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A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR

Guangzhou Institutes of Biomedicine and Health
2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors.

Chinese Academy of Sciences
Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents.

Soochow University
The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.

Chinese Academy of Sciences
Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors.

China Pharmaceutical University
Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors.

Jilin University
Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.

Guangzhou Institutes of Biomedicine and Health
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.

Guangzhou Institutes of Biomedicine and Health
1-Benzyl-4-phenyl-1H-1,2,3-triazoles improve the transcriptional functions of estrogen-related receptor¿ and promote the browning of white adipose.

Guangzhou Institutes of Biomedicine and Health
N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors.

Guangzhou Institutes of Biomedicine and Health
Small molecule discoidin domain receptor kinase inhibitors and potential medical applications.

Chinese Academy of Sciences
Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors.

China Pharmaceutical University
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.

Chinese Academy of Sciences
Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors.

China Pharmaceutical University
Evaluation of aminohydantoins as a novel class of antimalarial agents.

Saint Louis University
1-Phenyl-4-benzoyl-1H-1,2,3-triazoles as orally bioavailable transcriptional function suppressors of estrogen-related receptora.

Chinese Academy of Sciences
Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors.

Chinese Academy of Sciences
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.

Chinese Academy of Sciences
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)¿isoleucine(315) mutant.

Chinese Academy of Sciences
Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine7¿°¿ methionine7¿° mutant.

Chinese Academy of Sciences
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.

Guangzhou Institute of Biomedicine and Health
Structure-activity study on a series ofa-glutamic acid scaffold based compounds as new ADAMTS inhibitors.

Chinese Academy of Sciences
Hybrid compounds as new Bcr/Abl inhibitors.

Chinese Academy of Sciences
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.

TBA
Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction.

University of Michigan
Cell-active, irreversible covalent inhibitors that selectively target the catalytic lysine of EGFR by using fluorosulfate-based SuFEx chemistry.

National University of Singapore
Discovery of novel macrocyclic derivatives as potent and selective cyclin-dependent kinase 2 inhibitors.

Tianjin University
Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors.

Tianjin University
Discovery and optimization of thieno[3,2-d]pyrimidine derivatives as highly selective inhibitors of cyclin-dependent kinase 7.

Tianjin University
Discovery of Novel Diaryl-Substituted Fused Heterocycles Targeting Katanin and Tubulin with Potent Antitumor and Antimultidrug Resistance Efficacy.

Fudan University
Discovery of LHQ490 as a highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor.

East China Normal University
Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader.

Shanghai Institute of Organic Chemistry
Targeting EGFR degradation by autophagosome degraders.

Jinan University
Discovery of 5-aminopyrido[2,3-d]pyrimidin-7(8H)-one derivatives as new hematopoietic progenitor kinase 1 (HPK1) inhibitors.

Shanghai Institute of Organic Chemistry
Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.

Jinan University
Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer.

Jinan University
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.

University of Michigan
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.

Jinan University
Structural Mechanism and Inhibitors Targeting EGFR Exon 20 Insertion (Ex20ins) Mutations.

Jinan University
Rational Design of Covalent Kinase Inhibitors by an Integrated Computational Workflow (Kin-Cov).

Jinan University
Discovery of chiral 1,4-diarylazetidin-2-one-based hydroxamic acid derivatives as novel tubulin polymerization inhibitors with histone deacetylase inhibitory activity.

Fudan University
Discovery of a First-in-Class Degrader for the Lipid Kinase PIKfyve.

Chinese Academy of Sciences
Discovery of AXL Degraders with Improved Potencies in Triple-Negative Breast Cancer (TNBC) Cells.

Jinan University
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
Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.

Jinan University
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.

Jinan University
Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.

Chinese Academy of Sciences
Design of novel hexahydropyrazinoquinolines as potent and selective dopamine D3 receptor ligands with improved solubility.

University of Michigan
Discovery of Hexahydrofuro[3,2-

Jinan University
Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13.

Jinan University
Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors.

