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Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea

Chinese Academy of Sciences
Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.

East China Normal University
Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selectivea1A-Adrenoceptor Antagonists.

Chengdu University
Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.

Shanghai Institute of Materia Medica
Identification of 3,5,6-substituted indolin-2-one's inhibitors of Aurora B by development of a luminescent kinase assay.

Peking Union Medical College
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.

Zhejiang University
Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor.

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

Zhejiang University
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.

Philipps-Universit£T Marburg
Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors.

Chinese National Center For Drug Screening
Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors.

Zhejiang University
The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.

Novartis Institutes For Biomedical Research
Rediocide A, an Insecticide, induces G-protein-coupled receptor desensitization via activation of conventional protein kinase C.

Chinese Academy of Sciences
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.

Chinese Academy of Sciences
Synthesis and opioid receptor activity of indolopropellanes.

Chinese Academy of Sciences
Asymmetric synthesis and biological evaluation of N-cyclohexyl-4-[1-(2,4-dichlorophenyl)-1-(p-tolyl)methyl]piperazine-1-carboxamide as hCB1 receptor antagonists.

Shanghai Institute of Materia Medica
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.

Chinese Academy of Sciences
Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.

Chinese Academy of Sciences
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.

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

Novartis Institute For Tropical Diseases
A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice.

National Center For Drug Screening
Deuterium Editing of Small Molecules: A Case Study on Antitumor Activity of 1,4-Benzodiazepine-2,5-dione Derivatives.

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

Texas A&M University
Development of de-novo coronavirus 3-chymotrypsin-like protease (3CLpro) inhibitors since COVID-19 outbreak: A strategy to tackle challenges of persistent virus infection.

Shaanxi University of Science & Technology
Discovery of GPR84 Fluorogenic Probes Based on a Novel Antagonist for GPR84 Bioimaging.

Chinese Academy of Sciences
Development of novel hydrazidoarylaminopyrimidine-based BTK/FLT3 dual inhibitors with potent in vivo anti-hematological malignancies effects.

Nantong University
Application of Novel Degraders Employing Autophagy for Expediting Medicinal Research.

Chengdu University of Traditional Chinese Medicine
Design, synthesis, and pharmacological evaluations of pyrrolo[1,2-a]quinoxaline-based derivatives as potent and selective sirt6 activators.

University of Texas Medical Branch
Design, synthesis, and biological evaluation of novel dual inhibitors of heat shock protein 90/mammalian target of rapamycin (Hsp90/mTOR) against bladder cancer cells.

Sichuan University
Discovery of orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid.

Soochow University
Discovery of Novel 5,6-Dihydro-1,2,4-triazine Derivatives as Efficacious Glucagon-Like Peptide-1 Receptor Agonists.

Shanghai Institute of Materia Medica
Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases.

Guangzhou University of Chinese Medicine
Discovery of a novel GPR35 agonist with high and equipotent species potency for oral treatment of IBD.

University of Chinese Academy of Sciences
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.

Novartis Institutes For Biomedical Research
Identification of 1,4-Benzodiazepine-2,5-dione Derivatives as Potential Protein Synthesis Inhibitors with Highly Potent Anticancer Activity.

Tsinghua University
Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects.

Sun Yat-Sen University
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.

Celera Genomics
Novel Sphingosine Kinase 1 Inhibitor Suppresses Growth of Solid Tumor and Inhibits the Lung Metastasis of Triple-Negative Breast Cancer.

China Pharmaceutical University
Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis.

Shanghai Institute of Materia Medica
Structure-Based Design of Tropane Derivatives as a Novel Series of CCR5 Antagonists with Broad-Spectrum Anti-HIV-1 Activities and Improved Oral Bioavailability.

Shanghai Institute of Materia Medica
Multivalent peptide dendrimers inhibit the fusion of viral-cellular membranes and the cellular NF-κB signaling pathway.

The Third Affiliated Hospital of Guangzhou Medical University
Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis.

Chinese Academy of Sciences
Discovery of (

Nanjing University of Chinese Medicine
Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5

Chinese Academy of Sciences
Mangostanin Derivatives as Novel and Orally Active Phosphodiesterase 4 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis with Improved Safety.

Hainan University
Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors.

Nanjing Normal University
Discovery of 1,5-Dihydro-4

Zhejiang University
Modulation of the G-Protein-Coupled Receptor 84 (GPR84) by Agonists and Antagonists.

Chinese Academy of Sciences
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes.

Fudan University
A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.

Shenyang Pharmaceutical University
Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.

East China Normal University
Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.

Cadus Pharmaceutical
Design, synthesis, biological evaluation, and comparative docking study of 1,2,4-triazolones as CB1 receptor selective antagonists.

Zhejiang University
Lipophilic Isosteres of a π-π Stacking Interaction: New Inhibitors of the Bcl-2-Bak Protein-Protein Interaction.

Novartis Institutes For Biomedical Research
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.

Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of ring A modified 11-keto-boswellic acid derivatives as Pin1 inhibitors with remarkable anti-prostate cancer activity.

Shenyang Pharmaceutical University
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.

Chinese Academy of Sciences
Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.

University of Chinese Academy of Sciences
Design and synthesis of aryloxypropanolamine as β

East China Normal University
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrido[4,3-c]azepin-5-one-based novel chemotype CCR2 antagonists via scaffold hopping strategy.

Shanghai Institute of Materia Medica
Developing pyridazine-3-carboxamides to be CB2 agonists: The design, synthesis, structure-activity relationships and docking studies.

Zhejiang University
Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models.

Novartis Institutes For Biomedical Research
Amidoalkylindoles as Potent and Selective Cannabinoid Type 2 Receptor Agonists with in Vivo Efficacy in a Mouse Model of Multiple Sclerosis.

East China Normal University
Development of Quinazoline/Pyrimidine-2,4(1

Zhejiang University
Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth.

The University of Texas At Austin
PYRAZOLEAMIDE DERIVATIVES

Hoffmann-La Roche
Compounds and compositions for the treatment of parasitic diseases

Novartis
Substituted heteroaryls as inhibitors of the BCL6 BTB domain protein-protein interaction

Ontario Institute For Cancer Research (Oicr)
Azaspirocycles as monoacylglycerol lipase modulators

Janssen Pharmaceutica
Ketone inhibitors of lysine gingipain

Cortexyme
Factor XIa inhibitors

Merck Sharp & Dohme
Heterocyclic amide derivatives as P2X7 receptor antagonists

Actelion Pharmaceuticals
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.

Pfizer
Pyrazolopyrimidines Establish MurC as a Vulnerable Target in Pseudomonas aeruginosa and Escherichia coli.

Astrazeneca India
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.

Pfizer
UROKINASE in CSAR_FULL_RELEASE_3JULY2012

Csar
Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles.

Wyeth Research
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.

Bristol-Myers Squibb Pharmaceutical Research Institute
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.

Merck Research Laboratories