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

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5% @10−4M

11% @10−4M

1.28

9

25% @10−4M

15% @10−4M

2.44

  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).
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