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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]

From: Synthesis and in vitro and in vivo evaluation of urea-based PSMA inhibitors with increased lipophilicity

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