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EJNMMI Radiopharmacy and Chemistry

Table 2 Kinetics evaluation of the three compounds, performed with 1–3 nM radioligand

From: Preclinical evaluation of new GRPR-antagonists with improved metabolic stability for radiotheranostic use in oncology

[111In]In-AU-SAR-

ka1(1/(M*s))

kd1 (1/s)

KD1 (nM)

ka2 (1/(M*s))

kd2 (1/s)

KD2 (nM)

M1

1.4 × 104

5.4 × 10–6

0.39

1.9 × 105

2.1 × 10–4

1.1

M2

1.8 × 105

5.5 × 10–6

0.031

   

M3

1.5 × 104

4.4 × 10–6

0.30

3.1 × 105

3.4 × 10–4

1.1

  1. ka = rate of association (1/(M*s)), kd = rate of dissociation (1/s), KD = equilibrium dissociation constant (nM)
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