Name: GNE-274
Rating: 5 (10 reviews)

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HIT ID:HIT214323366
Cas No:2369048-69-9
常用名:GNE-274
IUPAC:(2S)-3-(3-hydroxyphenyl)-4-methyl-2-{4-[(1-propylazetidin-3-yl)methoxy]phenyl}-2H-chromen-6-ol
IUPAC:(2S)-3-(3-hydroxyphenyl)-4-methyl-2-{4-[(1-propylazetidin-3-yl)methoxy]phenyl}-2H-chromen-6-ol
InChI key:ABSGIUXAPWSTBC-LJAQVGFWSA-N

分子式:C29H31NO4
分子量:457.57
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:CCCN1CC(COc2ccc(cc2)[C@@H]2Oc3ccc(O)cc3C(C)=C2c2cccc(O)c2)C1 |c:26|
SMILES:CCCN1CC(COc2ccc(cc2)[C@@H]2Oc3ccc(O)cc3C(C)=C2c2cccc(O)c2)C1 |c:26|

GNE-274, a non-degrader compound structurally similar to GDC-0927 (an ER degrader), serves as a partial ER agonist in breast cancer cell lines without triggering ER turnover. Notably, GNE-274 enhances chromatin accessibility at ER-DNA binding sites, unlike GDC-0927. Acting as a potent inhibitor of the ER-ligand binding domain (LBD), GNE-274 exhibits potential for cancer research purposes.

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