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. Author manuscript; available in PMC: 2011 Sep 15.
Published in final edited form as: J Am Chem Soc. 2010 Sep 15;132(36):12711–12716. doi: 10.1021/ja104591m

Table 1.

Linker length dependence on PSMA inhibitory potency.

graphic file with name nihms231059t1.jpg
Compound X n IC50 (nM)b Ki (nM)c
1, ARM-P0 DNPa 0 1.76 ± 0.41 0.078 ± 0.018
2, ARM-P1 DNP 1 1.05 ± 0.11 0.047 ± 0.005
3, ARM-P2 DNP 2 0.54 ± 0.18 0.024 ± 0.008
4, ARM-P4 DNP 4 0.46 ± 0.18 0.020 ± 0.008
5, ARM-P6 DNP 6 2.29 ± 0.60 0.101 ± 0.027
6, ARM-P8 DNP 8 3.29 ± 1.14 0.145 ± 0.050
7, ARM-P12 DNP 12 37.3 ± 16.2 1.65 ± 0.72
8, MeO-P0 OMe 0 30.5 ± 12.1 1.35 ± 0.54
9, MeO-P2 OMe 2 40.8 ± 9.4 1.81 ± 0.42
10, MeO-P4 OMe 4 30.2 ± 14.4 1.34 ± 0.64
11, MeO-P8 OMe 8 131.0 ± 57.6 5.79 ± 2.54
12, MeO-P12 OMe 12 165.2 ± 58.9 7.30 ± 2.60
a

a

b

IC50 values represent the mean of triplicate experiments.

c

Ki values were calculated from IC50 and Km values using the Cheng-Prusoff equation as described in the supporting information.