Jinan University
A novel photocaged B-Raf

Shanghai Institute of Organic Chemistry
Enantiomerically pure hexahydropyrazinoquinolines as potent and selective dopamine 3 subtype receptor ligands.

University of Michigan
Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells.

Jinan University
Design, synthesis and structure-activity relationship studies of hexahydropyrazinoquinolines as a novel class of potent and selective dopamine receptor 3 (D3) ligands.

University of Michigan
The untapped potential of spermidine alkaloids: Sources, structures, bioactivities and syntheses.

Beijing University of Chinese Medicine
Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors.

Jinan University
Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors.

Jinan University
Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design.

Jinan University
Novel Electrophilic Warhead Targeting a Triple-Negative Breast Cancer Driver in Live Cells Revealed by "Inverse Drug Discovery".

Jinan University
Design, Synthesis, and Biological Evaluation of 2-Formyl Tetrahydronaphthyridine Urea Derivatives as New Selective Covalently Reversible FGFR4 Inhibitors.

Jinan University
Discovery of novel TrkA allosteric inhibitors: Structure-based virtual screening, biological evaluation and preliminary SAR studies.

Jinan University
Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders.

Chinese Academy of Sciences
Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR

Jinan University
Proteome-wide Identification of Off-Targets of a Potent EGFR

University of Macau
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.

Guangzhou Institutes of Biomedicine and Health
Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.

Jinan University
Structure-Based Discovery and Optimization of Benzo[ d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).

Guangzhou Medical University
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.

Jinan University
Design and synthesis of selective degraders of EGFR

Jinan University
Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.

Jinan University
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.

Jinan University
Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor.

Jinan University
Discovery of New Monocarbonyl Ligustrazine-Curcumin Hybrids for Intervention of Drug-Sensitive and Drug-Resistant Lung Cancer.

China Pharmaceutical University
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors.

Chinese Academy of Sciences
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.

Chinese Academy of Sciences
Colocalization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor.

Shanghaitech University
2-Amino-2,3-dihydro-1

Jinan University
Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).

School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects.

Jinan University
Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR

Jinan University
Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin.

Fudan University
Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.

Jinan University
Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors.

Chinese Academy of Sciences
Design and Optimization of 3'-(Imidazo[1,2-

Jinan University
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
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
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
Identification and synthesis of substituted pyrrolo[2,3-d]pyrimidines as novel firefly luciferase inhibitors.

Chinese Academy of Sciences
Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation.

Jinan University
Discovery of JND3229 as a New EGFR

Jinan University
Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.

Guangzhou Medical University
Design, synthesis, and discovery of 5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones and related derivatives as novel inhibitors of mPGES-1.

University of Kentucky
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.

Chinese Academy of Sciences
Rational Design and Structure Validation of a Novel Peptide Inhibitor of the Adenomatous-Polyposis-Coli (APC)-Rho-Guanine-Nucleotide-Exchange-Factor-4 (Asef) Interaction.

Jinan University
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.

Jinan University
Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.

Guangzhou Medical University
Selective inhibitors of human mPGES-1 from structure-based computational screening.

University of Kentucky
Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.

University of Macau
2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors.

Guangzhou Institutes of Biomedicine and Health
Tetrahydroisoquinoline-7-carboxamide Derivatives as New Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.

Jinan University
Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.

Chinese Academy of Sciences
STABLE CRYSTAL OF 4-OXOQUINOLINE COMPOUND

Japan Tobacco
Triazolopyrimidines, their preparation and use

Columbia University
Modulators of HSD17B13 and methods of use thereof

Regeneron Pharmaceuticals
Cyclobutyl amide monoacylglycerol lipase modulators

Janssen Pharmaceutica
Pyrrolopyrimidine compounds and uses thereof

Hutchison Medipharma
Galactoside inhibitors of galectins

Galecto Biotech
Characterization of a novel class of polyphenolic inhibitors of plasminogen activator inhibitor-1.

University of Michigan
Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants.

Max-Planck-Institut Fuer Biochemie