Identification of 3-Acetyl-2-aminoquinolin-4-one as a Novel, Nonpeptidic Scaffold for Specific Calpain Inhibitory Activity
Da-Hye Kang
Kyu-Yeon Jun
Jin Pyo Lee
Chwang Siek Pak
Younghwa Na
Youngjoo Kwon
10.1021/jm8014734.s001
https://acs.figshare.com/articles/journal_contribution/Identification_of_3_Acetyl_2_aminoquinolin_4_one_as_a_Novel_Nonpeptidic_Scaffold_for_Specific_Calpain_Inhibitory_Activity/2857135
A series of 3-acetyl-2-aminoquinolin-4-one derivatives selected from the Korean Chemical Bank were screened for calpain inhibitory activity by using a high-throughput fluorimetric calpain assay. We identified a potent and selective μ-calpain inhibitor, compound <b>17</b>, whose specificity and efficacy for μ-calpain inhibition was better than MDL28170. Docking studies revealed that the efficacy of its inhibitory effect on calpain depended on the size and charge properties of the substitutions on the phenylamino ring.
2009-05-14 00:00:00
Nonpeptidic Scaffold
charge properties
efficacy
MDL 28170. Docking studies
Korean Chemical Bank
phenylamino ring
calpain
Specific Calpain Inhibitory ActivityA series