295 articles for thisTarget
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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
Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy.
Takeda California
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.
Chinese Academy of Sciences
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)
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).
Takeda California
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
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
St. John'S University
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
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.
Chinese Academy of Sciences
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
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.
Southeast University
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
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
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).
Green Valley Research Institute
Anilinoquinazoline inhibitors of the RET kinase domain-Elaboration of the 7-position.
University of Manchester
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
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.
University of Manchester
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.
Shenyang Pharmaceutical University
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
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)
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.
Kangwon National University
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.
Sichuan University
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
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Genomics Institute of The Novartis Research Foundation
Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.
Entremed
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors.
Central China Normal University
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.
Astex Pharmaceuticals
RET Kinase Inhibitors May Treat Cancer and Gastrointestinal Disorders.
Therachem Research Medilab (India)
Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation.
The University of Arizona
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.
Qilu Pharmaceutical
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.
Chinese Academy of Sciences
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Gilead Sciences
Syk inhibitors with high potency in presence of blood.
Novartis Institutes For Biomedical Research
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
Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies.
University of Pisa
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
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Nerviano Medical Sciences
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors.
Nanjing University of Technology
Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.
Novartis Institutes For Biomedical Research
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
SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors.
Emd-Serono Research Institute
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.
Chinese Academy of Sciences
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
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Novel triazolopyridylbenzamides as potent and selective p38a inhibitors.
RhôNe-Poulenc Rorer
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
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
University of Genoa
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
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.
Chinese Academy of Sciences
Preparation of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET kinase inhibitors.
University of Gothenburg
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
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
Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.
TBA
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Amgen
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
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Abbott Laboratories
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
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
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.
Nerviano Medical Sciences Oncology
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
Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.
University of Milano-Bicocca
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
National Cancer Institute-Bethesda
Discovery and development of aurora kinase inhibitors as anticancer agents.
Vertex Pharmaceuticals
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
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
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
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
Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.
Boehringer Ingelheim Pharmaceuticals
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
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
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
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
Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors.
National Tsing Hua University
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Ariad Pharmaceuticals
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
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.
Astrazeneca R&D Boston
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
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
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Millennium Pharmaceuticals
4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II.
Johnson & Johnson Pharmaceutical Research & Development
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
Pfizer
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University of Thessaloniki
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
Nerviano Medical Sciences Oncology
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.
Technische Universit£T Braunschweig
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Novartis Institute of Biomedical Research
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
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.
Ambit Biosciences
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.
The Institute of Cancer Research
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
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
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
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
Synthesis, modeling, and RET protein kinase inhibitory activity of 3- and 4-substituted beta-carbolin-1-ones.
Universita Di Milano
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Genomics Institute of The Novartis Research Foundation
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.
Center for Lymphoid Malignancies
Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma.
Knight Cancer Institute
In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494).
AbbVie Bioresearch Center
Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase.
Nerviano Medical Sciences
CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients.
Mayo Clinic
Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1.
Pfizer
The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.
ARIAD Pharmaceuticals, Inc.
NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies.
Nerviano Medical Sciences Srl
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.
Eli Lilly and Company
Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor.
OSI Pharmaceuticals, Inc.
BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.
Boehringer Ingelheim Austria GmbH
Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model.
University of California Irvine (UCI)
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Johann Wolfgang Goethe University
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
AbbVie
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.
Dana-Farber Cancer Institute
Discovery of Sovleplenib, a Selective Inhibitor of Syk in Clinical Development for Autoimmune Diseases and Cancers.
HUTCHMED Limited
Design and synthesis of certain 7-Aryl-2-Methyl-3-Substituted Pyrazolo{1,5-a}Pyrimidines as multikinase inhibitors.
Sana'a University
Azaindole derivatives as potential kinase inhibitors and their SARs elucidation.
Hunan University of Science and Technology
Quinazoline-based VEGFR-2 inhibitors as potential anti-angiogenic agents: A contemporary perspective of SAR and molecular docking studies.
Tehran University of Medical Sciences
Research progress of VEGFR small molecule inhibitors in ocular neovascular diseases.
Southwest Jiaotong University
Side Chain Investigation of Imidazopyridazine as a Hinge Binder for Targeting Actionable Mutations of RET Kinase.
