The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28541695 |
192 |
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRa) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
East China University of Science and Technology |
28291695 |
36 |
Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy. |
Takeda California |
27789138 |
355 |
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors. |
Abbvie Bioresearch Center |
27750146 |
58 |
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
Chinese Academy of Sciences |
27814560 |
17 |
Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor. |
Korea Institute of Science & Technology (Kist) |
28280261 |
84 |
Non-kinase targets of protein kinase inhibitors. |
The University of Sydney |
27839918 |
28 |
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). |
Takeda California |
27815117 |
16 |
Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors. |
Ocean University of China |
27739691 |
7 |
Fragment-to-Lead Medicinal Chemistry Publications in 2015. |
Astex Pharmaceuticals |
27299736 |
37 |
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules. |
St. John'S University |
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 |
27115835 |
85 |
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. |
University of Edinburgh |
27288183 |
130 |
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. |
Southeast University |
27011159 |
97 |
Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
Experimental Therapeutics Centre |
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 |
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 |
27086121 |
120 |
Anilinoquinazoline inhibitors of the RET kinase domain-Elaboration of the 7-position. |
University of Manchester |
26951750 |
59 |
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
26874741 |
156 |
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. |
University of Manchester |
26717201 |
68 |
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs. |
Shenyang Pharmaceutical University |
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 |
26652860 |
68 |
A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants. |
Korea Institute of Science & Technology (Kist) |
26384287 |
65 |
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors. |
Kangwon National University |
26342867 |
52 |
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors. |
Sichuan 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 |
26005534 |
158 |
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors. |
Genomics Institute of The Novartis Research Foundation |
25625428 |
10 |
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. |
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif) |
25763473 |
108 |
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents. |
Entremed |
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 |
25589926 |
20 |
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase. |
Astex Pharmaceuticals |
25589919 |
2 |
RET Kinase Inhibitors May Treat Cancer and Gastrointestinal Disorders. |
Therachem Research Medilab (India) |
25232968 |
22 |
Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation. |
The University of Arizona |
24139169 |
175 |
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. |
Nerviano Medical Sciences |
24904961 |
27 |
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
Qilu Pharmaceutical |
24900886 |
66 |
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors. |
Chinese Academy of Sciences |
24779514 |
128 |
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. |
Gilead Sciences |
24726806 |
108 |
Syk inhibitors with high potency in presence of blood. |
Novartis Institutes For Biomedical Research |
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 |
24447248 |
18 |
Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies. |
Universit£ |
24359159 |
60 |
Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. |
Astrazeneca |
24183742 |
40 |
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. |
Chinese Academy of Sciences |
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 |
23999040 |
27 |
Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
Nanjing University of Technology |
23768909 |
50 |
Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2. |
Novartis Institutes For Biomedical Research |
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 |
23570792 |
61 |
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors. |
Emd-Serono Research Institute |
23474386 |
26 |
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors. |
Chinese Academy of Sciences |
23498918 |
41 |
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor. |
Takeda Pharmaceutical |
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 |
22521646 |
38 |
Novel triazolopyridylbenzamides as potent and selective p38a inhibitors. |
RhôNe-Poulenc Rorer |
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 |
23098265 |
46 |
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. |
University of Genoa |
22827572 |
67 |
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). |
Glaxosmithkline |
22257213 |
98 |
Discovery and development of spleen tyrosine kinase (SYK) inhibitors. |
Rigel |
22863529 |
31 |
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors. |
Chinese Academy of Sciences |
22559926 |
6 |
Preparation of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET kinase inhibitors. |
University of Gothenburg |
22394077 |
19 |
Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. |
Hoffmann-La Roche |
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 |
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 |
22465635 |
95 |
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. |
Abbott Laboratories |
22148921 |
48 |
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c |
Cephalon |
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 |
18469809 |
41 |
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. |
Nerviano Medical Sciences Oncology |
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 |
20117004 |
68 |
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. |
University of Milano-Bicocca |
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 |
19320489 |
125 |
Discovery and development of aurora kinase inhibitors as anticancer agents. |
Vertex Pharmaceuticals |
18077425 |
197 |
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
Harvard Medical School |
17113292 |
73 |
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. |
Targegen |
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 |
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 |
22056746 |
53 |
Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. |
Boehringer Ingelheim Pharmaceuticals |
22014550 |
337 |
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). |
Ansaris |
22018461 |
41 |
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066). |
Bristol-Myers Squibb Research and Development |
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 |
21724393 |
74 |
Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors. |
National Tsing Hua University |
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 |
21493067 |
22 |
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. |
Astrazeneca R&D Boston |
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 |
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 |
21341678 |
49 |
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. |
Millennium Pharmaceuticals |
21316232 |
41 |
4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II. |
Johnson & Johnson Pharmaceutical Research & Development |
24900250 |
81 |
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277 |
TBA |
20961062 |
42 |
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity. |
Pfizer |
20925433 |
21 |
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
Aristotle University of Thessaloniki |
20873740 |
111 |
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. |
