TABLE 2

PSMA Inhibition Potencies (Expressed as Ki) and Specific Internalization Values

CompoundKi (nM)Specific cell surfaceSpecific lysate
CA0021.9 ± 0.7048 ± 3.916 ± 2.4
CA0031.6 ± 0.5294 ± 6.935 ± 2.8
CA00415 ± 0.8945 ± 3.413 ± 2.2
CA0051.8 ± 0.6541 ± 4.319 ± 4.5
CA02212 ± 2.0123 ± 2239 ± 6.7
CA02314 ± 2.0103 ± 6.628 ± 8.7
CA02421 ± 4.035 ± 5.88.6 ± 7.0
CA02514 ± 1.768 ± 1116 ± 8.0
CA0264.4 ± 1.696 ± 1624.5 ± 14
PSMA-6172.3 ± 2.945 ± 3.615 ± 3.0
  • Data are mean ± SD (n = 3). Internalization is expressed as percentage injected activity per 106 cells.