Gachon University
Targeting Solvent-Front Mutations for Kinase Drug Discovery: From Structural Basis to Design Strategies.
Jinan University
Discovery of the first selective, small-molecule GFRα2/3 inhibitors through DNA-encoded library technology.
Cerevel Therapeutics
Non-kinase off-target inhibitory activities of clinically-relevant kinase inhibitors.
Purdue University
Discovery of 9H-pyrimido[4,5-b]indole derivatives as dual RET/TRKA inhibitors.
University of Arkansas for Medical Sciences
Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations.
Nanjing University of Chinese Medicine
Unlocking the synthetic approaches and clinical application of approved small-molecule drugs for gastrointestinal cancer treatment: A comprehensive exploration.
KU Leuven
Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.
Jinan University
Discovery of Novel Fedratinib-Based HDAC/JAK/BRD4 Triple Inhibitors with Remarkable Antitumor Activity against Triple Negative Breast Cancer.
Shandong University
Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones.
Università
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
Jinan University
Medicinal chemistry approaches to target the MNK-eIF4E axis in cancer.
Northwestern University
Discovery of 3,5-diaryl-1H-pyrazol-based ureas as potent RET inhibitors.
Jinan University
Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases.
China Pharmaceutical University
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
Identification of (S)-1-(2-(2,4-difluorophenyl)-4-oxothiazolidin-3-yl)-3-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)urea as a potential anti-colorectal cancer agent.
Zunyi Medical University
Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective.
University of Modena and Reggio Emilia
A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.
Novartis Institutes For Biomedical Research
1-Methyl-3-((4-(quinolin-4-yloxy)phenyl)amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions.
Jinan University
Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders.
China Pharmaceutical University
4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.
Yangtze University
Dual-target kinase drug design: Current strategies and future directions in cancer therapy.
Sichuan University
Pyrazolopyrimidines as anticancer agents: A review on structural and target-based approaches.
Isf College of Pharmacy
Novel Sphingosine Kinase 1 Inhibitor Suppresses Growth of Solid Tumor and Inhibits the Lung Metastasis of Triple-Negative Breast Cancer.
China Pharmaceutical University
Design and development of photoswitchable DFG-Out RET kinase inhibitors.
University of Gothenburg
Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.
Wenzhou Medical University
Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.
Università
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.
University of Arkansas For Medical Sciences
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.
Zunyi Medical University
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
Hefei University of Technology
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.
Hangzhou Medical College
Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors.
Jinan University
Development and Therapeutic Potential of NUAKs Inhibitors.
University of Science and Technology (Ust)
Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.
University of Arkansas For Medical Sciences
Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.
Chinese Academy of Sciences
Discovery and optimization of selective RET inhibitors via scaffold hopping.
Guangzhou Baiyunshan Pharmaceutical Holdings
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-
The Genomics Institute of The Novartis Research Foundation
Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor.
University of Arkansas For Medical Sciences
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
Chinese Academy of Sciences
Structure-activity relationship study of novel quinazoline-based 1,6-naphthyridinones as MET inhibitors with potent antitumor efficacy.
Central China Normal University
Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of RET: Design, synthesis and biological evaluation.
University of Arkansas For Medical Sciences
Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.
Jinan University
A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
Central South University
Discovery of orally active indirubin-3'-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia.
Gwangju Institute of Science and Technology
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.
Sichuan University/Collaborative Innovation Center of Biotherapy
From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.
Sichuan University
Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp
Takeda Research In California
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.
Sichuan University and Collaborative Innovation Center
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.
Genomics Institute of The Novartis Research Foundation
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR
Sun Yat-Sen University
Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.
Xiamen University
A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia.
University of Regensburg
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors.
Jinan University
Efficacy and Tolerability of Pyrazolo[1,5-
The Genomics Institute of The Novartis Research Foundation
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
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
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
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
Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology.
University of Naples Federico II
Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties.
Shenyang Pharmaceutical University
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET
University of Manchester
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.
Southeast University
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.
China Pharmaceutical University
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
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.
Vichem Chemie Research
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
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.
Dana-Farber Cancer Institute
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
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
Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies.
