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This research reviews on our ongoing investigation on hybridthird EM-2 analogues, in which the wonderful potential of beta-amino acids was exploited to create various conformational modifications at the vital positions three and four of the parent peptide. The impact around the opioid binding affinity was evaluated, by means of ligand stimulated binding Axitinib assays, which indicated a large nanomolar affinity toward the mu-receptor, with appreciable mu/delta selectivity, for a number of the brand new compounds. The three-dimensional properties of the higher affinity mu opioid receptor (MOR) ligands had been investigated by proton nuclear magnetic resonance, molecular dynamics, and docking research. In solution, the structures showed extended conformations, that are in agreement using the frequently accepted pharmacophore model for EM-2. Bicalutamide supplier From docking studies on an active kind of the MOR model, distinctive ligand-receptor interactions are already identified, therefore confirming the capability of active compounds to assume a biologically lively conformation.