Potent, second-generation, selective histamine-H1-receptor antagonist and mast cell stabilizer

Potent and selective ATP-competitive Dyrk1B kinase inhibitor

Antimicrobials, active against methicillin resistant S. aureus (MRSA)

Novel potent smoothened inhibitor, demonstrating in vivo activity in abrogating the Hh paracrine pathway as well as anti- tumor effects

Novel, potent and selective inhibitor of p38α MAP kinase

Novel selective inhibitor of 5-Lipoxygenase Activating Protein (FLAP) for the treatment of inflammatory diseases

Novel Fibrinolysis Inhibitor, Acting via Interference of a Protein-Protein Interaction

Glucokinase activator, decreasing fasting and postprandial glucose in type 2 diabetes mellitus patients

First-in-class selective, partial CDK2 degrader against hearing loss and cancer, protecting against cisplatin ototoxicity and kainic acid excitotoxicity

Novel potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis

Novel peroxisome proliferator-activated receptor alpha (PPARalpha) agonist, inducing alanine aminotransferase-1 gene and protein expression in human, but not in rat hepatocytes

Novel transient receptor potential vanilloid 1 (TRPV1) antagonist

Selective alpha7 nicotinic receptor activator

Novel CXCR2 antagonist with 200 times improvement in solubility than AZD8309

Novel selective GABA-C antagonist

Inhibitor of hepatic cholesterol biosynthesis, inhibiting the cytochrome P450 enzyme lanosterol 14alpha-demethylase

Inducer of Death Receptors and Sensitizer of Human Cancer Cells to TRAIL through a p53-Independent Mechanism

Near-IR probe for detecting conformational changes of Aβ1-42 soluble oligomers in vitro

Novel selective Cdc42 inhibitor, suppressing primary colon cancer growth and prolonging survival in a preclinical mouse xenograft model by downregulation of PAK1 activity

Novel weak PAR2 antagonist

Novel covalent ERK1/2 inhibitor

Novel tankyrase inhibitor, enhancing irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance

Novel potent EphB4 inhibitor

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Novel orally bioavailable inhibitor of Hedgehog signaling

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Second Generation

Cyclooxygenase Inhibitor;

Novel integrin-binding peptide, inhibiting hepatocyte growth factor (HGF) signaling through Met-integrin interactions, also being an antiangiogenic agent by reducing phosphorylation of VEGR2, IGFR, and PDGFR, stabilizing vessels by disrupting α5β1 signali