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Table 1 PSMA affinities (IC 50 ) of the compounds investigated

From: Synthesis and preclinical evaluation of DOTAGA-conjugated PSMA ligands for functional imaging and endoradiotherapy of prostate cancer

Ligand IC50[nM]
HBED-CC-Ahx-KuE   5.7 ± 0.5
[natGa]HBED-CC-Ahx-KuE   6.1 ± 0.8
DOTA-FFK(Sub-KuE) (10) 13.1 ± 2.3
[natGa]DOTA-FFK(Sub-KuE) (natGa-10) 29.5 ± 6.6
[natLu]DOTA-FFK(Sub-KuE) (natLu-10) 54.7 ± 6.1
DOTAGA-FFK(Sub-KuE) (11) 10.2 ± 1.5
[natGa]DOTAGA-FFK(Sub-KuE) (natGa-11) 12.1 ± 3.9
[natLu]DOTAGA-FFK(Sub-KuE) (natLu-11) 15.1 ± 1.5
DOTAGA-ffk(Sub-KuE) (12) 13.9 ± 0.4
[natGa]DOTAGA-ffk(Sub-KuE) (natGa-12) 15.9 ± 0.5
[natLu]DOTAGA-ffk(Sub-KuE) (natLu-12) 13.1 ± 2.2
  1. Binding assays were performed using LNCaP cells (150,000/well) and ([125I]I-BA)KuE (c = 0.2 nM) as the radioligand. Cells were incubated in HBSS (1% BSA) at 4°C for 1h. Data are expressed as mean ± SD (n = 3).