… Opioid receptors are peptide GPCRs whose binding sites display a more complex interaction
interface than those of receptors for small molecules. … the discovery of novel chemotypes …

… selective for δOR over the µ- and κ-opioid receptors (µOR … in the presence of small molecule
agonists and the implementation … with the purpose of finding molecules that underrecruit β-…

… antagonists have shown efficacy in the treatment of anxiety and depression. This review
summarizes the history, design strategy, discovery, … opioid receptors are expressed throughout …

… Diverse discovery strategies of KOR ligands targeting natural, … scaffolds, as small molecules
or peptides, with short or long-… knowledge into the discovery of novel bioactive molecules. …

… former chemotypes can be respectively subdivided into those … the possibility of discovering
DOP agonists that maintain their … opioid receptor antagonist) but not by CTOP (selective MOP …

… µ opioid receptor (µOR), which is activated by small molecules … This approach has yielded
many novel chemotypes across several … of the small molecule agonist DPI-287 and antagonist …

… analgesia and opioid-related adverse effects through the … used opioid analgesics belong
to one of six main chemotypes, … by acting as agonists at one or more opioid receptor types, …

… Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes
through a HTS and Hit Refinement Strategy. ACS Chem Neurosci 2012, 3, 221–236. (18) …

… Through a small-scale high-throughput screening assay, this … in the Schrödinger small
molecule drug discovery platform (… DPI-287 (PDB: 6PT3) and the antagonist-bound (PDB: 4N6H) X…

… This new chemotype bears the potential for favorable … 3D query pharmacophores to discover
novel ligands at the MOR. … A and various small molecules KOR antagonists (Table 4). In …