Table 1 Investigation of miscellaneous amide analogues.

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

  R hSUCNR1 mSUCNR1 ClogPb
pEC50 (efficacy, %)a
3 5.75 ± 0.08 (72.8 ± 2.6) 6.46 ± 0.06 (79.3 ± 1.6) 1.66
4 4.53 ± 0.13 (78.1 ± 7.5) 4.93 ± 0.05 (95.8 ± 2.9) 0.44
5 22% @10−4M 13% @10−4M 0.28
6 50% @10−4M 64% @10−4M 1.52
7 8% @10−4M 15% @10−4M 1.26
8 5% @10−4M 11% @10−4M 1.28
9 25% @10−4M 15% @10−4M 2.44