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. 2010 Dec;78(6):1105–1123. doi: 10.1124/mol.110.067207

TABLE 4.

Chemical optimization of VU0092273 combining optimal findings from each library

graphic file with name zmo012106260g009.jpg

Compound graphic file with name zmo012106260g017.jpg X Y Potency (EC50) Efficacy K i
nM % Glu Max nM
VU0366030 graphic file with name zmo012106260g010.jpg 3-F CH 23 ± 6 82 ± 8 1440 ± 150
VU0366027 graphic file with name zmo012106260g011.jpg 3-F CH 7.1 ± 2.1 72 ± 6 1580 ± 210
VU0366031 graphic file with name zmo012106260g012.jpg 3-F CH 3.8 ± 1.1 98 ± 8 40 ± 12
VU0366028 graphic file with name zmo012106260g013.jpg 3,4-difluoro CH 25 ± 5 103 ± 6 390 ± 50
VU0366029 graphic file with name zmo012106260g014.jpg 3-F CH 65 ± 16 104 ± 3 980 ± 20
VU0360175 graphic file with name zmo012106260g015.jpg 3-F N 49 ± 7 105 ± 4 N.D.
VU0360172 graphic file with name zmo012106260g016.jpg 3-F N 16 ± 6 87 ± 3 195 ± 20