Nerviano Medical Sciences |
20817473 |
57 |
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. |
Nerviano Medical Sciences Oncology |
19654408 |
2521 |
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
Ambit Biosciences |
20409618 |
31 |
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold. |
Technische Universit£T Braunschweig |
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 |
19646870 |
34 |
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors. |
Ambit Biosciences |
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 |
20143778 |
70 |
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. |
Curis |
20141146 |
234 |
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. |
Nerviano Medical Sciences |
19754199 |
29 |
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
Ambit Biosciences |
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 |
19053769 |
8 |
Synthesis, modeling, and RET protein kinase inhibitory activity of 3- and 4-substituted beta-carbolin-1-ones. |
Universita Di Milano |
18313174 |
26 |
Synthesis and biological evaluation of diversely substituted indolin-2-ones. |
Université |
17185414 |
30 |
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. |
Genomics Institute of The Novartis Research Foundation |
17532631 |
105 |
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents. |
Johnson & Johnson Pharmaceutical Research & Development |
17499504 |
5 |
Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones. |
Università |
17343372 |
143 |
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor. |
Abbott Laboratories |
16610779 |
10 |
Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. |
Università |
32832025 |
20 |
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors. |
Jinan University |
32292564 |
138 |
Efficacy and Tolerability of Pyrazolo[1,5- |
The Genomics Institute of The Novartis Research Foundation |
31757666 |
314 |
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors. |
Merck |
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 |
30973735 |
91 |
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. |
University of North Carolina At Chapel Hill |
31693351 |
473 |
Discovery of 4 |
TBA |
31250638 |
34 |
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)- |
Chinese Academy of Sciences |
32298114 |
14 |
Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology. |
Universit£ |
30927566 |
52 |
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
Shenyang Pharmaceutical University |
32292556 |
41 |
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET |
University of Manchester |
30987781 |
88 |
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. |
Southeast University |
30529543 |
57 |
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance. |
China Pharmaceutical University |
30384048 |
365 |
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. |
University of Florida |
31526603 |
379 |
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application. |
Takeda Pharmaceutical |
31614258 |
178 |
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
Vichem Chemie Research |
31335138 |
56 |
Discovery and Development of a Series of Pyrazolo[3,4- |
Shanghai University |
26568411 |
68 |
Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration. |
Novartis Institutes For Biomedical Research |
26568289 |
32 |
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
Dana-Farber Cancer Institute |
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 |
26843921 |
39 |
Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies. |
The University of Arizona |
30978288 |
113 |
A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. |
Northwestern University |
30170943 |
35 |
Design and synthesis of potent RSK inhibitors. |
Novartis Institutes For Biomedical Research |
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 |
30082069 |
359 |
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors. |
Vertex Pharmaceuticals |
29945794 |
193 |
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups. |
Vertex Pharmaceuticals |
29549836 |
47 |
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors. |
Universit£ |
29459144 |
4 |
Discovery of novel 4-aryl-thieno[1,4]diazepin-2-one derivatives targeting multiple protein kinases as anticancer agents. |
Hanyang University |
30034590 |
45 |
Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS. |
Glaxosmithkline |
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 |
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 |
29466002 |
193 |
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening. |
University of Edinburgh |
29407963 |
47 |
Identification of novel N |
Zhuhai Campus of Zunyi Medical University |
29107425 |
90 |
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders. |
Korea Institute of Science & Technology (Kist) |
29152045 |
74 |
Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis. |
Shenyang Pharmaceutical 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 |
29400470 |
41 |
The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration. |
Novartis Institutes For Biomedical Research |
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 |
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 |
28956923 |
34 |
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML. |
Chinese Academy of Sciences |
28404375 |
6 |
Synthesis and structure-activity relationship study of pyrazolo[3,4-d]pyrimidines as tyrosine kinase RET inhibitors. |
University of Science and Technology of China |
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 |
21985426 |
27 |
Chromone containing sulfonamides as potent carbonic anhydrase inhibitors. |
Ondokuz Mayis University |
28253432 |
3 |
Spectroscopic and Computational Investigations of Ligand Binding to IspH: Discovery of Non-diphosphate Inhibitors. |
University of Illinois |
28043720 |
9 |
Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
China Pharmaceutical University |
15356217 |
38 |
Heterologous expression of human {alpha}6{beta}4{beta}3{alpha}5 nicotinic acetylcholine receptors: binding properties consistent with their natural expression require quaternary subunit assembly including the {alpha}5 subunit. |
Targacept |
15356216 |
48 |
Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential. |
University of Piemonte Orientale |
12616631 |
18 |
D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. |
University of Queensland Brisbane |
7518514 |
46 |
(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization. |
Abbott Laboratories |
1656026 |
160 |
Characterization of the alpha-2C adrenergic receptor subtype in the opossum kidney and in the OK cell line. |
University of Nebraska |
1353247 |
71 |
Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. |
University of Nebraska |
1321043 |
17 |
Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist. |
UniversitÉ |
18556202 |
37 |
Discovery of a novel series of Notch-sparing gamma-secretase inhibitors. |
Wyeth Research |
19217284 |
67 |
1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position. |
Gsk |
19217781 |
21 |
The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore. |
Gsk |
18998662 |
15 |
Design, Structure-Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors. |
Bristol-Myers Squibb |
19007202 |
12 |
Development of Novel G-Protein-Coupled Receptor 54 Agonists with Resistance to Degradation by Matrix Metalloproteinase. |
Kyoto University |
16821772 |
270 |
Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase. |
Curacyte Chemistry |
18324760 |
34 |
Development of Potent and Selective Phosphinic Peptide Inhibitors of Angiotensin-Converting Enzyme 2. |
University of Athens |
18072718 |
37 |
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors. |
Novartis Pharmaceuticals |
12731874 |
10 |
Thermodynamic characterization of the binding of nucleotides to glycyl-tRNA synthetase. |
Medical College of Ohio |
15837314 |
53 |
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase. |
Gsk |