PMID
Data
Article Title
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Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors.

Roche Innovation Center Shanghai
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.

Chinese Academy of Sciences
Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment.

Wuxi Apptec (Shanghai)
Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.

Hangzhou Xixi Hospital
Recent Advances in Scaffold Hopping.

Rheinische Friedrich-Wilhelms-Universit£T
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.

Global Blood Therapeutics
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
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.

Zhejiang University
Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors.

Shanghai Institute of Materia Medica
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.

Chinese Academy of Sciences
Discovery of novel nonpeptide allosteric inhibitors interrupting the interaction of CDK2/cyclin A3 by virtual screening and bioassays.

Dalian Medical University
Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy.

Zhejiang University
Synthesis and Biological Evaluation of Novel Olean-28,13ß-lactams as Potential Antiprostate Cancer Agents.

China Pharmaceutical University
Species-dependent uptake of glycylsarcosine but not oseltamivir in Pichia pastoris expressing the rat, mouse, and human intestinal peptide transporter PEPT1.

University of Michigan
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.

Chinese Academy of Sciences
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold.

Zhejiang University
Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.

Zhejiang University
Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.

Zhejiang University
Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia.

TBA
Design, synthesis and biological evaluation of 6-(nitroimidazole-1H-alkyloxyl)-4-anilinoquinazolines as efficient EGFR inhibitors exerting cytotoxic effects both under normoxia and hypoxia.

Zhejiang University
Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed fromß-amino acid as proteasome inhibitors.

Zhejiang University
Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors.

Zhejiang University
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.

Zhejiang University
Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors.

Zhejiang University
Characterization of a novela-conotoxin TxID from Conus textile that potently blocks rata3ß4 nicotinic acetylcholine receptors.

Hainan University
Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3ß (GSK-3ß) inhibitors.

Zhejiang University
Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.

Zhejiang University
Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors.

Activx Biosciences
Amides of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid as zinc-dependent inhibitors of Lp-PLA2.

Activx Biosciences
Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents.

Nanjing University
Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors.

The Hong Kong University of Science and Technology
Development of substituted N-[3-(3-methoxylphenyl)propyl] amides as MT(2)-selective melatonin agonists: improving metabolic stability.

Hong Kong University of Science and Technology
Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.

Zhejiang Betapharma
Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.

Astrazeneca
Synthesis and structure-activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1/AADACL1).

Activx Biosciences
5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP.

University of Texas Medical Branch
Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinasea (PI3Ka) inhibitors.

Zhejiang University
Structure-activity relationship of a new series of reversible dual monoacylglycerol lipase/fatty acid amide hydrolase inhibitors.

Universidad Complutense De Madrid
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.

Zhejiang University
Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease.

Zhejiang University
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.

Wyeth Research
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.

Wyeth Research
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.

Zhejiang University
Synthesis, molecular docking and biological evaluation of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.

Nanjing University
Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2).

Activx Biosciences
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.

Zhejiang University
Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.

Pfizer
Pharmacophore identification, virtual screening and biological evaluation of prenylated flavonoids derivatives as PKB/Akt1 inhibitors.

Zhejiang University
Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition.

Pfizer
Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Ka inhibitors.

Zhejiang University
Identification and SAR of a new series of thieno[3,2-d]pyrimidines as Tpl2 kinase inhibitors.

Pfizer
Discovery of indazoles as inhibitors of Tpl2 kinase.

Pfizer
Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity.

Pfizer
Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity.

Pfizer
Compounds structurally related to ellagic acid show improved antiplasmodial activity.

Justus-Liebig-University
Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure-activity relationship.

Pfizer
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.

Pfizer
The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).

Wyeth Research
B-Raf kinase inhibitors: hit enrichment through scaffold hopping.

Wyeth Research
Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands.

Hong Kong University of Science and Technology
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.

Wyeth
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.

Wyeth Research
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.

Wyeth Research
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.

Wyeth Research
Discovery of highly potent and selective type I B-Raf kinase inhibitors.

Wyeth Research
Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.

Zhejiang University
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.

Wyeth Research
Novel pyrazolopyrimidines as highly potent B-Raf inhibitors.

Wyeth Research
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.

Wyeth Research
QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine.

Zhejiang University
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).

Institute of Pharmacology and Toxicology
3,4-Disubstituted benzofuran P1' MMP-13 inhibitors: optimization of selectivity and reduction of protein binding.

Wyeth Research
Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase.

Activx Biosciences
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.

Zhejiang University
Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.

Wyeth Research
Synthesis and biological activity of 2-desamino and 4-deoxy analogs of 5,10-dideazatetrahydrofolic acid (DDATHF)

TBA
Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors.

