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.
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