Structure–activity optimization of N -arylindole GPR52 agonists for enhanced antipsychotic efficacy: design, synthesis, and pharmacological evaluation

RSC Medicinal Chemistry 2026 Open access

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Authors: Xiaojie Hu, Qingshan Gu, Qiuyu Xiong, Donglei Chen, Qingkun Wu, Lu Zheng
DOI: 10.1039/d5md00944h
Cited by: 3
References: 26

Abstract

. Structure-activity relationship studies revealed that balanced flexibility and hydroxyl group incorporation were critical for activity. Molecular docking confirmed stable binding interactions with GPR52's "bird's claw" pocket, while ADMET predictions supported favorable drug-like properties. These designed small molecules will facilitate the development of novel GPR52 agonists.

Fields of Study & Subjects

Receptor Mechanisms and Signaling Diabetes Treatment and Management Neurotransmitter Receptor Influence on Behavior

Publication details

Journal / source
RSC Medicinal Chemistry
Publisher
Royal Society of Chemistry (RSC)
Volume
17
Issue
3
Pages
1749–1757
Publication date
1 January 2026
Language
EN