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. 2018 Oct 24;9(11):1099–1104. doi: 10.1021/acsmedchemlett.8b00318

Table 1. PSMA Inhibitory Activity of Compounds 7ac, 8ab, 9ab, 10, 9ab, 12, 13ab, 14, 15, 21ab, and 22aba.

compd IC50 (nM) compd IC50 (nM)
7a 2.32 ± 0.55 12 0.20 ± 0.11
7b 2.91 ± 0.33 13a 0.99 ± 0.05
7c 2.11 ± 1.01 13b 0.075 ± 0.005
8a 0.64 ± 0.07 14 1.31 ± 0.18
8b 0.46 ± 0.10 15 1.19 ± 0.73
9a 5.24 ± 1.45 21a 0.94 ± 0.26
9b 5.44 ± 2.54 21b 0.15 ± 0.02
10 4.46 ± 1.03 22a 1.11 ± 0.22
11a 0.35 ± 0.01 22b 0.13 ± 0.01
11b 0.28 ± 0.09 16 (DCIBzL) 0.021 ± 0.004
a

Inhibition constants of studied compounds were determined using the radioenzymatic assay with [3H]NAAG (radiolabeled at the terminal glutamate) as described previously.22