Table 1 Affinities (IC50 values) of the PSMA inhibitors in this study as determined in a competitive binding assay on LNCaP cells (150,000 cells/well, 4 °C, 1 h, c(125I-IBA) = 0.2 nM as the reference ligand). Data are expressed as mean ± SD (n = 3). *Data were taken from Ref. [17]
PSMA inhibitor | PSMA inhibitors (amino acid code) | IC50 |
|---|---|---|
1 | Ac-YFK(Sub-KuE) | 15.0 ± 1.3 |
2 | Ac-YWK(Sub-KuE) | 6.8 ± 3.3 |
3 | Ac-Y-(Benzothienyl-A)K(Sub-KuE) | 10.2 ± 4.0 |
4 | Ac-Y-(Biphenyl-A)K(Sub-KuE) | 139.4 ± 117.0 |
5 | Ac-Y-1-Nal-K(Sub-KuE) | 4.3 ± 0.9 |
6 | Ac-Y-2-Nal-K(Sub-KuE) | 3.9 ± 1.7 |
7 | Ac-Y(4-NO2-F)K(Sub-KuE) | 7.4 ± 0.5 |
8 | Ac-Y(3,5-di-I-Y)K(Sub-KuE) | 3.8 ± 0.6 |
9 | Ac-Y(3-CH3-Y)K(Sub-KuE) | 7.2 ± 0.9 |
PSMA I&T | DOTAGA-(I-y)fk(Sub-KuE) | 10.2 ± 3.5* |
natGa-PSMA I&T | natGa-DOTAGA-(I-y)fk(Sub-KuE) | 9.3 ± 3.3* |
natLu-PSMA I&T | natLu-DOTAGA-(I-y)fk(Sub-KuE) | 7.9 ± 2.4* |
10 | DOTAGA-y-2-nal-k(Sub-KuE) | 8.5 ± 2.5 |
natGa-10 | natGa-DOTAGA-y-2-nal-k(Sub-KuE) | 9.8 ± 3.2 |
natLu-10 | natLu-DOTAGA-y-2-nal-k(Sub-KuE) | 2.1 ± 0.8 |
11 | DOTAGA-y-2-nal-k((I-f)-Glut-KuE) | 4.6 ± 0.9 |
natGa-11 | natGa-DOTAGA-y-2-nal-k((I-f)-Glut-KuE) | 9.3 ± 2.9 |
natLu-11 | natLu-DOTAGA-y-2-nal-k((I-f)-Glut-KuE) | 6.1 ± 1.6 |