The ChEMBL-og

ATC Code: A08A (incomplete) Wikipedia: Lorcaserin On June 27 th , the FDA approved Lorcaserin hydrochloride (Tradename: Belviq TM ; Research Code: APD-356), a selective serotonin 2C receptor  (5HT2c) agonist, for chronic weight management in adults with an initial body mass index ( BMI ) equal or higher than 30 kg/m 2 (obese), or equal or higher than 27 kg/m 2 (overweight) and with one weight-associated comorbid condition (e.g. hypertension , dyslipidemia , type 2 diabetes ). Lorcaserin is believed to decrease food consumption and promote satiety by selectively activating 5-HT 2C receptors on anorexigenic pro-opiomelanocortin neurones in the hypothalamus. The exact mechanism of action is not fully established. However, at therapeutic concentrations, lorcaserin is selective for 5-HT 2C receptors as compared to 5-HT 2B receptors, making it less prone to cardiovascular side-effects, associated with previous 5-HT 2C  weight management drugs. It is the f...

We are pleased to announce the release of GPCR SARfari . GPCR SARfari is a web based workbench focused on Class A G Protein-Coupled Receptors (Rhodopsin-like). The system currently contains: 912 protein sequences 546,467 bioactivity data points 118,834 compounds The bioactivty and compound data stored in GPCR SARfari has been taken from the latest release of the ChEMBL database. You can query this data directly via the interface, or download it from the links provided on this page . We have been collecting the protein structures of rhodopsin-like GPCRs and plan to add a structural component to GPCR SARfari. There will be a blog announcement providing more detail about this soon. The system is very similar to Kinase SARfari , so if you are familiar with the kinase version, you should have no problems navigating around GPCR SARfari. If there is enough interest we will also be happy to set up a webinar describing how to use both systems, please mail us in this is something ...