The recently de-orphanized GPCR55 has been established to have a role in inflammatory and neuropathic pain. HTS presented four agonistic hits, from which the most potent and selective one was chosen as a lead. Synthesis of diverse analogues of the lead, which were designed based on a computer model of the target receptor, was done to optimize the potency and selectivity. This is crucial to accurately determine the potency and kinetics of antagonists which potentially have therapeutic applications. 

Synthesis and biological evaluation of GPR55 agonists

245th National Meeting (2013)

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