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Discovery of furan carboxylate derivatives as novel inhibitors of ATP-citrate lyase via virtual high-throughput screening.

Harvard Medical School
Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase.

Harvard Medical School
Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome.

National Institute of Biological Sciences
An adjustable release rate linking strategy for cytotoxin-peptide conjugates.

Tulane University Health Sciences Center
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.

Bristol-Myers Squibb Research and Development
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.

Pharmaron-Beijing
Discovery of mixed type thymidine phosphorylase inhibitors endowed with antiangiogenic properties: synthesis, pharmacological evaluation and molecular docking study of 2-thioxo-pyrazolo[1,5-a][1,3,5]triazin-4-ones. Part II.

National University of Singapore
Fragment-based approach to the design of 5-chlorouracil-linked-pyrazolo[1,5-a][1,3,5]triazines as thymidine phosphorylase inhibitors.

National University of Singapore
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).

Bristol-Myers Squibb
A structure-activity relationship study of 1,2,4-triazolo[1,5-a][1,3,5]triazin-5,7-dione and its 5-thioxo analogues on anti-thymidine phosphorylase and associated anti-angiogenic activities.

National University of Singapore
Synthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase.

National University of Singapore
Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.

Bristol-Myers Squibb R & D
Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents.

Institute of Pharmaceutical Industry
7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.

Bristol-Myers Squibb Research and Development
Aminofurazans as potent inhibitors of AKT kinase.

Glaxosmithkline
Pyrazolone based TGFbetaR1 kinase inhibitors.

Biogen Idec
Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives.

The Chinese Academy of Sciences
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.

Glaxosmithkline
Dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)).

Bristol-Myers Squibb
Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.

New York University Medical Center
Recent advances in targeting histone H3 lysine 36 methyltransferases for cancer therapy.

China Pharmaceutical University
Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease.

Texas A&M University
Development of potent and selective ULK1/2 inhibitors based on 7-azaindole scaffold with favorable in vivo properties.

H. Lee Moffitt Cancer Center and Research Institute
Medicinal chemistry strategies targeting NLRP3 inflammasome pathway: A recent update from 2019 to mid-2023.

Shenyang Pharmaceutical University
Scaffold hopping derived novel benzoxazepinone receptor-interacting protein kinase 1 (RIP1) inhibitors as anti-necroptosis agents: Anti-inflammatory effect in systemic inflammatory response syndrome (SIRS) and epilepsy.

Ningxia Medical University
Screening through Lead Optimization of High Affinity, Allosteric Cyclin-Dependent Kinase 2 (CDK2) Inhibitors as Male Contraceptives That Reduce Sperm Counts in Mice.

University of Minnesota
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.

Wyeth Research
Design, synthesis, and biological evaluation of deuterated indolepropionic acid derivatives as novel long-acting pan PPARα/γ/δ agonists.

Guangdong Pharmaceutical University
Design and development of a novel series of oral bivalent BET inhibitors with potent anticancer activities.

Shanghai University
Discovery, Crystallographic Studies, and Mechanistic Investigations of Novel Phenylalanine Derivatives Bearing a Quinazolin-4-one Scaffold as Potent HIV Capsid Modulators.

Shandong University
Discovery of an Anti-TNF-α 9-mer Peptide from a T7 Phage Display Library for the Treatment of Inflammatory Bowel Disease.

Tongji University
Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators.

Shandong University
Identification of potent and selective TACE inhibitors via the S1 pocket.

Wyeth Research
Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors.

Wyeth Research
Design, Synthesis, and Structure-Activity Relationship Studies of Bisamide Derivatives of Amphotericin B with Potent Efficacy and Low Toxicity.

Shanghai Institute of Materia Medica
Indolylarylsulfones bearing phenylboronic acid and phenylboronate ester functionalities as potent HIV‑1 non-nucleoside reverse transcriptase inhibitors.

Shandong University
Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.

Shandong University
Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.

Shandong University
Structural and PK-guided identification of indole-based non-acidic autotaxin (ATX) inhibitors exhibiting high in vivo anti-fibrosis efficacy in rodent model.

Shenyang Pharmaceutical University
Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.

Shandong University
An insight on medicinal aspects of novel HIV-1 capsid protein inhibitors.

