Table 3 Alkoxy analogues.

From: Structure-Activity Investigations and Optimisations of Non-metabolite Agonists for the Succinate Receptor 1

  R hSUCNR1 mSUCNR1 ClogPb
pEC50 (efficacy, %)a
17c Me 6.41 ± 0.14 (85.3 ± 4.5) 7.39 ± 0.07 (84.2 ± 1.8) 1.45
20 F3C 6.99 ± 0.15 (61.7 ± 3.6) 6.72 ± 0.11 (69.7 ± 2.8) 3.17
21 Et 6.59 ± 0.14 (56.3 ± 3.1) 7.44 ± 0.09 (70.2 ± 2.0) 1.98
22 iPr 6.84 ± 0.14 (69.6 ± 4.3) 7.29 ± 0.07 (75.6 ± 1.7) 2.29
23 6.27 ± 0.11 (76.5 ± 3.1) 6.97 ± 0.07 (82.4 ± 1.9) 1.81
24 6.10 ± 0.09 (63.9 ± 2.4) 7.33 ± 0.09 (74.6 ± 2.1) 0.53
  1. apEC50 values were determined from dose-response curves of induction of IP3 turnover in SUCNR1 transfected HEK cells (N = 3), efficacy is determined relative to succinate (100%). bCalculated by BioByte’s algorithm as implemented in ChemDraw Professional 16.0.1.4 (ClogP option). cDuplication of data from Table 2.