PMID
Data
Article Title
Organization
Design, synthesis and bioactivity of novel phthalimide derivatives as acetylcholinesterase inhibitors.

Chinese Academy of Agricultural Sciences
Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent ROR¿t inverse agonists.

Fudan University
Design, synthesis and structure-activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors.

Shenyang Pharmaceutical University
Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

TBA
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.

Synaptic Pharmaceutical
Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

TBA
Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.

Pfizer
Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

TBA
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.

Incyte
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

Incyte
Discovery of Benzo[d]oxazoles as Novel Dual Small-Molecule Inhibitors Targeting PD-1/PD-L1 and VISTA Pathway.

China Pharmaceutical University
Design, synthesis and biological evaluation of novel SIRT3 inhibitors targeting both NAD+ and substrate binding sites for the treatment of acute myeloid leukemia.

Shihezi University
Molecular understanding of the therapeutic potential of melanin inhibiting natural products.

Tianjin University
Discovery of Oxidized p-Terphenyls as Phosphodiesterase 4 Inhibitors from Marine-Derived Fungi.

Chinese Academy of Sciences
Rising Star in Immunotherapy: Development and Therapeutic Potential of Small-Molecule Inhibitors Targeting Casitas B Cell Lymphoma-b (Cbl-b).

China Pharmaceutical University
Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia.

China Pharmaceutical University
Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia.

Chinese Academy of Medical Sciences & Peking Union Medical College
Cyclic Peptide Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury.

Fujian University of Traditional Chinese Medicine
Design, Synthesis, and Bioevaluation of Novel Reversibly Photoswitchable PI3K Inhibitors Based on Phenylazopyridine Derivatives toward Light-Controlled Cancer Treatment.

Chinese Academy of Medical Sciences and Peking Union Medical College
Recent advances of targeting nicotinamide phosphoribosyltransferase (NAMPT) for cancer drug discovery.

China Pharmaceutical University
Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor.

Nankai University
Beyond inhibition against the PD-1/PD-L1 pathway: development of PD-L1 inhibitors targeting internalization and degradation of PD-L1.

China Pharmaceutical University
Design, synthesis, biological evaluation of urea substituted 1,2,5-oxadiazole-3-carboximidamides as novel indoleamine 2,3-dioxygenase-1 (IDO1) inhibitors.

China Pharmaceutical University
Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors.

China Pharmaceutical University
Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.

Sichuan University
Discovery of Novel PD-L1 Inhibitors That Induce the Dimerization, Internalization, and Degradation of PD-L1 Based on the Fragment Coupling Strategy.

China Pharmaceutical University
Design, synthesis, and evaluation of PD-1/PD-L1 small-molecule inhibitors bearing a rigid indane scaffold.

China Pharmaceutical University
Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release.

Chinese Academy of Medical Sciences and Peking Union Medical College
Structure-Activity Relationship Study of 1

University of Chinese Academy of Sciences
Antibacterial activities of anthraquinones: structure-activity relationships and action mechanisms.

Shanghai Veterinary Research Institute
Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis.

China Pharmaceutical University
Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells.

Nankai University
Discovery of Novel 1,3-Diphenylpyrazine Derivatives as Potent S-Phase Kinase-Associated Protein 2 (Skp2) Inhibitors for the Treatment of Cancer.

Zhengzhou University
Discovery of quinazolin-4-one-based non-covalent inhibitors targeting the severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2 M

China Pharmaceutical University
Synthesis and anticancer activity of novel histone deacetylase inhibitors that inhibit autophagy and induce apoptosis.

Wuyi University
Design and discovery of new selective and potent VEGF receptor 2 tyrosine kinase inhibitors.

Nankai University
Novel Benzimidazoles as Potent Small-Molecule Inhibitors and Degraders of V-Domain Ig Suppressor of T-Cell Activation (VISTA).

China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of Bipyridazine Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.

Fudan University
Dual Nicotinamide Phosphoribosyltransferase (NAMPT) and Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors for the Treatment of Drug-Resistant Nonsmall-Cell Lung Cancer.

China Pharmaceutical University
Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach.

Incyte
Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.

Nankai University
Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

Incyte Research Institute
Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors.

