Table 5 Combined analogues.

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

  Ring A Ring B hSUCNR1 mSUCNR1 ClogPb
pEC50 (efficacy, %)a
28 6.79 ± 0.12 (58.0 ± 2.7) 5.92 ± 0.09 (64.0 ± 2.5) 2.01
29 6.85 ± 0.19 (52.6 ± 3.9) 6.74 ± 0.13 (71.2 ± 3.2) 1.07
30 7.23 ± 0.14 (49.2 ± 2.7) 5.84 ± 0.16 (45.3 ± 3.4) 3.11
31 7.64 ± 0.13 (61.7 ± 2.5) 6.75 ± 0.09 (69.9 ± 2.2) 2.18
32 7.23 ± 0.23 (88.7 ± 6.1) 7.00 ± 0.09 (68.1 ± 2.5) 1.86
33 7.23 ± 0.37 (66.4 ± 7.2) 7.29 ± 0.18 (61.5 ± 3.8) 2.13