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Article Title
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Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes.

East China University of Science and Technology
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.

Shanghai Institute of Materia Medica
Discovery of CREBBP Bromodomain Inhibitors by High-Throughput Docking and Hit Optimization Guided by Molecular Dynamics.

University of Z£Rich
Fragment-Based Design of Selective Nanomolar Ligands of the CREBBP Bromodomain.

University of Z£Rich
Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors.

Academy of Military Medical Sciences
Design, synthesis, and biological evaluation of novel matrix metalloproteinase inhibitors as potent antihemorrhagic agents: from hit identification to an optimized lead.

University of Navarra
Design, synthesis, X-ray crystallographic analysis, and biological evaluation of thiazole derivatives as potent and selective inhibitors of human dihydroorotate dehydrogenase.

East China University of Science and Techology
Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors.

TBA
Novel selective and potent inhibitors of malaria parasite dihydroorotate dehydrogenase: discovery and optimization of dihydrothiophenone derivatives.

State Key Laboratory of Bioreactor Engineering
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.

TBA
Discovery of diverse human dihydroorotate dehydrogenase inhibitors as immunosuppressive agents by structure-based virtual screening.

State Key Laboratory of Bioreactor Engineering
The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.

Amgen
[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.

Novartis Institutes For Biomedical Research
C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.

Chinese Academy of Sciences
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.

Novartis Institutes For Biomedical Research
ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.

Chinese Academy of Sciences
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.

Merck Research Laboratories
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

Incyte
Peptide deformylase inhibitors of Mycobacterium tuberculosis: synthesis, structural investigations, and biological results.

Novartis Institute For Tropical Diseases
Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.

University of Oklahoma Health Sciences Center
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

Incyte
Discovery of DNL343: A Potent, Selective, and Brain-Penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative Diseases.

Denali Therapeutics Inc.
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.

Incyte
Glycan-Modified Peptides for Dual Inhibition of Human Immunodeficiency Virus Entry into Dendritic Cells and T Cells.

Chinese Academy of Sciences
Cannabinoid Receptor Type II Ligands from Sandalwood Oil and Synthetic α-Santalol Derivatives.

University of Mississippi
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.

TBA
Bisindole natural products: A vital source for the development of new anticancer drugs.

Hubei University of Science and Technology
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

Incyte
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.

Novartis Institutes For Biomedical Research
Discovery of Potent and Selective Dual Leucine Zipper Kinase/Leucine Zipper-Bearing Kinase Inhibitors with Neuroprotective Properties in In Vitro and In Vivo Models of Amyotrophic Lateral Sclerosis.

Denali Therapeutics
Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer.

Pfizer
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.

Incyte Research Institute
Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.

Rapt Therapeutics
Design, synthesis, and structure-activity relationship of PD-1/PD-L1 inhibitors with a benzo[d]isoxazole scaffold.

Peking Union Medical College
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with

University of Navarra
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

Incyte
Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.

Bristol-Myers Squibb Pharmaceuticals
Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach.

Sun Yat-Sen University
High Selectivity of an α-Conotoxin LvIA Analogue for α3β2 Nicotinic Acetylcholine Receptors Is Mediated by β2 Functionally Important Residues.

Guangxi University
Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.

Wuhan Institute of Technology
Novel N-Substituted oseltamivir derivatives as potent influenza neuraminidase inhibitors: Design, synthesis, biological evaluation, ADME prediction and molecular docking studies.

The Hong Kong Polytechnic University
Anti-oligomerization sheet molecules: Design, synthesis and evaluation of inhibitory activities against α-synuclein aggregation.

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

Zhejiang University
Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.

China Pharmaceutical University
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.

Aarhus University
Structure-activity relationship (SAR) studies of synthetic glycogen synthase kinase-3β inhibitors: A critical review.

Wuhan Institute of Technology
Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.

Shanghai Institute of Materia Medica
Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4'-Ethynyl-2-fluoro-2'-deoxyadenosine).

Idenix An Msd
Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces.

Wuxi Apptec (Tianjin) Co.
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.

University of Chinese Academy of Sciences
Phenotypic Screening To Discover Novel Chemical Series as Efficient Antihemorrhagic Agents.

Universidad De Navarra
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.

Universidad De Oviedo-Principado De Asturias
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.

Xinjiang Technical Institute of Physics and Chemistry
N-(2-(substituted-naphth-1-yl)ethyl) substituted amide compound, preparation and uses thereof

Beijing Greatway Pharmaceutical Technology Co.
SUBSTITUTED S-ALANINATE DERIVATIVES

Bayer Aktiengesellschaft
Amide compounds as kinase inhibitors, compositions and methods of treatment

Translational Drug Development
Triple combination of pure 5-HT6 receptor antagonists, acetylcholinesterase inhibitors and NMDA receptor antagonist

Suven Life Sciences
Quinoline and isoquinoline derivatives for treating pain and pain related conditions

Esteve Pharmaceuticals
Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2-negative allosteric modulators, compositions, and their use

Merck Sharp & Dohme
Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors

Pfizer
Amido spirocyclic amide and sulfonamide derivatives

Forma Tm
Compounds, compositions and methods

Denali Therapeutics
1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins

Incyte
Compounds and methods for inhibiting JAK

Dizal (Jiangsu) Pharmaceutical
Inhibitors of syk and JAK protein kinases

Portola Pharmaceuticals
IBAT inhibitors for the treatment of liver diseases

TBA
Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use

Merck Sharp & Dohme
Pyrrolo[2,3-B]pyrazines as SYK inhibitors

Hoffmann-La Roche
Oxazine derivatives

Shionogi
PIM kinase inhibitors and methods of their use

Novartis
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.

Merck Frosst Canada
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.

Glaxosmithkline