391610 |
139 |
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors. |
Vertex Pharmaceuticals |
| 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 |
| 19926477 |
100 |
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization. |
Abbott Laboratories |
| 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 |
| 19101143 |
70 |
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). |
Glaxosmithkline |
| 18818075 |
25 |
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors. |
Glaxosmithkline |
| 18667312 |
24 |
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. |
The Scripps Research Institute |
| 32631510 |
44 |
Potent dual EGFR/Her4 tyrosine kinase inhibitors containing novel (1,2-dithiolan-4-yl)acetamides. |
Sabila Biosciences |
| 11378364 |
34 |
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. |
Research Biomet. Glaxo Wellcome Medicines Research Centre |
| 30893553 |
62 |
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). |
Bristol-Myers Squibb Research and 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 |
| 27531604 |
55 |
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177). |
Bristol-Myers Squibb Research and Development |
| 31381333 |
302 |
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
TBA |
| 30562697 |
84 |
The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
University of Silesia In Katowice |
| 31493743 |
32 |
Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors. |
Anadolu University |
| 29522671 |
80 |
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
Chinese Academy of Sciences |
| 28528303 |
171 |
Discovery of a potent dual ALK and EGFR T790M inhibitor. |
Harvard Medical School |
| 31693351 |
473 |
Discovery of 4 |
TBA |
| 32083858 |
145 |
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. |
TBA |
| 30565923 |
34 |
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology. |
Eberhard Karls University T£Bingen |
| 30875504 |
34 |
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis. |
Sichuan University and Collaborative Innovation Center |
| 30878832 |
57 |
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
Arromax Pharmatech |
| 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 |
| 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 |
| 31335138 |
56 |
Discovery and Development of a Series of Pyrazolo[3,4- |
Shanghai University |
| 28139931 |
85 |
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. |
Pfizer |
| 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 |
| 26706113 |
10 |
Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents. |
Xi'An Jiaotong 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 |
| 26451770 |
52 |
Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
| 26455919 |
87 |
Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study. |
Argenta Discovery |
| 24124898 |
26 |
Design, synthesis, and biological evaluation of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible epidermal growth factor receptor inhibitors with improved pharmacokinetic properties. |
Chinese Academy of Sciences |
| 24053674 |
80 |
Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant. |
East China University of Science & Technology |
| 23930994 |
67 |
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). |
Astrazeneca |
| 23668441 |
39 |
Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer. |
China Pharmaceutical University |
| 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 |
| 30423248 |
226 |
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. |
Pfizer |
| 30097367 |
96 |
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series. |
Bristol-Myers Squibb |
| 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 |
| 28844493 |
14 |
Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting. |
Eberhard-Karls-University Tuebingen |
| 29730188 |
10 |
Discovery of new erbB4 inhibitors: Repositioning an orphan chemical library by inverse virtual screening. |
University of Salerno |
| 29631132 |
33 |
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. |
Shaanxi University of Science & Technology |
| 28734581 |
37 |
Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC. |
Sichuan University and Collaborative Innovation Center |
| 28720503 |
146 |
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis. |
Merck |
| 28282122 |
9 |
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
High Magnetic Field Laboratory |
| 28438385 |
24 |
Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth. |
Indiana University School of Medicine |
| 29457982 |
80 |
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. |
Genentech |
| 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 |
| 24634223 |
8 |
Trimethylation of histone H3 lysine 36 by human methyltransferase PRDM9 protein. |
University of Toronto |
| 19836247 |
49 |
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles. |
Wyeth Research |
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