Recently we described an innovative class of non-peptide CCK1 antagonists keeping appropriate pharmacophoric groups on the anthranilic
acid employed as a molecular scaffold. The lead compound obtained, VL-0395, characterized by the presence of Phe and the 2-indole moiety
at the C- and N-termini of anthranilic acid, respectively, is endowed with submicromolar affinity towards CCK1 receptors. Thus, we have
prepared and tested on CCK receptors a library of VL-0395 analogues in order to investigate the precise topological and essential key
interactions of the 2-indole group of the lead with the CCK1 receptor. The obtained results confirm that this group establishes very specific
interactions with this receptor sub-site and may be viewed as a “needle” group.
