Novel highly potent FAK-targeting PROTAC degrader, showing a rapid and reversible FAK degradation

Novel blocker of focal adhesion kinase (FAK) autophosphorylation

Novel inhibitor of fungal fatty acid biosynthesis, demonstrating broad-spectrum activity against Candida auris and mucormycetes and retained the activity against azole-resistant candida isolates

Novel folate-appended 2-hydroxypropyl-ß-cyclodextrin (HP-ß-CyD), showing strong anti-leukemia and cell-binding activities, inhibiting the growth of FR-expressing cells, enterjng CML cells through endocytosis and inducing both apoptosis and autophagy via m

Novel Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging, exhibited strong cytotoxicity against FR-overexpressing SK-Hep-1, HeLa, and Siha cells, with IC50 values of 2-3 μM, but had no effe

Novel antileukaemic alkaloid; Inhibitor of reverse transcriptase activity of RNA-tumor viruses; Inhibitor of topoisomerase I

Novel factor VIIa inhibitor

Novel factor VIIa inhibitor

Novel dual inhibitor of fatty acid binding protein 4 (FABP4) and fatty acid binding protein 5 (FABP5)

Novel dual inhibitor of fatty acid binding protein 4 (FABP4) and fatty acid binding protein 5 (FABP5)

Novel FABP4/5 inhibitor, inhibiting lipolysis in 3T3-L1 adipocytes and in primary human adipocytes, reducing plasma triglyceride and free fatty acid levels, ameliorating dyslipidemia but not insulin resistance in mice with diet-induced obesity

Novel inhibitor of β-ketoacyl-(acyl-carrier-protein) synthase III (FabH).

Novel FabH Inhibitor, showing potent antibacterial activity with a MIC value of 3.89–7.81 μM−1 against the tested bacterial strains and exhibiting potent E. coli FabH inhibitory activity with an IC 50 value of 1.6 μM

Novel clickable fumarate-competitive chemoproteomic probe

Novel pyrimidine synthesis inhibitor, exhibiting low micromolar antiviral activity against various influenza A and B virus strains, including the highly pathogenic influenza A strains H5N1 and H7N9, enterovirus A71, respiratory syncytial virus, human rhin

Novel matrix metalloproteinase inhibitor, reducing secretion of very low density lipoprotein-triacylglycerol, lowering TAG levels in serum and the liver, VLDL-TAG secretion, de novo FA synthesis in the liver, and serum levels of insulin and glucose

Novel and potent inhibitor of PCAF catalytic domain

Selective, potent inhibitor of the late current mediated by the cardiac isoform of the sodium channel (NaV1.5)

Novel bactericidal, killing Mycobacterium tuberculosis by targeting iron-sulfur protein Rv0338c (IspQ), a putative redox sensor

Novel bactericidal, killing Mycobacterium tuberculosis by targeting iron-sulfur protein Rv0338c (IspQ), a putative redox sensor

Novel potent and selective MAP4K4 inhibitor

Novel antifungal agent against Candida albicans persister cells

Novel influenza A hemagglutinin (HA) fusion inhibitor (EC 50 = 1.9 ± 0.3 μM), preventing HA from transitioning to the postfusion state at pH 5.0

Polyethylene glycol conjugate of SN38, acting as a topoisomerase I inhibitor,, exerting significant anti-leukaemia activity, overcoming ABCG2-mediated topotecan resistance

Novel potent MCT1 inhibitor, exhibiting good single agent anticancer efficacy properties

Novel Dual-Analyte Fluorescent Chemosensor for Visualizing Neurotransmitter Exocytosis

Topoisomerase I inhibitor

Potent and selective SIRT1 inhibitor

Novel glucagon-like peptide 1 (GLP-1) receptor agonist, displaying significantly elongated half-lives and improved long-acting antidiabetic activity in the presence of endogenous anti-DNP antibodies

Novel ALK5 inhibitor