The University of Arizona
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.
Northwestern University
Design and synthesis of potent RSK inhibitors.
Novartis Institutes For Biomedical Research
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
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.
University of Naples Federico II
Discovery of novel 4-aryl-thieno[1,4]diazepin-2-one derivatives targeting multiple protein kinases as anticancer agents.
Hanyang University
Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS.
Glaxosmithkline
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
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
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.
University of Edinburgh
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.
Korea Institute of Science & Technology (Kist)
Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.
Shenyang Pharmaceutical University
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
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
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
The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer.
Fudan University
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
Synthesis and structure-activity relationship study of pyrazolo[3,4-d]pyrimidines as tyrosine kinase RET inhibitors.
University of Science and Technology of China
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.
Hangzhou Xixi Hospital
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
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
2-OXO-DIHYDROQUINOLINE-3-CARBOXAMIDE DERIVATIVES AS GABA TYPE A RECEPTOR MODULATORS
University College Cardiff Consultants
In-flow photooxygenation of aminothienopyridinones generates novel PTP4A3 phosphatase inhibitors
University of Virginia Patent Foundation
IMIDAZOLE ORGANIC COMPOUNDS AND THEIR USE AGAINST INFLAMMATORY BOWEL DISEASE
Benevolentai Cambridge
METHODS AND COMPOSITIONS COMPRISING A BRAF INHIBITOR AND A PD-1 BINDING ANTAGONIST
Hoffmann-La Roche
2-aminoaryl-5-aryloxazole analogs for the treatment of neurodegenerative diseases
Southern Research Institute
Oxopyridine derivatives useful as aminocarboxymuconate semialdehyde decarboxylase (ACMSD) inhibitors
Orsobio
Histone deacetylase inhibitors for immunomodulation in tumor microenvironment
Great Novel Therapeutics Biotech & Medicals
Polypeptide compound, pharmaceutical composition, preparation method and application thereof
Chengdu Sintanovo Biotechnology
Therapeutic compounds and methods of use thereof
Agency For Science, Technology and Research (A*Star)
Pyrazolo[3,4-B]pyridines and imidazo[1,5-B]pyridazines as PDE1 inhibitors
H. Lundbeck
Indazole compound for use in inhibiting kinase activity, composition and application thereof
Shenzhen Targetrx
Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors
Incyte
Azetidine derivative, preparation method therefor, and use thereof
Sichuan Kelun-Biotech Biopharmaceutical
N4-hydroxycytidine and derivatives and anti-viral uses related thereto
Emory University
Pyrazolopyridine derivative having GLP-1 receptor agonist effect
Chugai Seiyaku Kabushiki Kaisha
Compositions and methods for treating KIT- and PDGFRA-mediated diseases
Blueprint Medicines
3-phenyl-pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
Arena Pharmaceuticals
Tyrosinase inhibitory activities of the compounds isolated from Neolitsea aciculata (Blume) Koidz.
Jeju National University
Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
Bristol-Myers Squibb
Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands.
Suven Life Sciences
Synthesis of new 8(S)-HETE analogs and their biological evaluation as activators of the PPAR nuclear receptors.
Universit�� De Rennes 1
Synthesis, in vitro ß-glucuronidase inhibitory activity and in silico studies of novel (E)-4-Aryl-2-(2-(pyren-1-ylmethylene)hydrazinyl)thiazoles.
University of Karachi
Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Structural and Enzymatic Analysis of Tumor-Targeted Antifolates That Inhibit Glycinamide Ribonucleotide Formyltransferase.
Duquesne University
Methods and compositions for studying, imaging, and treating pain
The Leland Stanford Junior University
Inhibitor Discovery for the Human GLUT1 from Homology Modeling and Virtual Screening.
Icahn School of Medicine At Mount Sinai
26- and 27-Methyl groups of 2-substituted, 19-nor-1a,25-dihydroxylated vitamin D compounds are essential for calcium mobilization in vivo.
University of Wisconsin-Madison
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
F. Hoffmann-La Roche
Identification of presynaptic serotonin autoreceptors using a new ligand: 3H-PAT.
College of France
Inverse in silico screening for identification of kinase inhibitor targets.
University of Munich