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. Author manuscript; available in PMC: 2015 Dec 1.
Published in final edited form as: Eur J Med Chem. 2014 Sep 8;86:714–723. doi: 10.1016/j.ejmech.2014.09.023

Table 1.

RET SAR for compounds 6a–g and 13a–g.a

<!–Col Count:2– > Compound RET IC50 (µM)
6a >100
6b >100
6c >100
6d 67.8 ± 1.1
6e 18.8 ± 4.6
6f 15.7 ± 2.9
6g 0.21 ± 0.04
13a 22.3 ± 7.7
13b 20.4 ± 5.6
13c 19.3 ± 2.8
13d 17.2 ± 3.1
13e 14.3 ± 1.9
13f 9.1 ± 2.6
13g 0.75 ± 0.03
Vandetanib 0.102 ± 0.008
a

IC50 values represent the concentration required to inhibit enzyme activity by 50%. The screening was completed at 9 µM ATP concentration in duplicate.