Incyte Research Institute
Discovery of Small Molecules Simultaneously Targeting NAD(P)H:Quinone Oxidoreductase 1 and Nicotinamide Phosphoribosyltransferase: Treatment of Drug-Resistant Non-small-Cell Lung Cancer.

China Pharmaceutical University
Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site.

Peking Union Medical College
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-

Astrazeneca
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.

Peking Union Medical College
Diastereomeric Resolution Yields Highly Potent Inhibitor of SARS-CoV-2 Main Protease.

Bio-Techne (Tocris)
Development of Inhibitors Targeting the V-Domain Ig Suppressor of T Cell Activation Signal Pathway.

China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment.

TBA
Design, Synthesis, and Evaluation of PD-1/PD-L1 Antagonists Bearing a Benzamide Scaffold.

China Pharmaceutical University
Novel Biphenyl Pyridines as Potent Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction.

China Pharmaceutical University
Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy.

Peking Union Medical College
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).

China Pharmaceutical University
Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer.

China Pharmaceutical University
Discovery of a novel small-molecule inhibitor of Fam20C that induces apoptosis and inhibits migration in triple negative breast cancer.

Southwest Jiaotong University
Discovery of 1,3,4-oxadiazole derivatives as potential antitumor agents inhibiting the programmed cell death-1/programmed cell death-ligand 1 interaction.

China Pharmaceutical University
Synthesis, bioconversion, pharmacokinetic and pharmacodynamic evaluation of N-isopropyl-oxy-carbonyloxymethyl prodrugs of CZh-226, a potent and selective PAK4 inhibitor.

Shenyang Pharmaceutical University
Isoquinolinone derivatives as potent CNS multi-receptor D

Jiangsu Ocean University
Discovery of pyrazole derivatives as cellular active inhibitors of histone lysine specific demethylase 5B (KDM5B/JARID1B).

Zhengzhou University
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors.

Peking Union Medical College
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.

Synaptic Pharmaceutical
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).

Incyte
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.

Synaptic Pharmaceutical
Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer.

Chinese Academy of Sciences
Targeting dihydrofolate reductase: Design, synthesis and biological evaluation of novel 6-substituted pyrrolo[2,3-d]pyrimidines as nonclassical antifolates and as potential antitumor agents.

Hebei Medical University
Modulating Heparanase Activity: Tuning Sulfation Pattern and Glycosidic Linkage of Oligosaccharides.

Wayne State University
Development of Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Signaling Pathway.

China Pharmaceutical University
Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis.

TBA
Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.

Wuyi University
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.

TBA
Design, synthesis and biological evaluation of 6-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of TS and AICARFTase and as potential antitumor agents.

Hebei Medical University
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.

Peking Union Medical College
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.

Peking Union Medical College
NAD(P)H:Quinone Oxidoreductase 1 (NQO1) as a Therapeutic and Diagnostic Target in Cancer.

China Pharmaceutical University
Novel 6-substituted benzoyl and non-benzoyl straight chain pyrrolo[2,3-d]pyrimidines as potential antitumor agents with multitargeted inhibition of TS, GARFTase and AICARFTase.

Hebei Medical University
Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells.

Shihezi University
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.

The University of Texas M.D. Anderson Cancer Center
ULK1 AND ULK2 INHIBITORS

Michigan State University
SUBSTITUTED HYDANTOIN COMPOUNDS, METHODS FOR PREPARATION THEREOF AND USE THEREOF IN THE TREATMENT AND/OR PREVENTION OF A CORONA VIRUS DISEASE

Individual
Cyclin dependent kinase inhibitors

Pfizer
Fused pyrimidine derivatives as A2A / A2B inhibitors

Incyte
Compounds as neurokinin-1 receptor antagonists and uses thereof

Xwpharma
Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of ASGPR

Pfizer
Cyclopropylamines as LSD1 inhibitors

Incyte
Covalent small molecule DCN1 inhibitors and therapeutic methods using the same

University of Michigan
Heterocycle-substituted pyridyl benzothiophenes as kinase inhibitors

Allergan
Diamide compounds having muscarinic receptor antagonist and BETA2 adrenergic receptor agonist activity

Theravance Respiratory
Thyroid hormone analogs

Hoffmann-La Roche
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.

University of Toronto