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

China Pharmaceutical 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
Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.

Washington University
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.

Guangzhou Institute of Biomedicine and Health
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.

Washington University
Synthesis and biological evaluation of 3,5-disubstituted-4-alkynylisoxozales as a novel class of HSP90 inhibitors.

Chengdu University of Tcm
Design, Synthesis, and Characterization of 3-(Benzylidene)indolin-2-one Derivatives as Ligands fora-Synuclein Fibrils.

Washington University
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.

Washington University
N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors.

Guangzhou Institutes of Biomedicine and Health
Synthesis of Deuterated Benzopyran Derivatives as Selective COX-2 Inhibitors with Improved Pharmacokinetic Properties.

Institutes of Biomedicine and Health
Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.

Chinese Academy of Sciences
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues ass2 receptor ligands.

Washington University
Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.

Washington 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
Evaluation of aminohydantoins as a novel class of antimalarial agents.

Saint Louis University
Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization.

First Affiliated Hospital of Guangzhou Medical University
Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter.

Washington University
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
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.

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
Synthesis, radiolabeling and initial in vivo evaluation of [(11)C]KSM-01 for imaging PPAR-a receptors.

Washington University
Synthesis and in vitro evaluation ofa-synuclein ligands.

Washington University
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.

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

Chinese Academy of Sciences
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization.

Chinese Academy of Sciences
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.

University of Minnesota
2-(2-Piperidyl)- and 2-(2-pyrrolidyl)chromans as nicotine agonists: synthesis and preliminary pharmacological characterization.

University of Minnesota
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues fors1 receptors.

Washington University
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.

Washington University
Hybrid compounds as new Bcr/Abl inhibitors.

Chinese Academy of Sciences
Synthesis and pharmacological evaluation of fluorine-containing D3 dopamine receptor ligands.

Washington University
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.

Washington University
Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.

Jinan University
Advanced Design, Synthesis, and Evaluation of Highly Selective Wee1 Inhibitors: Enhancing Pharmacokinetics and Antitumor Efficacy.

China Pharmaceutical University
Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.

Jinan University
Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography.

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

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

Jinan University
Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2-

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

Jinan University
Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.

Jinan University
Design, synthesis and structure-activity relationship studies of pyrido[2,3-d]pyrimidin-7-ones as potent Janus Kinase 3 (JAK3) covalent inhibitors.

Chinese Academy of Sciences
Discovery of Hexahydrofuro[3,2-

Jinan University
Discovery of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and selective CDK9 inhibitors that enable transient target engagement for the treatment of hematologic malignancies.

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

Jinan University
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.

Washington University
Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring

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

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

Guangzhou Institutes of Biomedicine and Health
Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer.

China Pharmaceutical University
Structure-activity relationship studies and bioactivity evaluation of 1,2,3-triazole containing analogues as a selective sphingosine kinase-2 inhibitors.

Washington University School of Medicine
4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl-

Saint Louis University
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors.

Jinan University
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.

Chinese Academy of Sciences
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.

Hefei University of Technology
4-Aryl Pyrrolidines as a Novel Class of Orally Efficacious Antimalarial Agents. Part 1: Evaluation of 4-Aryl- N-benzylpyrrolidine-3-carboxamides.

Saint Louis University
Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer.

Chinese Academy of Sciences
Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor.

Washington University
Substituent Position of Iminocyclitols Determines the Potency and Selectivity for Gut Microbial Xenobiotic-Reactivating Enzymes.

Academia Sinica
Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents.

Guangzhou Institutes of Biomedicine and Health
Synthesis and

Washington University School of Medicine
Synthesis and

Washington University School of Medicine
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
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.

Chinese Academy of Sciences
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
Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold.

Hefei University of Technology
Pentafluorosulfanyl-Substituted Benzopyran Analogues As New Cyclooxygenase-2 Inhibitors with Excellent Pharmacokinetics and Efficacy in Blocking Inflammation.

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

Jinan University
KRAS Modulating Compounds

Gilead Sciences
ESTROGEN RECEPTOR ANTAGONIST

Shenzhen Forward Pharmaceuticals Co.
NOVEL DIOXANE DERIVATIVES

Boehringer Ingelheim International
Cyclobutyl amide monoacylglycerol lipase modulators

Janssen Pharmaceutica
Substituted benzimidazoles, their preparation and their use as pharmaceuticals

Neomed Institute
Compositions and methods for the production of pyrimidine and pyridine compounds with BTK inhibitory activity

Merck Patent
Pyrrolopyrimidine compounds and uses thereof

Hutchison Medipharma
5-substituted-2-phenylamino benzamides as MEK inhibitors

Chugai Seiyaku Kabushiki Kaisha
Characterization of a novel class of polyphenolic inhibitors of plasminogen activator inhibitor-1.

University of Michigan
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.

Dupont Pharmaceuticals