MS48107 is a Selective GPR68 PAM
G protein-coupled receptor 68 (GPR68) is originally discovered as a clinically related receptor in an ovarian cancer cell line. GPR68 widely expresses in most cells and tissues, including the spleen,…
HS271 is a Highly Potent, Orally Active and Selective IRAK4 Inhibitor
IRAK-4 (interleukin-1 receptor-associated kinase 4) is a protein kinase involved in signal transduction of innate immune response from toll-like receptors. Specifically, it also supports signal transduction from T cell receptors.…
AE-3763 is a Peptide-Based Human Neutrophil Elastase Inhibitor
Neutrophil elastase (HNE) is a serine protease, similar to chymotrypsin, and has a wide range of substrate specificity. Specifically, secreted by neutrophils and macrophages during inflammation, it destroys bacteria and…
Cobicistat is a Selective CYP3A Inhibitor and a Pharmacokinetic Enhancer of HIV Inhibitors
The highly active antiretroviral therapy (HAART) can transform the human immunodeficiency virus (HIV) infection into a manageable chronic disease in a little over a decade. The combination of antiretroviral drugs…
MR-L2 is a Reversible and Noncompetitive Allosteric Activator of Long-Isoform PDE4
Cyclic AMP (cAMP) is a universal second messenger in cells of all biological systems. Specifically, cAMP homeostasis is affected by synthesis, interaction, and degradation, and is realized by the multigene…
CB-5083 is a Selective and Orally Bioavailable p97 Inhibitor
The AAA+ ATPase p97 is essential to a wide range of cellular functions. The p97 acts downstream from ubiquitin signaling events and utilizes the energy from ATP hydrolysis to extract…
RRD-251 is an Inhibitor of Rb-Raf-1 Interaction
Retinoblastoma protein (Rb), a tumor suppressor protein, is dysfunctional in several major cancers. Specifically, one of the functions of Rb is to prevent excessive cell growth by inhibiting cell cycle…
GR 125743 is a Selective 5-HT1B/1D Receptor Antagonist
The negative feedback system regulates the 5-Hydroxytryptamine 5-HT release. Besides, the negative feedback system is mediated by autoreceptors located on neuronal terminals and cell bodies. The terminal autoreceptor in the…