Wyeth Research
Identification of pharmacophore model, synthesis and biological evaluation of N-phenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors.

Zhejiang University
Discovery of the catechol structural moiety as a Stat3 SH2 domain inhibitor by virtual screening.

Wyeth Pharmaceuticals
2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity.

Zhejiang University
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.

Zhejiang University
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.

Zhejiang University
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.

Wyeth Research
Recent advances in small molecule and peptide inhibitors of glucose-regulated protein 78 for cancer therapy.

The First Affiliated Hospital of Henan University
Research progress of VEGFR small molecule inhibitors in ocular neovascular diseases.

Southwest Jiaotong University
Discovery of new tetrahydroisoquinolines as potent and selective LSD1 inhibitors for the treatment of MLL-rearranged leukemia.

Zhejiang Ocean University
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.

Wyeth Research
Cellular, Structural Basis, and Recent Progress for Targeting Murine Double Minute X (MDMX) in Tumors.

Yantai University
Discovery and Optimization of Hsp110 and sGC Dual-Target Regulators for the Treatment of Pulmonary Arterial Hypertension.

Central South University
Total synthesis/semi-synthesis of natural isopentenyl flavonoids with inhibitory activity on NLRP3 inflammasome.

East China University of Science and Technology
Benzodioxane Carboxamide Derivatives As Novel Monoamine Oxidase B Inhibitors with Antineuroinflammatory Activity.

Zunyi Medical University
Design, synthesis and evaluation of novel UDCA-aminopyrimidine hybrids as ATX inhibitors for the treatment of hepatic and pulmonary fibrosis.

Chinese Academy of Medical Sciences and Peking Union Medical College
Coumarin-furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies.

Hubei University
Discovery of N-alkyl-N-benzyl thiazoles as novel TRPC antagonists for the treatment of glioblastoma multiforme.

Yantai University
Discovery and Optimization of Tetrahydroisoquinoline Derivatives To Enhance Lysosome Biogenesis as Preclinical Candidates for the Treatment of Alzheimer's Disease.

Nanjing University of Chinese Medicine
Thiophene substituted acylguanidines as BACE1 inhibitors.

Wyeth Research
New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs.

China Pharmaceutical University
Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles.

Wyeth Research
Design, Synthesis, and Antitumor Efficacy of Substituted 2-Amino[1,2,4]triazolopyrimidines and Related Heterocycles as Dual Inhibitors for Microtubule Polymerization and Janus Kinase 2.

Wuyi University
A novel BODIPY-based theranostic agent for

Shanghai Institute of Materia Medica
Discovery of marine phidianidine-based Nrf2 activators and their potential against oxLDL- and HG-induced injury in HUVECs.

University of Jinan
Degradation of Cyclin-Dependent Kinase 9/Cyclin T1 by Optimized Microtubule-Associated Protein 1 Light Chain 3 Beta-Recruiting Coumarin Analogs.

Shanghai Institute of Materia Medica
Machine learning- and structure-based discovery of a novel chemotype as FXR agonists for potential treatment of nonalcoholic fatty liver disease.

Chinese Academy of Medical Sciences&Peking Union Medical College
Discovery of (

Shanghai Institute of Materia Medica
Discovery of Novel Sesquiterpene Lactone Derivatives as Potent PKM2 Activators for the Treatment of Ulcerative Colitis.

Nanjing University of Chinese Medicine
Discovery of selective Na

Shanghai Institute of Materia Medica
Affinity of Rimantadine Enantiomers against Influenza A/M2 Protein Revisited.

National and Kapodistrian University of Athens
Recent advances of dual FGFR inhibitors as a novel therapy for cancer.

Southwest Jiaotong University
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.

Ariad Pharmaceuticals
Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.

Wyeth Research
Discovery and preclinical evaluations of GST-HG131, a novel HBV antigen inhibitor for the treatment of chronic hepatitis B infection.

Wuxi Apptec
Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.

Sun Yat-Sen University Cancer Center
Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold.

University of Chinese Academy of Sciences
Long Residence Time at the Vasopressin V

Xuzhou Medical University
Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer.

Fujian Medical University (Fmu)
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors.

The University of Arizona
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel ALK inhibitors.

Shenyang Pharmaceutical University
Discovery of highly potent SARS-CoV-2 M

Nanjing University of Chinese Medicine
Progress and Challenges in Targeting the SARS-CoV-2 Papain-like Protease.

The State University of New Jersey
Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.

Wyeth Research
Synthesis and SAR of highly selective MMP-13 inhibitors.

