Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865) was written by Owen, Robert M.;Blakemore, David;Cao, Lishuang;Flanagan, Neil;Fish, Rebecca;Gibson, Karl R.;Gurrell, Rachel;Huh, Chan Woo;Kammonen, Juha;Mortimer-Cassen, Elisabeth;Nickolls, Sarah A.;Omoto, Kiyoyuki;Owen, Dafydd;Pike, Andy;Pryde, David C.;Reynolds, David S.;Roeloffs, Rosemarie;Rose, Colin;Stead, Clara;Takeuchi, Mifune;Warmus, Joseph S.;Watson, Christine. And the article was included in Journal of Medicinal Chemistry in 2019.Recommanded Product: 3939-12-6 This article mentions the following:
The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective pos. allosteric modulators (PAMs) for the GABAA ligand-gated ion channel are described. From a set of initial hits multiple subseries were designed and evaluated based on binding affinity and functional activity. As designing in the desired level of functional selectivity proved difficult, a probability-based assessment was performed to focus the project’s efforts on a single subseries that had the greatest odds of delivering the target profile. These efforts ultimately led to the identification of two precandidates from this subseries, which were advanced to preclin. safety studies and subsequently to the identification of the clin. candidate PF-06372865. In the experiment, the researchers used many compounds, for example, 6-Fluoronicotinonitrile (cas: 3939-12-6Recommanded Product: 3939-12-6).
6-Fluoronicotinonitrile (cas: 3939-12-6) belongs to pyridine derivatives. Pyridine is diamagnetic and has a diamagnetic susceptibility of â?8.7 à 10â? cm3·molâ?.The molecular electric dipole moment is 2.2 debyes. The standard enthalpy of formation is 100.2 kJ·molâ? in the liquid phase and 140.4 kJ·molâ? in the gas phase. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Recommanded Product: 3939-12-6