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Design, synthesis and antithrombotic evaluation of novel non-peptide thrombin inhibitors.

China Pharmaceutical University
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

Janssen Research and Development
Discovery of a Series of 5,11-Dihydro-6

Dana-Farber Cancer Institute
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.

Fudan University
Discovery of highly potent TNFa inhibitors using virtual screen.

Peking University
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.

Pkucare Pharmaceutical R & D Center
Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.

University of Texas At Dallas
Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E(2) synthase-1.

Peking University
Identification of small molecule sphingomyelin synthase inhibitors.

Fudan University
Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.

Astex Pharmaceuticals
Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11ß-HSD1 inhibitors: potential impact in diabetes.

Chinese Academy of Sciences
SAR Based Optimization of a 4-Quinoline Carboxylic Acid Analog with Potent Anti-Viral Activity.

University of Texas Southwestern Medical Center
X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.

University of Oxford
Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase.

Janssen Research and Development
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.

Glaxosmithkline
Brain Penetrant LRRK2 Inhibitor.

TBA
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

University of Dundee
Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1.

TBA
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.

Glaxosmithkline
Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors.

TBA
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.

University of Washington
Expanding the diversity of allosteric bcr-abl inhibitors.

Harvard Medical School
Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration.

Xiamen University
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.

University of Dundee
Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).

Harvard Medical School
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.

Harvard Medical School
Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.

The Scripps Research Institute
Design, Synthesis, and Biological Activity of Novel Quinone Derivatives as Potent STAT3 Inhibitors for Psoriasis Treatment.

Central South University
Discovery of meisoindigo derivatives as noncovalent and orally available Mpro inhibitors: their therapeutic implications in the treatment of COVID-19.

Central South University
Structure-based design of SARS-CoV-2 papain-like protease inhibitors.

State University of New Jersey
Discovery of Novel ERα and Aromatase Dual-Targeting PROTAC Degraders to Overcome Endocrine-Resistant Breast Cancer.

Zhongnan Hospital of Wuhan University
pH regulators and their inhibitors in tumor microenvironment.

University of South China
Discovery of a Meisoindigo-Derived PROTAC as the ATM Degrader: Revolutionizing Colorectal Cancer Therapy via Synthetic Lethality with ATR Inhibitors.

Central South University
Novel estrogen receptor β/histone deacetylase dual-targeted near-infrared fluorescent probes as theranostic agents for imaging and treatment of prostate cancer.

Zhongnan Hospital of Wuhan University
Discovery of novel amide derivatives as potent quorum sensing inhibitors of Pseudomonas aeruginosa.

South China Agricultural University
Synthesis-accessibility-oriented design of c-Jun N-terminal kinase 1 inhibitor.

East China University of Science and Technology
Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants.

Sichuan Normal University
Identification of Novel Dual-Target Estrogen Receptor α Degraders with Tubulin Inhibitory Activity for the Treatment of Endocrine-Resistant Breast Cancer.

Zhongnan Hospital of Wuhan University
Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer

Zhongnan Hospital of Wuhan University
Structure-guided identification of novel dual-targeting estrogen receptor α degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast cancer.

Zhongnan Hospital of Wuhan University
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.

Abbott Laboratories
Sulfonamide derivatives as potential anti-cancer agents and their SARs elucidation.

Hunan University of Science and Technology
Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.

Abbott Laboratories
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.

Johnson and Johnson Pharmaceutical Research and Development
Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.

Abbott Laboratories
Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer.

Wuhan University
Recent development of BTK-based dual inhibitors in the treatment of cancers.

Nantong University
Imaging Autotaxin

Harvard Medical School
Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.

Sichuan Normal University
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.

Medicines For Malaria Venture
Discovery of methyl 3-((2-((1-(dimethylglycyl)-5-methoxyindolin-6-yl)amino)-5-(trifluoro-methyl) pyrimidin-4-yl)amino)thiophene-2-carboxylate as a potent and selective polo-like kinase 1 (PLK1) inhibitor for combating hepatocellular carcinoma.

Xiamen University
Fluoro analogs of bioactive oxy-sterols: Synthesis of an EBI2 agonist with enhanced metabolic stability.

Janssen Research & Development
Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors.

Shanghai Jiao Tong 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
Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.

University of Washington
Design, synthesis and bioactivity study of N-salicyloyl tryptamine derivatives as multifunctional agents for the treatment of neuroinflammation.

Lanzhou University
Synthesis and pharmacokinetic study of a

Harvard Medical School
Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors.

Xiamen University
Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6

Harvard Medical School
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.

University of Washington
Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors.

Guangxi Medical University
Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study.

Guangxi Medical University
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.

Jinan University
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
Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.

Uit The Arctic University of Norway
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

Janssen Research and Development
NON-ACID INHIBITORS OF INOSITOL HEXAKISPHOSPHATE KINASE (IP6K) AND METHODS OF USE THEREOF

Lieber Institute
Cereblon ligands and bifunctional compounds comprising the same

Arvinas Operations
ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE THEREOF

Merck Sharp & Dohme
PYRAZOLE-SUBSTITUTED CYCLOPENTANOL ESTER DERIVATIVE AND USE THEREOF

Chia Tai Tianqing Pharmaceutical Group
COMPOUND AS ATR KINASE INHIBITOR

Suzhou Ark Biopharmaceutical Co.
MACROCYCLIC 1,3-BRIDGED 6-CHLORO-7-PYRAZOL-4-YL-1 H-INDOLE-2-CARBOXYLATE AND 6-CHLORO-7-PYRIMIDIN-5-YL-1H-INDOLE-2-CARBOXYLATE DERIVATIVES AS MCL-1 INHIBITORS FOR THE TREATMENT OF CANCER

Janssen Pharmaceutica
Substituted pyrazolopyrimidines useful as kinases inhibitors

Teligene
2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof

Shanghai Haiyan Pharmaceutical Technology
Cosmetic compositions containing substituted azole and methods for improving the appearance of aging skin

The Procter & Gamble
Isatin based Schiff bases as inhibitors of a-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies.

Hazara University
(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives, preparation thereof and pharmaceutical use thereof as AKT(PKB) phosphorylation inhibitors

Sanofi
Structure-activity study of brassinin derivatives as indoleamine 2,3-dioxygenase inhibitors.

Bryn Mawr College