Wyeth Research
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.

Activx Biosciences
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.

Activx Biosciences
NAE modulators: A potential therapy for gastric carcinoma.

Southwest Jiaotong University
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.

Schering-Plough Research Institute
Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.

Wuxi Apptec
Synthesis and application of phosphorylated saccharides in researching carbohydrate-based drugs.

Henan University of Chinese Medicine
Identification of the Benzoimidazole Compound as a Selective FLT3 Inhibitor by Cell-Based High-Throughput Screening of a Diversity Library.

Sun Yat-Sen University Cancer Center
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.

Takeda Pharmaceuticals International
A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice.

The Hong Kong University of Science and Technology
Discovery of Potent Antiallergic Agents Based on an

Chinese Academy of Sciences
Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.

Shenyang Pharmaceutical University
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.

Millennium Pharmaceuticals, A Wholly Owned Subsidiary of Takeda Pharmaceuticals
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.

Schering-Plough Research Institute
Discovery of

Zhejiang University
Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.

Shanghai Jiao Tong University (Sjtu)
A theranostic probe of indoleamine 2,3-dioxygenase 1 (IDO1) for small molecule cancer immunotherapy.

Second Military Medical University
Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H

Zhejiang University
Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.

Shanghai Institute of Materia Medica
Discovery of 1,5-Dihydro-4

Zhejiang University
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes.

Fudan University
Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells.

Hangzhou Institute of Innovative Medicine
Structurally novel PI3Kδ/γ dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation.

Anhui University of Chinese Medicine
Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine γ-Lyase.

Shanghai Jiao Tong University
Synthesis and Anti-HCV Activity of Sugar-Modified Guanosine Analogues: Discovery of

Janssen Biopharma
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth.

Georgetown University Medical Center
Synthesis and aromatase inhibitory evaluation of 4-N-nitrophenyl substituted amino-4H-1,2,4-triazole derivatives.

Key Laboratory of Industrial Fermentation Microbiology (Tianjin University of Science & Technology)
Novel tricyclic poly (ADP-ribose) polymerase-1/2 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis and biological evaluation.

China Pharmaceutical University
Effective Virtual Screening Strategy toward heme-containing proteins: Identification of novel IDO1 inhibitors.

China Pharmaceutical University
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.

Chinese Academy of Sciences
Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.

Zhejiang University
Synthesis and Anti-HCV Activities of 4'-Fluoro-2'-Substituted Uridine Triphosphates and Nucleotide Prodrugs: Discovery of 4'-Fluoro-2'- C-methyluridine 5'-Phosphoramidate Prodrug (AL-335) for the Treatment of Hepatitis C Infection.

Janssen Biopharma
Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies.

Zhejiang University
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.

TBA
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.

Zhejiang University
Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors.

Zhejiang University
Discovery of N

Zhuhai Campus of Zunyi Medical University
Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an

Chinese Academy of Sciences
Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors.

Hangzhou Institute of Innovative Medicine
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.

Zhejiang University
Design and synthesis of novel 3-substituted-indole derivatives as selective H3 receptor antagonists and potent free radical scavengers.

Zhejiang University
Structure-based drug design using GPCR homology modeling: toward the discovery of novel selective CysLT2 antagonists.

Zhejiang University
Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors.

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

Chinese Academy of Sciences
Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.

Chinese Academy of Sciences
Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors.

Chinese Academy of Sciences
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.

Wyeth Research
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.

Georgetown University Medical Center
Design, synthesis, and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors.

Shenyang Pharmaceutical University
Synthesis and biological evaluation of coumarin derivatives containing imidazole skeleton as potential antibacterial agents.

Northwest A&F University
Synthesis and biological evaluation of NH

Shenyang Pharmaceutical University
Design, synthesis and structure-activity relationship study of novel naphthoindolizine and indolizinoquinoline-5,12-dione derivatives as IDO1 inhibitors.

Peking University
Discovery of N-aryl-N'-pyrimidin-4-yl ureas as irreversible L858R/T790M mutant selective epidermal growth factor receptor inhibitors.

Shanghai Haiyan Pharmaceutical Technology Co. Itd.
Discovery of imidazoleisoindole derivatives as potent IDO1 inhibitors: Design, synthesis, biological evaluation and computational studies.

China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.

Chinese Academy of Sciences
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors.

Shanghai Jiao Tong University
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.

University of Michigan
Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.

TBA
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.

School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
Slow but Steady Wins the Race: Dissimilarities among New Dual Inhibitors of the Wild-Type and the V27A Mutant M2 Channels of Influenza A Virus.

