Table 2 Investigation of ring A.

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

  Ring A hSUCNR1 mSUCNR1 ClogPb
pEC50 (efficacy, %)a
3c 5.75 ± 0.08 (72.8 ± 2.6) 6.46 ± 0.06 (79.3 ± 1.6) 1.66
10 5.29 ± 0.19 (81.6 ± 8.4) 6.16 ± 0.11 (81.3 ± 3.6) 1.47
11 5.27 ± 0.18 (94.7 ± 8.7) 6.13 ± 0.10 (76.7 ± 3.1) 1.67
12 5.02 ± 0.10 (91.9 ± 5.3) 6.07 ± 0.09 (81.6 ± 3.0) 1.97
13 6.33 ± 0.14 (69.1 ± 3.9) 6.83 ± 0.11 (73.2 ± 2.7) 1.97
14 4.81 ± 0.20 (74.2 ± 11.8) 5.71 ± 0.09 (79.6 ± 3.7) 0.43
15 6.13 ± 0.14 (71.1 ± 4.2) 6.82 ± 0.08 (74.8 ± 2.0) 0.87
16 5.29 ± 0.15 (103.8 ± 7.9) 6.14 ± 0.10 (78.1 ± 3.1) 0.89
17 6.41 ± 0.14 (85.3 ± 4.5) 7.39 ± 0.07 (84.2 ± 1.8) 1.45
18 6.55 ± 0.25 (81.0 ± 7.2) 6.81 ± 0.17 (80.6 ± 4.6) 2.43
19 6.39 ± 0.11 (72.1 ± 3.2) 6.79 ± 0.06 (76.0 ± 1.5) 1.00