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Article

Discovery of CN-3 as a Next-Generation RET Inhibitor Potently Overcoming Multiple Mutations.

Journal of medicinal chemistry - 14 May 2026

Wang Zi-Xuan, He Rui, Chen Min-Hui, Yang Kun, Liu Qian, Yang Jin, Zhang Meng-Yuan, Qiao Nuo, Zhou Ming-Dan, Yu Yan-Cheng, Sun Shan-Liang, Lai Yuan-Hui, Yang Ye, Zhang Zhang, Li Nian-Guang, Shi Zhi-Hao

Abstract excerpt

RET fusions and activating mutations drive multiple human cancers, while resistance mutations limit the efficacy of current selective RET inhibitors. Here, we report CN-3, a potent RET inhibitor active against clinically relevant mutants, including solvent-front (G810R/S/C), gatekeeper (V804M), hinge (Y806H), and catalytic loop (M918T) variants. CN-3 inhibited all tested RET mutants (IC50 < 5 nM) and selectively...

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Source

Identifiers

PMID: 42068291
DOI: 10.1021/acs.jmedchem.6c00376

Genes

RET
F3

Variants

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 8 Sept 2026.

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