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Structure–Activity Relationship Study Reveals ML240 and ML241 as Potent and Selective Inhibitors of p97 ATPase

To discover more potent p97 inhibitors, we carried out a structure–activity relationship study of the quinazoline scaffold previously identified from our HTS campaigns. Two improved inhibitors, ML240 and ML241, inhibit p97 ATPase with IC(50) values of 100 nm. Both compounds inhibited degradation of...

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Detalles Bibliográficos
Autores principales: Chou, Tsui-Fen, Li, Kelin, Frankowski, Kevin J, Schoenen, Frank J, Deshaies, Raymond J
Formato: Online Artículo Texto
Lenguaje:English
Publicado: WILEY-VCH Verlag 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3662613/
https://www.ncbi.nlm.nih.gov/pubmed/23316025
http://dx.doi.org/10.1002/cmdc.201200520