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Table 1 Percent inhibition of the synthesized 4,6-substituted 2-amino-pyridin-3-carbonitriles at 10 µM (PDE10A) or IC50 (µM) and percentage displacement at 0.1 µM (A1R and A2AR), or Ki

From: Computer-aided design of multi-target ligands at A1R, A2AR and PDE10A, key proteins in neurodegenerative diseases

  1. IC50 values of the 2-aminopyridines-3-carbonitriles were measured for the four phosphodiesterases PDE7A, PDE7B, PDE9A and PDE10A at 10 μM concentration. For those compounds that showed percentage inhibition greater than 70% and selectivity against other measured isoenzymes, IC50 were determined. Calculation of the Ki values at A1R, A2AR, A2BR and A3R was approximated using the Cheng-Prusoff equation: Ki = IC50/[1 + (C/KD)], where IC50 is the concentration of compound that displaces the binding of the radioligand by 50%, C is the concentration of radioligand, and KD is the dissociation constant of each radioligand