Shandong University
Synthesis and structural characterization of a monocarboxylic inhibitor for GRB2 SH2 domain.

H. Lee Moffitt Cancer Center and Research Institute
Neuroactive Type-A γ-Aminobutyric Acid Receptor Allosteric Modulator Steroids from the Hypobranchial Gland of Marine Mollusk,

University of Utah
Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.

Shandong University
2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.

Shandong University
Discovery of Potent Selective Nonzinc Binding Autotaxin Inhibitor BIO-32546.

Biogen
Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.

Shandong University
Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.

Shandong University
Hepatoselective Dihydroquinolizinone Bis-acids for HBsAg mRNA Degradation.

Baruch S. Blumberg Institute
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.

Chinese Academy of Sciences
Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.

Chinese Academy of Sciences
Novel lipid side chain modified exenatide analogs emerged prolonged glucoregulatory activity and potential body weight management properties.

China Pharmaceutical University
Design, synthesis and biological evaluation of 3-hydroxyquinazoline-2,4(1H,3H)-diones as dual inhibitors of HIV-1 reverse transcriptase-associated RNase H and integrase.

Shandong University
Design, synthesis and biological evaluation of "Multi-Site"-binding influenza virus neuraminidase inhibitors.

Shandong University
Discovery of Selective Small Molecule Degraders of BRAF-V600E.

Cullgen
Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.

Yanbian University College of Pharmacy
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.

Shandong University
Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases.

Sugen
Chemical synthesis, microbial transformation and biological evaluation of tetrahydroprotoberberines as dopamine D1/D2 receptor ligands.

Huzhou University
Scaffold Simplification Strategy Leads to a Novel Generation of Dual Human Immunodeficiency Virus and Enterovirus-A71 Entry Inhibitors.

Instituto De Qu£Mica M£Dica (Iqm-Csic)
Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors.

Yanbian University
Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice.

Peking University
Antitumor Activity of Lankacidin Group Antibiotics Is Due to Microtubule Stabilization via a Paclitaxel-like Mechanism.

University of Alberta
Design, synthesis, and biological activity of novel dicoumarol glucagon-like peptide 1 conjugates.

China Pharmaceutical University
Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic agents.

University of North Carolina
Synthesis and biological evaluation of NH

Shenyang Pharmaceutical University
Novel fatty acid chain modified GLP-1 derivatives with prolonged in vivo glucose-lowering ability and balanced glucoregulatory activity.

China Pharmaceutical University
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.

China Pharmaceutical University
5-Hydroxypyrido[2,3-b]pyrazin-6(5H)-one derivatives as novel dual inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H and integrase.

Shandong University
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.

Shandong University
A novel glucagon-like peptide-1/glucagon receptor dual agonist exhibits weight-lowering and diabetes-protective effects.

China Pharmaceutical University
Design, synthesis and pharmacological evaluation of 4,5-diarylisoxazols bearing amino acid residues within the 3-amido motif as potent heat shock protein 90 (Hsp90) inhibitors.

China Pharmaceutical University
Phosphonate linkers and their use to facilitate cellular retention of compounds

Merck Sharp & Dohme
Heteroaryl compounds as 5-HT4 receptor ligands

Suven Life Sciences
Amidoethyl azole orexin receptor antagonists

Merck Sharp & Dohme
Sulfonamide retinoic acid receptor-related orphan receptor modulators and uses thereof

Innov17
P2X7 modulators

Janssen Pharmaceutica
Cyclopropanamine compound and use thereof

Takeda Pharmaceutical
Enhancer of zeste homolog 2 inhibitors

Glaxosmithkline
Synthesis and characterization of phenolic Mannich bases and effects of these compounds on human carbonic anhydrase isozymes I and II.

Dumlupinar University
Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.

Universit�� Lille Nord De France
Buprenorphine analogs

Purdue Pharma
HIV protease inhibitors

Merck Canada
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.

Albany Medical College
Targeting NAD biosynthesis in bacterial pathogens: Structure-based development of inhibitors of nicotinate mononucleotide adenylyltransferase NadD.

Burnham Institute For Medical Research
Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors.

Dupont Pharmaceuticals
Tetracyclic 4-oxo-pyridine-3-carboxylic acid derivatives for the treatment and prophylaxis of hepatitis B virus infection

Hoffmann-La Roche