PSMA Inhibition Potencies (Expressed as Ki) and Specific Internalization Values
Compound | Ki (nM) | Specific cell surface | Specific lysate |
CA002 | 1.9 ± 0.70 | 48 ± 3.9 | 16 ± 2.4 |
CA003 | 1.6 ± 0.52 | 94 ± 6.9 | 35 ± 2.8 |
CA004 | 15 ± 0.89 | 45 ± 3.4 | 13 ± 2.2 |
CA005 | 1.8 ± 0.65 | 41 ± 4.3 | 19 ± 4.5 |
CA022 | 12 ± 2.0 | 123 ± 22 | 39 ± 6.7 |
CA023 | 14 ± 2.0 | 103 ± 6.6 | 28 ± 8.7 |
CA024 | 21 ± 4.0 | 35 ± 5.8 | 8.6 ± 7.0 |
CA025 | 14 ± 1.7 | 68 ± 11 | 16 ± 8.0 |
CA026 | 4.4 ± 1.6 | 96 ± 16 | 24.5 ± 14 |
PSMA-617 | 2.3 ± 2.9 | 45 ± 3.6 | 15 ± 3.0 |
Data are mean ± SD (n = 3). Internalization is expressed as percentage injected activity per 106 cells.