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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
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.

East China University of Science and Technology
Discovery of novel BTK inhibitors with carboxylic acids.

Merck
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.

Genentech
Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the 'reversed' amide scaffold.

Soochow University
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.

Peking Union Medical College
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).

Constellation Pharmaceuticals
Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors.

Soochow University
Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.

Genentech
2-Aminopyrimidin-4(1H)-one as the novel bioisostere of urea: discovery of novel and potent CXCR2 antagonists.

Glaxosmithkline
Thermodynamic and structural characterization of halogen bonding in protein-ligand interactions: a case study of PDE5 and its inhibitors.

Chinese Academy of Sciences (Cas)
Reaction intermediate analogues as bisubstrate inhibitors of pantothenate synthetase.

Soochow University
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles as inhibitors of transforming growth factor-ß type I receptor (ALK5).

Capital Normal University
Discovery and optimization of novel 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazones as c-Met kinase inhibitors.

Shenyang Pharmaceutical University
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11ß-Hydroxysteroid Dehydrogenase Type 1 Inhibitors.

TBA
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.

TBA
Targeting zymogen activation to control the matriptase-prostasin proteolytic cascade.

University of Maryland
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.

Vitae Pharmaceuticals
Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.

Vitae Pharmaceuticals
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.

East China University of Science and Technology
Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.

Shanghai Hengrui Pharmaceuticals
Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.

Vitae Pharmaceuticals
Optimization of orally bioavailable alkyl amine renin inhibitors.

Vitae Pharmaceuticals
Design, structure activity and x-ray crystallographic studies of pseudosymmetrical nonpeptidyl HIV-1 protease inhibitors

TBA
Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers.

Huanghuai University
Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma.

Chinese Academy of Sciences
Synthesis and biological evaluation of multimodal monoaminergic arylpiperazine derivatives with potential antidepressant profile.

University of Chinese Academy of Sciences
Rational Design of a Novel 6H-Benzo[c]chromen Series as Selective PI3Kα Inhibitors.

Xi'an Jiaotong University
Discovery of JAB-3312, a Potent SHP2 Allosteric Inhibitor for Cancer Treatment.

Jacobio Pharmaceuticals
Discovery of ZJCK-6-46: A Potent, Selective, and Orally Available Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A Inhibitor for the Treatment of Alzheimer's Disease.

Shenyang Pharmaceutical University
Impact of atropisomerism on a non-steroidal glucocorticoid receptor agonist.

WuXi AppTec
Design, synthesis and structure-activity relationship of 1,8-naphthalimide derivatives as highly potent hCYP1B1 inhibitors.

Nanjing University of Chinese Medicine
Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor.

WuXi AppTec
Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer.

China Pharmaceutical University
Discovery, Optimization, and Evaluation of Novel Pyridin-2(1H)-one Analogues as Potent TRK Inhibitors for Cancer Treatment.

Shanghai Tech University
Small Molecule Targeting PPM1A Activates Autophagy for Mycobacterium tuberculosis Host-Directed Therapy.

Nanjing University of Chinese Medicine
Structure-Based Optimization of Novel Sterol 24-C-Methyltransferase Inhibitors for the Treatment of Candida albicans Infections.

Shandong University
Design, synthesis, and biological evaluation of 5-(1H-indol-5-yl)isoxazole-3-carboxylic acids as novel xanthine oxidase inhibitors.

Wuhan Institute of Technology
Recent updates on 1,2,3-triazole-containing hybrids with in vivo therapeutic potential against cancers: A mini-review.

Wuhan University of Science and Technology
Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo.

Shanghai Institute of Materia Medica
Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel coumarin derivatives as multifunctional ligands for the treatment of Alzheimer's disease.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of salicylanilides as novel allosteric inhibitors of human pancreatic lipase.

Shanghai University of Traditional Chinese Medicine
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib.

Anhui University of Chinese Medicine
Discovery of a Series of Indane-Containing NBTIs with Activity against Multidrug-Resistant Gram-Negative Pathogens.

Roche Pharma Research & Early Development
Discovery of Linvencorvir (RG7907), a Hepatitis B Virus Core Protein Allosteric Modulator, for the Treatment of Chronic HBV Infection.

China Innovation Center of Roche
The Development and Design Strategy of Leucine-Rich Repeat Kinase 2 Inhibitors: Promising Therapeutic Agents for Parkinson's Disease.

China Pharmaceutical University
The lipidation and glycosylation enabling bioactivity enhancement and structural change of antibacterial peptide G3.

Fujian Normal University
Design, synthesis and anticancer evaluation of selective 2,4-disubstituted pyrimidine CDK9 inhibitors.

Southeast University
Design, synthesis and evaluation of fused hybrids with acetylcholinesterase inhibiting and Nrf2 activating functions for Alzheimer's disease.

China Pharmaceutical University
Overview of piperlongumine analogues and their therapeutic potential.

Nantong University
A concise review of recent advances in anti-heart failure targets and its small molecules inhibitors in recent years.

University of Electronic Science and Technology of China
Long Residence Time at the Vasopressin V

Xuzhou Medical University
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease.

Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects.

Shenyang Pharmaceutical University
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.

Genentech
Chemo- and Site-Selective Lysine Modification of Peptides and Proteins under Native Conditions Using the Water-Soluble Zolinium.

Chinese Academy of Sciences
Recent development of BTK-based dual inhibitors in the treatment of cancers.

Nantong University
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.

Hubei Polytechnic University
Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.

Nantong University
Glycosylation increases the anti-QS as well as anti-biofilm and anti-adhesion ability of the cyclo (L-Trp-L-Ser) against Pseudomonas aeruginosa.

