Compound Library for Lipid GPCR (EDG) Receptors

EDG-buttonA screening library of >8,000 compounds has been designed in collaboration with Enamine based on available and newly synthesized compounds. These target the family of 8 EDG receptors (S1P1-5 and LPA1-3). The compounds may also be appropriate for screening at GPR3, GPR6 and GPR12 orphan receptors given some TM bundle binding site similarity and/or GPR23, GPR92 and P2Y5 given their more recent classification as additional, albeit distinct, LPA receptors. Compounds targeting the receptors have potential application in inflammation, immune disease, cancer, CNS diseases as well as other indications. The compounds have been selected using a combination of ligand-based methods including chemical fingerprints, 2D pharmacophores and 3D shape/feature matches. They represent a combination of compounds for expanding SAR around known chemotypes and scaffold hops seeking novelty. The current set of compounds covers the non-acidic classes of ligand, with acidic compounds being designed via a different procedure and offered separately.