RV521 is an orally bioactive, highly potent small-molecule inhibitor of RSV (respiratory syncytial virus) fusion protein. It is with promising pharmaceutical properties and is currently in clinical development for the treatment of RSV disease in paedriatrics, the elderly and immune-compromised patients. RV521 targets (RSV) fusion which is a surface protein that mediates RSV binding to […]

Tautomycin is naturally occurring antifungal antibiotic found in shellfish and is produced by the bacterium Streptomyces spiroverticillatus. It is a polyketide-based structure characterized by a three hydroxyl groups, two ketones, a dialkylmaleic anhydride, an ester linkage (connecting anhydride unit to polyketide chain), a spiroketal and one methyl ether among others. Tautomycin is an antifungal antibiotic […]

Calyculin A is a novel, potent, selective and cell-permeable inhibitor of protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) with IC50s of 0.5 to 1 nM. Calyculin A is a natural product and a marine toxin isolated from Disodermia calyx. Calyculin A does not have significant effect against PP2B, PP2C, and PP4.2 Through its […]

Fosnetupitant (07PNET; 07-PNET; Fosnetupitant chloride; Akynzeo), the prodrug of netupitant, is a novel and potent antagonist of neurokinin receptor used in combination with palonosetron to prevent nausea and vomiting caused by chemotherapy. Neurokinin 1 (NK1) receptor antagonists are a class of drug used to treat nausea and vomiting associated with chemotherapy. Aprepitant, casopitant, and fosaprepitant […]

Epelsiban (also known as GSK557296; GSK-557296) is a novel, potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor. It was initially developed by GSK for the treatment of premature ejaculation in men and then as an agent to enhance embryo or blastocyst implantation in women undergoing embryo […]

ABT-639 hydrochloride (HCl) is a new potent, peripherally acting, selective T-type Ca2+ channel blocker that blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50=2 μM) and attenuates low voltage-activated (LVA) currents in rat DRG neurons (IC50=8 μM). ABT-639 is significantly less active at other Ca2+ channels (e.g. Cav1.2 and Cav2.2) (IC50>30 mM). […]

RO-7 is a novel, potent and next-generation PA (polymerase) endonuclease inhibitor of influenza A and B viruses, but its drug resistance potential is unknown. The effectiveness of antiviral drugs can be severely compromised by the emergence of resistant viruses. Therefore, determination of the mechanisms by which viruses become resistant is critical for drug development and […]

RO 4938581 (also known as Ro 4882224) is a novel, potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction. RO4938581 displays strong CYP1A2 […]

RV521 Hcl is an orally bioactive, highly potent small-molecule inhibitor of RSV (respiratory syncytial virus) fusion protein. It is with promising pharmaceutical properties and is currently in clinical development for the treatment of RSV disease in paedriatrics, the elderly and immune-compromised patients. RV521 targets (RSV) fusion which is a surface protein that mediates RSV binding […]

Epetraborole R-Mandelate (also known as GSK2251052 and AN3365) is a novel, potent and selective leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase. Epetraborole was under investigation for the treatment of infections caused by multidrug-resistant Gram-negative pathogens. GSK2251052 is a novel boron-containing antibiotic that inhibits […]