Fujian Normal University
Synthesis and activity of substituted 4-(indazol-3-yl)phenols as pathway-selective estrogen receptor ligands useful in the treatment of rheumatoid arthritis.

Wyeth Research
Identification of Small Molecule Inhibitors of RNase L by Fragment-Based Drug Discovery.

Peking University Shenzhen Graduate School
Discovery of chiral N-2'-aryletheryl-1'-alkoxy-ethyl substituted arylisoquinolones with anti-inflammatory activity from the nucleophilic addition reactions of the thiophenols and oxazolinium.

Chinese Academy of Sciences
Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.

Shenyang Pharmaceutical University
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.

Merck
Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.

Lanzhou University
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.

Merck
Identification of Potent Reverse Indazole Inhibitors for HPK1.

Merck
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.

Merck Research Laboratories
Piperlonguminine and Piperine Analogues as TrxR Inhibitors that Promote ROS and Autophagy and Regulate p38 and Akt/mTOR Signaling.

Nantong University
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.

Genentech
Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5).

Merck
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research and Early Development
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.

Roche Innovation Center Shanghai
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.

Genentech
Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.

Wuxi Apptec
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.

Chinese Academy of Sciences
Inhibition of polypeptide N-acetyl-α-galactosaminyltransferases is an underlying mechanism of dietary polyphenols preventing colorectal tumorigenesis.

Shanghai Jiao Tong University
Benzofuran derivatives and their anti-tubercular, anti-bacterial activities.

Huanghuai University
Coumarin-containing hybrids and their anticancer activities.

Tsinghua University
Tetrazole hybrids with potential anticancer activity.

Henan University of Chinese Medicine
1,2,4-Triazole-quinoline/quinolone hybrids as potential anti-bacterial agents.

Henan University of Chinese Medicine
1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.

Guizhou University of Traditional Chinese Medicine
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.

Genentech
Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies.

The University of Arizona
Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction.

Roche Innovation Center Shanghai
Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors.

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

Wyeth Research
Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors.

Wuhan University
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.

University of Wollongong
Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids.

Peking Union Medical College
Quinoline hybrids and their antiplasmodial and antimalarial activities.

Hubei Engineering University
Triazole derivatives and their anti-tubercular activity.

Wuhan University of Science and Technology
Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.

Shanghai Hengrui Pharmaceutical
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.

Walter and Eliza Hall Institute of Medical Research
Discovery of new MD2-targeted anti-inflammatory compounds for the treatment of sepsis and acute lung injury.

Wenzhou Medical University
Recent advances of pyrazole-containing derivatives as anti-tubercular agents.

Wuhan University of Science and Technology
GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).

Genentech
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.

Merck
Discovery of potent and selective CDK8 inhibitors through FBDD approach.

Roche Innovation Center Shanghai
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.

Gsk Pharmaceuticals R & D
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor.

Vitae Pharmaceuticals
Novel coumarin- and quinolinone-based polycycles as cell division cycle 25-A and -C phosphatases inhibitors induce proliferation arrest and apoptosis in cancer cells.

Sapienza University of Rome
Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as new potent and selective human sirtuin 2 inhibitors.

Xihua University
TRIAZOLOPYRIMIDINES AS A2A / A2B INHIBITORS

Incyte
DELIVERY OF THERAPEUTIC ALKALOID COMPOUNDS

Sensorium Therapeutics
BICYCLIC PYRIDINE DERIVATIVE

Sumitomo Pharma
FUSED HETEROAROMATIC PYRROLIDINONES

Calithera Biosciences
Substituted pyrazlo[3,4-c]pyridines as selective BTK kinase inhibitors

Jumbo Drug Bank
Azaindole derivatives and their use as ERK kinase inhibitors

Agv Discovery
N-cyano-7-azanorbornane derivatives and uses thereof

Amgen
Substituted imidazolidin-2-one derivatives as PRMT5 inhibitors

Aurigene Discovery Technologies
Cyclic dinucleotides as sting agonists

Janssen Biotech
TEAD inhibitors and uses thereof

Ikena Oncology
Compounds, salts thereof and methods for treatment of diseases

Acadia Pharmaceuticals
Macrocyclic indole derivatives

The Broad Institute
Dual mode of action soluble guanylate cyclase activators and phosphodiesterase inhibitors and uses thereof

Topadur Pharma
Inhibitors of RIP1 kinase and methods of use thereof

Genentech
Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Vanderbilt University
Tricyclic compounds as modulators of TNF-alpha synthesis and as PDE4 inhibitors

Vtv Therapeutics
Inhibitors of RET

Blueprint Medicines
Pyrrolone or pyrrolidinone melanin concentrating hormone receptor-1 antagonists

Bristol-Myers Squibb
Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use

Merck Sharp & Dohme
Depsipeptide and uses thereof

Novobiotic Pharmaceuticals
Crystal structure and pharmacological characterization of a novel N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site.

University of Copenhagen
Inhibitors of bruton's tyrosine kinase

Pharmacyclics
Development of 2-(Substituted Benzylamino)-4-Methyl-1, 3-Thiazole-5-Carboxylic Acid Derivatives as Xanthine Oxidase Inhibitors and Free Radical Scavengers.

Jamia Hamdard
5 oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives as CaMKII kinase inhibitors for treating cardiovascular diseases

Sanofi
Inhibitors of STAT3

University of Central Florida Research Foundation
Pharmacology and functions of metabotropic glutamate receptors.

Emory University
In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist.

Hoechst Marion Roussel
In vivo receptor occupancy of the angiotensin II receptor by nonpeptide antagonists: relationship to in vitro affinities and in vivo pharmacologic potency.

Merck Research Laboratories
The main features of central 5-HT1 receptors.

Sorbonne University
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.

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

Vernalis (R&D)