Immunophage Biomedical Co. Ltd. has divulged G-protein coupled receptor 183 (GPR183; EBI2) antagonists reported to be useful for the treatment of autoimmune disease, cancer, liver diseases, osteoporosis and neuropathic pain.
Scientists from Shanghai Jiao Tong University and affiliated organizations have discovered novel GPR183 antagonists as potential therapeutic candidates for the treatment of inflammatory bowel disease (IBD). With the aim of improving the pharmacokinetic (PK) and safety profile of previously reported oxysterol receptor GPR183 antagonists, structural optimization of the reference antagonist NIBR-189 was conducted.
Synthesis and optimization of several series of G-protein coupled receptor 183 (GPR183) antagonists at Immunophage Biomedical Co. Ltd. led to the discovery of a lead candidate with promising potency (IC50=31.3 nM), reduced hERG inhibition and improved aqueous solubility.
Immunophage Biomedical Co. Ltd. have prepared and tested G-protein coupled receptor 183 (GPR183; EBI2) antagonists that are reported to be useful for the treatment of autoimmune disease, cancer, liver diseases, osteoporosis and neuropathic pain.
