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

Novel highly potent and orally bioavailable Axl inhibitor

Novel potent dual ERK5 and BRD4 inhibitor

Novel potent and selective ERK5 inhibitor

Novel dual ERK5 and BRD4 inhibitor

Highly specific JNK inhibitor #212121; font-style: normal; font-variant-ligatures: normal; font-variant-caps: normal; font-weight: 400; letter-spacing: normal; text-align: start; text-indent: 0px; text-transform: none; white-space: normal; word-spacing: 0

Zn -dependent inhibitor of human plasma Lp-PLA2

Novel potent dual inhibitor of Ax1 and Mer

Novel specific inhibitor of HIV-1 entry through interaction with the Env spike by virtue of the incorporation of a guandinium group