Kim, Doyoung Lee, Jieon Kwag, Rina Kim, Hyunbin Oh, Hyunji Moon, Bongjin Kim, Hak Joong Seong, Jihye Jeon, Byungsun Kang, Taek Choo, Hyunah 2024-01-19T13:02:43Z 2024-01-19T13:02:43Z 2022-01-10 2022-01 0253-2964 https://pubs.kist.re.kr/handle/201004/115913 There has been much attention to biased ligands of G protein-coupled receptors (GPCRs) for potential pharmacological benefits. Recently, we reported N-((6-chloro-2'-methoxy-[1,1'-biphenyl]-3-yl)methyl)ethanamine 1 as G protein-biased agonist of 5-HT7R, which could be used as a chemical probe for the study on treatment discovery of autism spectrum disorder. Herein, we describe the synthesis of derivatives of the compound 1 and their biological evaluations in both G protein and beta-arrestin signaling pathway. Total 16 compounds were synthesized and evaluated, and the compounds 3c, 3f, 3i, and 3p could be called as G protein-biased agonists like the compound 1. Among the four compounds, the compound 3c was the best in efficacy with an E-max value of 73% and the compound 3f was the most potent agonist with an EC50 value of 0.094 mu M. English 대한화학회 N-(Biphenyl-3-ylmethyl)ethanamines as G protein-biased agonists of 5-HT7R Article 10.1002/bkcs.12427 1 Bulletin of the Korean Chemical Society, v.43, no.1, pp.73 - 77 Bulletin of the Korean Chemical Society 43 1 73 77 N scie scopus kci ART002805786 000715579100001 2-s2.0-85118581548 Chemistry, Multidisciplinary Chemistry Article AUTISM SPECTRUM DISORDER RECEPTORS CLONING 5-HT7R autism G protein-biased ligand partial agonist serotonin receptor