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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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Autores principales: Chou, Tsui-Fen, Li, Kelin, Frankowski, Kevin J, Schoenen, Frank J, Deshaies, Raymond J
Formato: Artigo
Lenguaje:Inglês
Publicado: WILEY-VCH Verlag 2013
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Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC3662613/
https://ncbi.nlm.nih.gov/pubmed/23316025
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/cmdc.201200520
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