Novel, Orally Active Bioavailable Inhibitor of VEGFR2 Signaling with Potent Antiangiogenic Activity and Antitumor Efficacy

Novel Inducer of Apoptosis in Human Colorectal Cells via Mitochondrial Apoptosis Pathway, Inhibiting Tumor Growth

Novel non-analogous leukotriene agonist

Selective growth inhibitor of endothelial cells

YM-244769 is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice.

Potent and selective mGLu1 antagonist

Novel AMPA receptor antagonist

Potent and selective microbicidal agent against wild type (wt) HIV-1, NNRTI-, NRTI-, PRI-resistant mutants

Water-soluble analog of YNT-707, acting as a potent orexin 1 receptor (OX1R) antagonist

Novel potent orexin 1 receptor (OX1R) antagonist

DNA-intercalating dye as sensitive amyloid probe

Novel Proteasome Inhibitor, Enhancing Cisplatin Cytotoxicity in Cisplatin-Resistant Human Ovarian Cancer Cells, inducing cell cycle arrest on G2 phase in MCF-7 cells via ERα and PI3K/Akt pathways

Selective A 2A receptor agonist

Novel γ-lactam pyrazolidinone, targeting penicillin-binding proteins (PBPs) and incorporating a siderophore moiety to facilitate uptake into the periplasm, being effective against multidrug-resistant gram-negative Bacilli

Novel inhibitor of Wnt signaling by stabilizing Axin-1, a scaffolding protein that regulates proteasome degradation of β-catenin

Novel YycG inhibitor, inhibiting planktonic cells of E. faecalis, including the vancomycin- or linezolid-resistant strains

Novel YycG inhibitor, significantly inhibited biofilm formation in static and dynamic conditions

Novel activator of JNK, binding directly to microtubules, inducing ERK-mediated mitotic arrest and subsequent apoptosis

Novel first-in-class inhibitor of BRD4 and EGFR kinase

Novel potent ligand of σ2 receptor (K i =7nM)

Novel riboswitch activator, binding ZTP riboswitches, and activating transcription more strongly than ZMP in vitro

Novel potent dual σ1/2 ligand (σ1 K i =5nM, σ2 K i =3nM), showing anti-allodynic in a model of neuropathic pain