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2751856 
Journal Article 
Correspondence analysis of protein kinase C (PKC) inhibition by bis-basic substituted benzamides 
Gilbert, J; Cheminant, M; Bignon, E; Pons, M; Dore, JC; Et al 
1998 
Yes 
Drug Design and Discovery
ISSN: 1055-9612 
IPA/99/1178425 
Discov 
REF 45 
253-267 
English 
IPA COPYRIGHT: ASHP A novel series of bis-basic substituted benzamides were synthesized and the relative potency of the compounds in inhibiting rat brain protein kinase alpha activity was determined using multivariate factor analysis (correspondence analysis). None of the compounds inhibited enzyme activity via the catalytic domain, but several did via the regulatory domain at concentrations of 1-5 mum. Inhibition was comparable to that of several di- and triphenylacrylonitriles and triphenylethylenes. Hydrophobicity and hydration energy were the most discriminant descriptors. Inhibitory activity was correlated with high hydrophobicity and low hydration energy.