Salmeterol (AHR-3929; GR33343X; AHR3929; GR-33343G; Salmetedur, Serevent) is a potent and long-acting β2-adrenergic receptor agonist with anti-inflammatory effects (Ki of 1.5 nM for WT β2AR). It has been approved for use in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms. These symptoms include shortness of breath, wheezing, coughing and chest tightness. […]

GSK598809 is a novel, potent and selective dopamine D3 Receptor (DRD3) antagonist with a pKi of 8.9. GSK598809 is currently in Phase I trials. GSK-598809 may decrease the rewarding effects of contextual cues associated with drug intake preclinically, which may reduce drug craving in humans. GSK598809 has been proposed as a medication to treat cocaine […]

GSK-J2 is the isomer of GSK-J1 without any specific activity. GSKJ1 (GSK-J1) is a novel, highly selective and potent inhibitor of histone demethylase H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A. It that has significant activity (IC50 60 nM for human JmjD3) in vitro and in cell assays using an ester prodrug derivative (GSK-J4: 1 µM < IC50 < […]

Fabomotizole (also known as CM346; CM-346; Fabomotizole; trade name: Afobazole) is a novel and selective anxiolytic drug that produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. It was launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of […]

GSK 525768A is the inactive enantiomer of GSK525762A, and has no activity towards BET. Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant acetylation levels have been linked to the development of several diseases. Acetyl-lysine modifications create docking sites for bromodomains, which are small interaction modules found on diverse proteins, some of which […]

GSK2838232, a betulin derivative, is a novel and potent inhibitor of human immune virus (HIV) maturation that is being developed for the treatment of chronic HIV infection. Human immunodeficiency virus type 1 (HIV-1 ) leads to the contraction of acquired immune deficiency disease (AIDS). The number of cases of HIV continues to rise, and currently […]

TPT-260 (also known as TPU260 and R55) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, it is temporally called as TPT-260. TPT260 acts as a chaperone to stabilize the retromer complex against thermal denaturation (Kd = ~ 5 µM). In cultured hippocampal neurons, TPT-260 […]

GSK2807 (GSK-2807) is a novel, potent, selective and SAM-competitive inhibitor of SMYD3 (SET And MYND Domain Containing 3) with anticancer activity. It inhibits SMYD3 with a Ki of 14 nM. SMYD3 is a lysine methyltransferase overexpressed in many cancers such as colorectal, breast, prostate, and hepatocellular tumors, and has been implicated as an oncogene in […]

Eleclazine (also known as GS-6615) is a novel late Na+ current inhibitor with IC50 value of 0.7 uM. Enhanced late Na+ current (late INa ) in the myocardium is pro-arrhythmic. Inhibition of this current is a promising strategy to stabilize ventricular repolarization and suppress arrhythmias. Eleclazine was a selective inhibitor of late INa , stabilizes […]

CID797718 is novel potent and selective PKD (Protein kinase D) inhibitor. Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to […]