Universitat De Barcelona
Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety.

Xinxiang Medical University
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.

The University of Arizona
BICYCLIC CX3CR1 RECEPTOR AGONISTS

University of Texas System
SUBSTITUTED 6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF

Sanofi
Compounds and uses thereof

Foghorn Therapeutics
Inhibitors

Vivoryon Therapeutics
3-BETA-HSD1 INHIBITORS AND COMPOSITIONS AND USES THEREOF

The Cleveland Clinic Foundation
3-[(1H-PYRAZOL-4-YL)OXY]PYRAZIN-2-AMINE COMPOUNDS AS HPK1 INHIBITOR AND USE THEREOF

BeiGene
METHODS FOR INHIBITING PARASITIC GLUCOKINASE AND/OR HEXOKINASE

University of South Carolina
TYK2 INHIBITORS

Biogen Ma
Substituted benzodiazoles and use thereof in therapy

Thomas Helledays Stiftelse FÖR Medicinsk Forskning
Methods of inhibiting cyclooxygenase

King Faisal University
Advantageous benzofuran compositions for mental disorders or enhancement

Tactogen
Substituted pyridopyrimidinonyl compounds useful as T cell activators

Bristol-Myers Squibb
ACLY inhibitors and uses thereof

Nimbus Artemis
Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, Rasopathies, and fibrotic disease

Shy Therapeutics
Heterocyclic compounds for the inhibition of PASK

Bioenergenix
Pyridazines

Boehringer Ingelheim International
Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same

Sk Biopharmaceuticals
Inhibitors of lysine specific demethylase-1

Celgene Quanticel Research
Therapeutically active compounds and their methods of use

Agios Pharmaceuticals
Imidazopyrazine compounds, preparation methods and uses thereof

Dongguan Zhenxing-Beite Medicine Technology
KV1.3 inhibitors and their medical application

4Sc
4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase

Eastern Virginia Medical School
Macrocylic compounds as ROS1 kinase inhibitors

Array Biopharma
Chemokine CXCR1 and CXCR2 receptor antagonist compounds, and use thereof in the treatment of chemokine-mediated pathologies

Galderma Research & Development
Inhibitors of RET

Blueprint Medicines
2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use

Genentech
[4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or salt thereof

Santen Pharmaceutical
Pyridinone and pyrimidinone derivatives as factor Xia

Ono Pharmaceutical
7-azaindole derivatives

Merck Patent
Inhibitors of RET

Blueprint Medicines
Somatostatin receptor subtype 4 (SSTR4) agonists

Centrexion Therapeutics
Alkylene derivatives

Shionogi
Piperidinone derivatives as MDM2 inhibitors for the treatment of cancer

Amgen
Inhibitors of lysine specific demethylase-1

Celgene Quanticel Research
Synthesis and HIV-1 RT inhibitory action of novel (4/6-substituted benzo[d]thiazol -2-yl)thiazolidin-4-ones. Divergence from the non-competitive inhibition mechanism.

Aristotle University of Thessaloniki
Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cell migration.

University of Colorado School of Medicine
Synthesis and biological evaluation of novel flavanone derivatives as potential antipsychotic agents.

Key Laboratory For Neurodegenerative Diseases of Ministry of Education
Synthesis and in silico studies of novel sulfonamides having oxadiazole ring: As ß-glucuronidase inhibitors.

Universiti Teknologi Mara (Uitm)
Piperidylpyrimidine derivatives as modulators of protein kinase inhibitors and of vascular endothelial growth factor receptor 2

Allergan
Triazolopyridinone PDE10 inhibitors

Merck Sharp & Dohme
Discovery and Characterization of Allosteric WNK Kinase Inhibitors.

Novartis Institutes For Biomedical Research
Morpholinylbenzotriazines for use in cancer therapy

Merck Patent
Inhibitors of human EZH2, and methods of use thereof

Epizyme
Rosuvastatin and atorvastatin derivatives

Redx Pharma
Design, Synthesis, and Evaluation of Polyamine Deacetylase Inhibitors, and High-Resolution Crystal Structures of Their Complexes with Acetylpolyamine Amidohydrolase.

University of Pennsylvania
Mechanistic studies of inactivation of inducible nitric oxide synthase by amidines.

Northwestern University
Modulators of calcium release-activated calcium channel

Rhizen Pharmaceuticals
Piperazine compound capable of inhibiting prostaglandin D synthase

Taiho Pharmaceutical
Substituted benzamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same

Vanderbilt University
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.

Purdue University
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors.

Santhera Pharmaceuticals
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.

Vernalis (R&D)