Live Cell-Binding Affinity of Small Molecules Targeted to PSMA
| Live cell-binding affinity (nM)* | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Molecule | Description | Metal conjugate | M.W. | Net charge (pH 7.0) | Charge-to-mass ratio (× 10−3) | LNCaP cells (TBS) | LNCaP cells (PBS) | LNCaP cells (serum) | PC-3 cells (TBS) | TsuPR1 cells (TBS) |
| I | GPI | None | 311.2 | −3 | −9.6 | 10.4 ± 0.3 | ND | ND | ND | ND |
| Ia | GPI | Re-MAS3 | 844.7 | −4 | −4.7 | 35.5 ± 0.1 | ND | ND | ND | ND |
| IIa | AdamGPI monomer | Re-MAS3 | 1,307.3 | −6 | −4.6 | 31.3 ± 0.4 | ND | ND | ND | ND |
| IIIa | AdamGPI dimer | Re-MAS3 | 1,600.5 | −9 | −5.6 | 14.4 ± 1.4 | 20.3 ± 1.5 | 17.4 ± 1.0 | ND | ND |
| IV | AdamGPI trimer | None | 1,359.5 | −11 | −8.1 | 0.4 ± 0.1 | 0.5 ± 0.2 | 0.7 ± 0.2 | ND | ND |
| IVa | AdamGPI trimer | Re-MAS3 | 1,893.5 | −12 | −6.3 | 3.3 ± 0.1 | 2.9 ± 0.1 | 2.1 ± 0.1 | ND | ND |
↵* Mean affinity ± 95% confidence interval from 3 independent experiments is shown.
ND = None detected.