TABLE 1

Granisetron orientation in docked models

Docking simulations were carried out using AutoDock as described under Materials and Methods. The orientation of granisetron in the binding site of the four clusters with highest affinity was examined to determine which portions of the ligand were near Trp90 and Arg92.

Cluster Frequency Ki At Indazole At Tropane
nM
1 0.6 2.6 Trp90 Arg92
2 0.2 3.4 Trp90 Arg92
3 0.1 4.6 Trp90 Arg92
4 0.1 5.5 Arg92 Trp90